ACT-132577
(Synonyms: N-[5-(4-溴苯基)-6-[2-[(5-溴-2-嘧啶基)氧基]乙氧基]-4-嘧啶基]氨基磺酰胺,ACT-132577) 目录号 : GC13236
A dual ETA and ETB receptor antagonist and an active metabolite of macitentan
Cas No.:1103522-45-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
ACT-132577 is a dual antagonist of ETA and ETB receptors with IC50 values of 3.4nM and 987nM, respectively [1].
ACT-132577 is a major metabolite of macitentan which is a dual ET receptor antagonist with strong affinity for the tissues. Macitentan is metabolized into ACT-132577 in vivo. ACT-132577 is also a dual ET receptor antagonist and has a longer half-life than its parent compound. In assays using microsomal membranes of CHO cells overexpressing human ETA and ETB receptors, ACT-132577 shows potent effects on ETA and ETB receptors with IC50 values of 3.4nM and 987nM, respectively. In the in vitro functional assay, ACT-132577 completely inhibits the intracellular calcium increase induced by ET-1with IC50 values of 14nM, 5.8nM and 10.9nM in HPASMC, RASMC and m3T3 cells, respectively. ACT-132577 also causes a significant reduction of sarafotoxin S6c-induced contraction in isolated rat trachea [1].
In normotensive rats, administration of macitentan increases plasma ET-1 concentration. In hypertensive DOCA-salt rats, macitentan decreases mean arterial blood pressure. Besides that, macitentan suppresses the development of pulmonary hypertension and right ventricle hypertrophy in the monocrotaline model of pulmonary hypertension as well as in the streptozotocin model of diabetes [1].
References:
[1] Iglarz M, Binkert C, Morrison K, et al. Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. Journal of Pharmacology and Experimental Therapeutics, 2008, 327(3): 736-745.
| Cas No. | 1103522-45-7 | SDF | |
| 别名 | N-[5-(4-溴苯基)-6-[2-[(5-溴-2-嘧啶基)氧基]乙氧基]-4-嘧啶基]氨基磺酰胺,ACT-132577 | ||
| Canonical SMILES | BrC1=CC=C(C2=C(OCCOC3=NC=C(Br)C=N3)NC=N/C2=N\S(N)(=O)=O)C=C1 | ||
| 分子式 | C16H14Br2N6O4S | 分子量 | 546.19 |
| 溶解度 | DMSO : 25 mg/mL (45.77 mM; ultrasonic and warming and heat to 60°C) | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8309 mL | 9.1543 mL | 18.3086 mL |
| 5 mM | 0.3662 mL | 1.8309 mL | 3.6617 mL |
| 10 mM | 0.1831 mL | 0.9154 mL | 1.8309 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。