Darusentan
(Synonyms: 达卢生坦,Lu-135252) 目录号 : GC35811
An ETA receptor antagonist
Cas No.:171714-84-4
Sample solution is provided at 25 µL, 10mM.
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Darusentan is an endothelin type A (ETA) receptor antagonist (Ki = 13 nM in rat aortic vascular smooth muscle cells).1 It inhibits contractions induced by human endothelin-1 in isolated rat aortic rings and mesenteric microvessels with pA2 values of 8.1 and 7.97, respectively. Darusentan (50 mg/kg) decreases systolic blood pressure in DOCA-salt hypertensive rats, as well as reduces mean arterial pressure (MAP) and left ventricular developed pressure (LVDP) in normotensive pigs when administered at doses of 1 and 5 mg/kg.2,3 It reduces myocardial infarct size as a percentage of the area at risk in a porcine model of ischemia-reperfusion injury induced by ligation of the left anterior descending (LAD) coronary artery.3
1.Liang, F., Glascock, C.B., Schafer, D.L., et al.Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteriesCan. J. Physiol. Pharmacol.88(8)840-849(2010) 2.Schiffrin, E.L., Turgeon, A., and Deng, L.Y.Effect of chronic ETA-selective endothelin receptor antagonism on blood pressure in experimental and genetic hypertension in ratsBr. J. Pharmacol.121(5)935-940(1997) 3.Gonon, A.T., Wang, Q.D., Shimizu, M., et al.The novel non-peptide selective endothelin A receptor antagonist LU 135 252 protects against myocardial ischaemic and reperfusion injury in the pigActa Physiol. Scand.163(2)131-137(1998)
| Cas No. | 171714-84-4 | SDF | |
| 别名 | 达卢生坦,Lu-135252 | ||
| Canonical SMILES | COC1=NC(O[C@H](C(O)=O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)=NC(OC)=C1 | ||
| 分子式 | C22H22N2O6 | 分子量 | 410.42 |
| 溶解度 | DMSO: ≥ 125 mg/mL (304.57 mM); Water: < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4365 mL | 12.1826 mL | 24.3653 mL |
| 5 mM | 0.4873 mL | 2.4365 mL | 4.8731 mL |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4365 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet