规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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体外研究 (In Vitro) |
体外活性:阿那格雷是一种口服咪唑并喹唑啉药物,具有抗环 AMP 磷酸二酯酶活性,可抑制人和动物的血小板聚集。阿那格雷通过抑制巨核细胞血小板的成熟起作用。细胞测定:阿那格雷是一种成熟的血小板减少药物。研究还调查了阿那格雷对血小板的影响,表明血小板功能与 ET 中的血小板计数同样重要
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动物实验 |
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毒性/毒理 (Toxicokinetics/TK) |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No information is available on the use of anagrelide during breastfeeding. The manufacturer recommends that the drug not be used during breastfeeding and for 1 week after the last dose. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
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参考文献 |
Semin Thromb Hemost.1997;23(4):379-83;N Engl J Med.1988 May 19;318(20):1292-4.
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其他信息 |
Anagrelide hydrochloride is the hydrochloride salt of anagrelide. It has a role as an antifibrinolytic drug and a platelet aggregation inhibitor. It contains an anagrelide.
Anagrelide Hydrochloride Anhydrous is the hydrochloride salt of a synthetic quinazoline derivative, Anagrelide Hydrochloride reduces platelet production through a decrease in megakaryocyte maturation. Anagrelide inhibits cyclic AMP phosphodiesterase, as well as ADP- and collagen-induced platelet aggregation. At therapeutic doses, it does not influence white cell counts or coagulation parameters. Anagrelide is used for treatment of essential thrombocythemia to reduce elevated platelet counts and the risk of thrombosis. (NCI04) Anagrelide Hydrochloride is the hydrochloride salt of a synthetic quinazoline derivative, Anagrelide Hydrochloride reduces platelet production through a decrease in megakaryocyte maturation. Anagrelide inhibits cyclic AMP phosphodiesterase, as well as ADP- and collagen-induced platelet aggregation. At therapeutic doses, it does not influence white cell counts or coagulation parameters. Anagrelide is used for treatment of essential thrombocythemia to reduce elevated platelet counts and the risk of thrombosis. (NCI04) See also: Anagrelide (annotation moved to). Drug Indication Xagrid is indicated for the reduction of elevated platelet counts in at-risk essential-thrombocythaemia (ET) patients who are intolerant to their current therapy or whose elevated platelet counts are not reduced to an acceptable level by their current therapy. An at-risk patientAn at-risk ET is defined by one or more of the following features: > 60 years of age or; a platelet count > 1000 x 109/l or; a history of thrombohaemorrhagic events. |
分子式 |
C10H7CL2N3O.HCL
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分子量 |
292.55
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精确质量 |
290.973
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CAS号 |
58579-51-4
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相关CAS号 |
Anagrelide;68475-42-3;Anagrelide hydrochloride monohydrate;823178-43-4
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PubChem CID |
135413494
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外观&性状 |
White to off-white solid powder
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密度 |
1.77g/cm3
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沸点 |
376.5ºC at 760 mmHg
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熔点 |
>280ºC
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闪点 |
181.5ºC
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LogP |
2.43
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tPSA |
44.7
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氢键供体(HBD)数目 |
2
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氢键受体(HBA)数目 |
2
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可旋转键数目(RBC) |
0
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重原子数目 |
17
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分子复杂度/Complexity |
360
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定义原子立体中心数目 |
0
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InChi Key |
TVWRQCIPWUCNMI-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C10H7Cl2N3O.ClH/c11-6-1-2-7-5(9(6)12)3-15-4-8(16)14-10(15)13-7;/h1-2H,3-4H2,(H,13,14,16);1H
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化学名 |
Imidazo(2,1-b)quinazolin-2(3H)-one, 6,7-dichloro-1,5-dihydro-, monohydrochloride
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别名 |
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外实验) |
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溶解度 (体内实验) |
配方 1 中的溶解度: 0.77 mg/mL (2.63 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 悬浮液;超声助溶。
例如,若需制备1 mL的工作液,可将100 μL 7.7 mg/mL澄清的DMSO储备液加入到400 μL PEG300中,混匀;再向上述溶液中加入50 μL Tween-80,混匀;然后加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: 0.77 mg/mL (2.63 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 悬浊液; 超声助溶。 例如,若需制备1 mL的工作液,可将 100 μL 7.7 mg/mL 澄清 DMSO 储备液加入 900 μL 20% SBE-β-CD 生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 0.77 mg/mL (2.63 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 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。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 3.4182 mL | 17.0911 mL | 34.1822 mL | |
5 mM | 0.6836 mL | 3.4182 mL | 6.8364 mL | |
10 mM | 0.3418 mL | 1.7091 mL | 3.4182 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02076815 | Completed | Drug: Anagrelide retard Drug: Thromboreductin |
Essential Thrombocythemia | AOP Orphan Pharmaceuticals AG | February 2014 | Phase 3 |
NCT02125318 | Completed | Drug: Anagrelide CR | Thrombocytosis Myeloproliferative Neoplasms |
Galena Biopharma, Inc. | May 2014 | Phase 2 |
NCT01552928 | Completed Has Results | Drug: Anagrelide 0.5 mg Drug: Anagrelide 2.5 mg |
Healthy | Shire | March 29, 2012 | Phase 1 |
NCT01352585 | Completed Has Results | Drug: Anagrelide hydrochloride | Essential Thrombocythemia (ET) | Shire | July 19, 2011 |