GLP-1 receptor

体外活性：阿必鲁肽是一种小蛋白质/肽，由两个拷贝的修饰人 GLP-1（片段 7-36）的 30 个氨基酸序列组成，用甘氨酸取代 8 位天然存在的丙氨酸进行修饰。以增强对 DPP-4 的抵抗力。

单剂量阿必鲁肽后，由于该分子与 GLP-1 受体结合，24 小时内就会产生降血糖作用。空腹和餐后血糖水平的降低与剂量相关。阿必鲁肽的效力不如 GLP-1。在糖尿病动物模型中，阿必鲁肽给药可刺激 β 细胞质量增加。 2型糖尿病患者皮下注射单次30毫克剂量后，3-5天内达到最大浓度，半衰期为3.6-6.8天。单剂量阿必鲁肽后的表观分布容积为8.2-18.5 L。阿必鲁肽在循环中的最终命运是降解成小肽和单个氨基酸。阿必鲁肽对雄性食蟹猴的心血管功能、心率、心电图间隔或呼吸功能没有明显影响，并且没有产生任何心电图异常或心律失常的证据。此外，对神经行为功能评估没有阿必鲁肽相关的影响。阿必鲁肽不会穿过血脑屏障到达饱腹感中枢。阿必鲁肽可减少心肌梗死面积，改善心肌 I/R 损伤后的心脏功能和能量学，这与心肌葡萄糖摄取增强以及通过增加葡萄糖和乳酸氧化向更有利的底物代谢转变有关。

Absorption, Distribution and Excretion
Maximum concentrations of albiglutide were reached at 3 to 5 days post-dosing following a single 30mg dose. The mean peak concentration (Cmax) and mean area under the time-concentration curve (AUC) of albiglutide were 1.74 mcg/mL and 465 mcg.h/mL, respectively
11 L.
67 mL/h.
/MILK/ It is not known whether albiglutide is distributed into milk in humans ... .
Albiglutide is a glucagon-like peptide-1 analogue composed of tandem copies of modified human glucagon-like peptide-1 (7-36) coupled to recombinant human albumin that is approved in adults for the treatment of type 2 diabetes mellitus. After subcutaneous administration, albiglutide is likely primarily absorbed via the lymphatic circulation, with maximum concentrations being reached in 3 to 5 days; steady-state exposures are achieved following approximately 4 to 5 weeks of once-weekly administration. The elimination half-life of albiglutide is approximately 5 days. Clearance of albiglutide is 67 mL/h with between-subject variability of 34.9%; no covariates have been identified that would require dose adjustment of albiglutide. Albiglutide lowers the fasting plasma glucose and reduces postprandial glucose excursions. In addition, beta-cell secretion is enhanced by albiglutide during hyperglycemia, whereas secretion is suppressed during hypoglycemia; alpha-cell response to hypoglycemia is not impaired by albiglutide. Albiglutide does not prolong the corrected QT interval but has a modest effect on heart rate in patients with type 2 diabetes mellitus. Dose adjustment is not suggested in patients with renal impairment, but experience in patients with severe renal impairment is very limited, and it is recommended that albiglutide be used with care in such patients due to an increased frequency of diarrhea, nausea, and vomiting. No clinically relevant drug interactions have been observed in clinical trials.
Following SC administration of a single 30-mg dose to subjects with type 2 diabetes mellitus, maximum concentrations of albiglutide were reached at 3 to 5 days post-dosing. The mean peak concentration (C max) and mean area under the time-concentration curve (AUC) of albiglutide were 1.74 mcg/mL and 465 mcg.h/mL, respectively, following a single dose of 30 mg albiglutide in type 2 diabetes mellitus subjects. Steady-state exposures are achieved following 4 to 5 weeks of once-weekly administration. Exposures at the 30-mg and 50-mg dose levels were consistent with a dose-proportional increase. Similar exposure is achieved with SC administration of albiglutide in the abdomen, thigh, or upper arm. The absolute bioavailability of albiglutide following SC administration has not been evaluated. The mean estimate of apparent volume of distribution of albiglutide following SC administration is 11 L. As albiglutide is an albumin fusion molecule, plasma protein binding has not been assessed. The mean apparent clearance of albiglutide is 67 mL/hr with an elimination half-life of approximately 5 days, making albiglutide suitable for once-weekly administration.

