Big Endothelin-1 (1-31) (human, bovine)   中文名称: 大内皮素-1（1-31）（人、牛）

人内皮素-1 (1-31)（100 pM-100 nM；24 小时）刺激系膜细胞的生长 [2]。人内皮素-1 (1-31)，100 nM，持续 0-10 分钟

结肠系膜动脉收缩由 ET-1(1-31)（100 nM；单剂量）诱导。年龄可能会导致宫缩恶化，并且可能是由 ETA 受体介导的。慢性糖尿病现状

细胞增殖测定[2]
细胞类型： 人类系膜细胞
测试浓度： 100 pM-100 nM
孵育时间： 24 小时
实验结果： 原因[3H] - 胸苷掺入增加）诱导人系膜细胞中的 ERK 激活 [2]。以浓度依赖性方式进入细胞。

---

蛋白质印迹分析[2]
细胞类型： 人类系膜细胞
测试浓度： 100 nM
孵育持续时间：0、5、10、15和30分钟
实验结果：ERK活性在5分钟时迅速增加2.45倍，并在10分钟时达到峰值。刺激后 30 分钟，两种 ERK 的活性迅速减弱并恢复到基线控制值。

Animal/Disease Models: ICR mouse, streptozotocin-induced diabetes model [1]
Doses: 100 nM
Route of Administration: in organ bath, single dose
Experimental Results: in 1 week control (but not in non-diabetic In the group, the induced contraction and contractile response of female mice were Dramatically stronger than that of male mice, and there were no significant differences between age-matched controls and diabetic mice in either male or female mice. In the 8-week group, compared with the corresponding The contractions in all mice increased or tended to increase compared to the 1-week group. Although in male mice, there was no difference in this contraction between the control and diabetic groups, the contractions in diabetic female mice were Dramatically greater than those in the control group of female mice, and contractions in female diabetic mice were Dramatically greater than in male diabetic mice. ETA receptor inhibitors inhibited contractions.

[1]. Gender differences in vascular reactivity to endothelin-1 (1-31) in mesenteric arteries from diabetic mice. Peptides. 2008 Aug;29(8):1338-46.

[2]. Effect of endothelin-1 (1-31) on human mesangial cell proliferation. Jpn J Pharmacol. 2000 Oct;84(2):146-55.

C162H236N38O47S5

3628.15867233276

3625.584

133972-52-8

Endothelin-1 (1-31) (Human) TFA;Endothelin-1 (1-31) (Human) acetate

Typically exists as solid at room temperature

1.3±0.1 g/cm3

1.570

0.04

1460

S1C([H])([H])[C@@]([H])(C(N([H])[C@@]([H])(C([H])([H])C2=C([H])N([H])C([H])=N2)C(N([H])[C@@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])C(N([H])[C@@]([H])(C([H])([H])C(=O)O[H])C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])C2=C([H])N([H])C3=C([H])C([H])=C([H])C([H])=C23)C(N([H])[C@@]([H])(C([H])(C([H])([H])[H])C([H])([H])[H])C(N([H])[C@@]([H])(C([H])([H])C(N([H])[H])=O)C(N([H])[C@@]([H])([C@@]([H])(C([H])([H])[H])O[H])C(N2C([H])([H])C([H])([H])C([H])([H])[C@@]2([H])C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])C2=C([H])N([H])C([H])=N2)C(N([H])[C@@]([H])(C([H])(C([H])([H])[H])C([H])([H])[H])C(N([H])[C@@]([H])(C([H])(C([H])([H])[H])C([H])([H])[H])C(N2C([H])([H])C([H])([H])C([H])([H])[C@@]2([H])C(N([H])[C@]([H])(C(=O)O[H])C([H])([H])C2C([H])=C([H])C(=C([H])C=2[H])O[H])=O)=O)=O)=O)=O)C([H])([H])C([H])([H])C(=O)O[H])=O)=O)=O)=O)=O)=O)[C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)[C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)=O)=O)=O)N([H])C([C@]([H])(C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])N([H])C([C@]([H])(C([H])([H])C2C([H])=C([H])C(=C([H])C=2[H])O[H])N([H])C([C@]([H])(C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C([C@]2([H])C([H])([H])SSC([H])([H])[C@@]([H])(C(N([H])[C@@]([H])(C([H])([H])O[H])C(N([H])[C@@]([H])(C([H])([H])O[H])C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])C(=O)O[H])C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N2[H])=O)C([H])([H])C([H])([H])C(=O)O[H])=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])=O)=O)C([H])([H])C([H])([H])SC([H])([H])[H])=O)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)=O)=O)N([H])C([C@]([H])(C([H])([H])O[H])N([H])C([C@]([H])(C([H])([H])S1)N([H])[H])=O)=O)=O)=O)=O)=O