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Metabolism / Metabolites
Biotransformation studies have not been performed. Because albiglutide is an albumin fusion protein, it likely follows a metabolic pathway similar to native human serum albumin, which is catabolized primarily in the vascular endothelium.
Albiglutide is a protein for which the expected metabolic pathway is degradation to small peptides and individual amino acids by ubiquitous proteolytic enzymes. Classical biotransformation studies have not been performed. Because albiglutide is an albumin fusion protein, it likely follows a metabolic pathway similar to native human serum albumin which is catabolized primarily in the vascular endothelium.

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Biological Half-Life
4-7 days.
The elimination half-life of albiglutide following subcutaneous administration is 5 days, making the drug suitable for once-weekly administration.

Toxicity Summary
IDENTIFICATION AND USE: Albiglutide (trade name: Tanzeum) is a prescription medication approved to improve glycemic control in adults with type 2 diabetes mellitus. HUMAN EXPOSURE AND TOXICITY: In epidemiological meta-analyses, pancreatitis and thyroid cancer were observed, but it was not clear if they were related to the treatment. Additional adverse events included gastrointestinal symptoms (nausea, vomiting, and diarrhea), and hypoglycemia. In patients treated with GLP-1 receptor agonists, there have been post marketing reports of acute renal failure and worsening of chronic renal failure, which may sometimes require hemodialysis. Some of these events were reported in patients without known underlying renal disease. The risk of hypoglycemia is increased when albiglutide is used in combination with insulin secretagogues (e.g., sulfonylureas) or insulin. In clinical trials, acute pancreatitis has been reported in association with albiglutide. There may be an increased risk of thyroid C-cell tumors in patients treated with albiglutide. Albiglutide is an agonist of the GLP-1 receptor and augments glucose-dependent insulin secretion. Albiglutide also slows gastric emptying. ANIMAL STUDIES: Carcinogenicity of albiglutide could not be assessed in rodents, but other glucagon-like peptide-1 (GLP-1) receptor agonists have caused thyroid C-cell tumors in rodents at clinically relevant exposures. Human relevance of GLP-1 receptor agonist induced C-cell tumors in rodents has not been determined. In pregnant mice given subcutaneous doses from gestation Day 6 through 15 (organogenesis), embryo-fetal lethality (post-implantation loss) and bent (wavy) ribs were observed, in addition to maternal toxicity (body weight loss and reduced food consumption). Offspring exhibited reduced body weight pre-weaning, dehydration and coldness, and a delay in balanopreputial separation. Increased mortality and morbidity were seen at all doses in lactating females. Reduced weight gain in the pups was also observed during the treatment period. In a mouse fertility study, reductions in estrous cycles were observed at 50 mg/kg/day, a dose associated with maternal toxicity (body weight loss and reduced food consumption). Females were treated with SC doses for 7 days prior to cohabitation with males, and continuing through mating. Reductions in estrous cycles were observed.

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Hepatotoxicity
In large clinical trials, serum enzyme elevations were no more common with albiglutide therapy than with placebo or comparator agents, and no instances of clinically apparent liver injury were reported. Since licensure, there have been no published case reports of hepatotoxicity due to albiglutide and the product label does not list liver injury as an adverse event. Thus, liver injury due to albiglutide must be rare, if it occurs at all.
Likelihood score: E (unlikely cause of clinically apparent liver injury).

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Interactions
Potential pharmacokinetic interactions (altered absorption because of albiglutide-induced slowing of gastric emptying). In clinical trials, albiglutide did not affect the absorption of concomitantly administered oral drugs to any clinically relevant degree. However, caution should be exercised when albiglutide is administered concomitantly with oral drugs.
To review drug interaction studies of glucagon-like peptide-1 receptor agonists (GLP-1RAs) and concurrent oral medications. PubMed was searched (to December 5, 2011) using the terms exenatide, liraglutide, albiglutide, and lixisenatide. The AUCs of acetaminophen and lovastatin were decreased after exenatide administration and those of lisinopril and digoxin were decreased after liraglutide administration. In 10 studies, GLP-1RAs decreased the C(max) and, in 14 studies, prolonged the t(max) of study drug. Pharmacokinetic properties of drugs and differences in study design can explain differences in interaction potential. GLP-1RAs may produce clinically significant interactions with drugs that require achievement of target peak concentrations or a rapid onset of action. Studies in patients with type 2 diabetes are needed to further assess and allow comparison of several GLP-1RA agents' impact on steady-state pharmacokinetics and pharmacodynamics of concomitant oral medications.

[1]. Expert Opin Biol Ther . 2016 Dec;16(12):1557-1569.

Albiglutide is a glucagon-like peptide-1 agonist (GLP-1) biologic drug indicated in the treatment of type 2 diabetes. It is marketed under the brands Eperzan and Tanzeum by GSK (GlaxoSmithKline). It is a dipeptidyl peptidase-4-resistant glucagon-like peptide-1 dimer fused to human albumin. Albiglutide was approved on April 15, 2014 by the FDA.
Albiglutide is a recombinant DNA produced polypeptide analogue of human glucagon-like peptide-1 (GLP-1) which is used in combination with diet and exercise in the therapy of type 2 diabetes, either alone or in combination with other antidiabetic agents. There have been no published reports of hepatotoxicity attributed to albiglutide therapy.
Albiglutide is a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist, with antihyperglycemic activity. Albiglutide is composed of a GLP-1 (7-36) dimer fused to recombinant human albumin. Upon subcutaneous administration, this agent has a half-life of 4-7 days and resists degradation by dipeptidyl peptidase-4 (DPP-4).
See also: Albiglutide (annotation moved to).

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Drug Indication
Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Eperzan is indicated for the treatment of type 2 diabetes mellitus in adults to improve glycaemic control as: MonotherapyWhen diet and exercise alone do not provide adequate glycaemic control in patients for whom use of metformin is considered inappropriate due to contraindications or intolerance. Add-on combination therapyIn combination with other glucose-lowering medicinal products including basal insulin, when these, together with diet and exercise, do not provide adequate glycaemic control (see section 4. 4 and 5. 1 for available data on different combinations).
Treatment of type II diabetes mellitus

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Mechanism of Action
Albiglutide is an agonist of the GLP-1 (glucagon-like peptide 1) receptor and augments glucose-dependent insulin secretion. Albiglutide also slows gastric emptying.
Tanzeum is an agonist of the GLP-1 receptor and augments glucose-dependent insulin secretion. Tanzeum also slows gastric emptying.

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Therapeutic Uses
Incretins; Antidiabetic
/CLINICAL TRIALS/ ClinicalTrials.gov is a registry and results database of publicly and privately supported clinical studies of human participants conducted around the world. The Web site is maintained by the National Library of Medicine (NLM) and the National Institutes of Health (NIH). Each ClinicalTrials.gov record presents summary information about a study protocol and includes the following: Disease or condition; Intervention (for example, the medical product, behavior, or procedure being studied); Title, description, and design of the study; Requirements for participation (eligibility criteria); Locations where the study is being conducted; Contact information for the study locations; and Links to relevant information on other health Web sites, such as NLM's MedlinePlus for patient health information and PubMed for citations and abstracts for scholarly articles in the field of medicine. Albiglutide is included in the database.
Tanzeum is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. /Included in US product label/
EXPL THER Rats were treated with albiglutide and subjected to 30 min myocardial ischemia followed by 24 hr reperfusion. Left ventricle infarct size, hemodynamics, function and energetics were determined. In addition, cardiac glucose disposal, carbohydrate metabolism and metabolic gene expression were assessed. Albiglutide significantly reduced infarct size and concomitantly improved post-ischemic hemodynamics, cardiac function and energetic parameters. Albiglutide markedly increased both in vivo and ex vivo cardiac glucose uptake while reducing lactate efflux. Analysis of metabolic substrate utilization directly in the heart showed that albiglutide increased the relative carbohydrate versus fat oxidation which in part was due to an increase in both glucose and lactate oxidation. Metabolic gene expression analysis indicated upregulation of key glucose metabolism genes in the non-ischemic myocardium by albiglutide. Albiglutide reduced myocardial infarct size and improved cardiac function and energetics following myocardial I/R injury.