JKSRICZEYPPRFI-UHFFFAOYSA-N

InChI=1S/C162H236N38O47S5/c1-19-83(15)129(158(242)183-105(59-89-65-168-96-33-25-24-32-94(89)96)143(227)192-125(79(7)8)156(240)184-108(62-120(165)207)145(229)198-131(85(17)204)161(245)200-52-29-35-118(200)153(237)174-99(46-48-122(210)211)134(218)178-107(61-91-67-167-76-170-91)144(228)193-127(81(11)12)157(241)195-128(82(13)14)160(244)199-51-28-36-119(199)154(238)185-111(162(246)247)58-88-39-43-93(206)44-40-88)197-159(243)130(84(16)20-2)196-146(230)110(64-124(214)215)181-138(222)102(55-78(5)6)175-141(225)106(60-90-66-166-75-169-90)179-150(234)115-72-250-249-71-95(164)132(216)186-112(68-201)149(233)191-116-73-251-252-74-117(152(236)194-126(80(9)10)155(239)182-104(57-87-37-41-92(205)42-38-87)139(223)177-103(140(224)190-115)56-86-30-22-21-23-31-86)189-135(219)98(45-47-121(208)209)172-133(217)97(34-26-27-50-163)171-142(226)109(63-123(212)213)180-136(220)100(49-53-248-18)173-137(221)101(54-77(3)4)176-147(231)113(69-202)187-148(232)114(70-203)188-151(116)235/h21-25,30-33,37-44,65-67,75-85,95,97-119,125-131,168,201-206H,19-20,26-29,34-36,45-64,68-74,163-164H2,1-18H3,(H2,165,207)(H,166,169)(H,167,170)(H,171,226)(H,172,217)(H,173,221)(H,174,237)(H,175,225)(H,176,231)(H,177,223)(H,178,218)(H,179,234)(H,180,220)(H,181,222)(H,182,239)(H,183,242)(H,184,240)(H,185,238)(H,186,216)(H,187,232)(H,188,235)(H,189,219)(H,190,224)(H,191,233)(H,192,227)(H,193,228)(H,194,236)(H,195,241)(H,196,230)(H,197,243)(H,198,229)(H,208,209)(H,210,211)(H,212,213)(H,214,215)(H,246,247)

4-[[1-[2-[[4-amino-2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[31-amino-7-(4-aminobutyl)-39-benzyl-4-(2-carboxyethyl)-10-(carboxymethyl)-19,22,28-tris(hydroxymethyl)-42-[(4-hydroxyphenyl)methyl]-16-(2-methylpropyl)-13-(2-methylsulfanylethyl)-3,6,9,12,15,18,21,24,27,30,38,41,44,47-tetradecaoxo-45-propan-2-yl-33,34,49,50-tetrathia-2,5,8,11,14,17,20,23,26,29,37,40,43,46-tetradecazabicyclo[23.22.4]henpentacontane-36-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-3-methylpentanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-methylbutanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-[[1-[[1-[[1-[2-[[1-carboxy-2-(4-hydroxyphenyl)ethyl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]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)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

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。

---

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。

View More

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)

---

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。

View More

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

---

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。

---

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。