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Drug Warnings
/BOX WARNING/ Tanzeum is contraindicated in patients with a personal or family history of medullary thyroid carcinoma (MTC) or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2). Counsel patients regarding the potential risk of MTC with the use of Tanzeum and inform them of the symptoms of thyroid tumors (e.g., mass in the neck, dysphagia, dyspnea, persistent hoarseness). Routine monitoring of serum calcitonin or using thyroid ultrasound monitoring is of uncertain value for early detection of MTC in patients treated with Tanzeum.
/BOX WARNING/ Carcinogenicity of albiglutide could not be assessed in rodents, but other glucagon-like peptide-1 (GLP-1) receptor agonists have caused thyroid C-cell tumors in rodents at clinically relevant exposures. Human relevance of GLP-1 receptor agonist induced C-cell tumors in rodents has not been determined. It is unknown whether Tanzeum causes thyroid C-cell tumors, including medullary thyroid carcinoma (MTC), in humans.
In patients treated with GLP-1 receptor agonists, there have been postmarketing reports of acute renal failure and worsening of chronic renal failure, which may sometimes require hemodialysis. Some of these events were reported in patients without known underlying renal disease. Use caution when initiating or escalating doses of Tanzeum in patients with renal impairment.
Serious hypersensitivity reactions (pruritus, rash, dyspnea) have been reported in patients receiving albiglutide.1 If a hypersensitivity reaction occurs, albiglutide should be discontinued and the patient should be treated according to the standard of care and monitored until manifestations resolve.
For more Drug Warnings (Complete) data for Albiglutide (14 total), please visit the HSDB record page.

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Albiglutide has a chemical structure quite distinct from that of other marketed GLP-1 RAs. The agent has less gastrointestinal side effects than other comparable GLP-1 RAs and is safe in patients with renal failure. As a sole treatment for diabetes and used with other hypoglycemic agents, it achieves a lowering of HbA1c of up to 1%, less than several competitor GLP-1 RAs. The benefit on weight reduction is minimal compared to other GLP-1 RAs. There exists concern about an imbalance of pancreatitis cases in the approval program as well as injection site reactions which led to discontinuance of therapy in up to 2% of participants. A large long term study now underway will determine if albiglutide, with its lower level of GI intolerance, has a place in the treatment of patients with increased risk of cardiovascular events.[1]

C148H224N40O45

3283.6

3281.646

782500-75-8

Albiglutide fragment TFA; Albiglutide fragment; 224638-84-0

145994868

H-His-Gly-Glu-Gly-aThr-Phe-aThr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-D-Ala-D-Ala-Lys-Glu-Phe-aIle-D-Ala-Trp-Leu-Val-Lys-Gly-Arg-NH2; L-histidyl-glycyl-L-alpha-glutamyl-glycyl-L-allothreonyl-L-phenylalanyl-L-allothreonyl-L-seryl-L-alpha-aspartyl-L-valyl-L-seryl-L-seryl-L-tyrosyl-L-leucyl-L-alpha-glutamyl-glycyl-L-glutaminyl-D-alanyl-D-alanyl-L-lysyl-L-alpha-glutamyl-L-phenylalanyl-L-alloisoleucyl-D-alanyl-L-tryptophyl-L-leucyl-L-valyl-L-lysyl-glycyl-L-argininamide

HGEGXFXSDVSSYLEGQAAKEFXAWLVKGR

White to yellow powder

1.5±0.1 g/cm3

1.661

-5.2

1390

49

50

109

233

7620

29

O=C([C@H](CC(C)C)NC([C@H](CC1=CNC2C=CC=CC1=2)NC([C@@H](C)NC([C@H]([C@H](C)CC)NC([C@H](CC1C=CC=CC=1)NC([C@H](CCC(=O)O)NC([C@H](CCCCN)NC([C@@H](C)NC([C@@H](C)NC([C@H](CCC(N)=O)NC(CNC([C@H](CCC(=O)O)NC([C@H](CC(C)C)NC([C@H](CC1C=CC(=CC=1)O)NC([C@H](CO)NC([C@H](CO)NC([C@H](C(C)C)NC([C@H](CC(=O)O)NC([C@H](CO)NC([C@H]([C@H](C)O)NC([C@H](CC1C=CC=CC=1)NC([C@@H]([C@H](C)O)NC(CNC([C@H](CCC(=O)O)NC(CNC([C@H](CC1=CN=CN1)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)N[C@H](C(N[C@H](C(NCC(N[C@H](C(N)=O)CCCNC(=N)N)=O)=O)CCCCN)=O)C(C)C

JYDZPPZAYQTOIV-OTSUTHPESA-N

InChI=1S/C148H224N40O45/c1-16-76(10)119(145(231)166-79(13)125(211)174-103(59-85-62-158-90-35-24-23-34-88(85)90)135(221)176-99(55-73(4)5)136(222)185-117(74(6)7)143(229)173-92(36-25-27-51-149)127(213)160-65-109(196)167-91(122(153)208)38-29-53-157-148(154)155)187-137(223)101(56-82-30-19-17-20-31-82)177-132(218)97(46-50-115(204)205)172-131(217)93(37-26-28-52-150)170-124(210)78(12)164-123(209)77(11)165-130(216)96(43-47-108(152)195)169-111(198)66-161-129(215)95(45-49-114(202)203)171-133(219)98(54-72(2)3)175-134(220)100(58-84-39-41-87(194)42-40-84)178-140(226)105(68-189)181-142(228)107(70-191)182-144(230)118(75(8)9)186-139(225)104(61-116(206)207)179-141(227)106(69-190)183-147(233)121(81(15)193)188-138(224)102(57-83-32-21-18-22-33-83)180-146(232)120(80(14)192)184-112(199)67-162-128(214)94(44-48-113(200)201)168-110(197)64-159-126(212)89(151)60-86-63-156-71-163-86/h17-24,30-35,39-42,62-63,71-81,89,91-107,117-121,158,189-194H,16,25-29,36-38,43-61,64-70,149-151H2,1-15H3,(H2,152,195)(H2,153,208)(H,156,163)(H,159,212)(H,160,213)(H,161,215)(H,162,214)(H,164,209)(H,165,216)(H,166,231)(H,167,196)(H,168,197)(H,169,198)(H,170,210)(H,171,219)(H,172,217)(H,173,229)(H,174,211)(H,175,220)(H,176,221)(H,177,218)(H,178,226)(H,179,227)(H,180,232)(H,181,228)(H,182,230)(H,183,233)(H,184,199)(H,185,222)(H,186,225)(H,187,223)(H,188,224)(H,200,201)(H,202,203)(H,204,205)(H,206,207)(H4,154,155,157)/t76-,77-,78-,79-,80+,81+,89+,91+,92+,93+,94+,95+,96+,97+,98+,99+,100+,101+,102+,103+,104+,105+,106+,107+,117+,118+,119+,120+,121+/m1/s1

(4S)-5-[[2-[[(2S,3S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2R)-1-[[(2R)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]acetyl]amino]-5-oxopentanoic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Note: 如何溶解多肽产品？请参考本产品网页右上角“产品说明书”文件，第4页。

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注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。