AT2 receptor agonist C21
(Synonyms: AT2 receptor agonist C21) 目录号 : GC39554
An AT2 receptor agonist
Cas No.:477775-14-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
AT2 agonist C21 is an agonist of the angiotensin II type 2 (AT2) receptor.1 It selectively binds to the AT2 receptor over the AT1 receptor (Kis = 0.4 and >10 ?M, respectively). AT2 agonist C21 (0.1 ?M) induces neurite outgrowth in NG 108-15 cells. It reduces mean arterial blood pressure in anaesthetized spontaneously hypertensive rats (SHRs) when administered at a dose of 0.05 mg/kg. AT2 agonist C21 (0.03 mg/kg) reduces right ventricle hypertrophy and fibrosis, as well as lung interstitial and perivascular fibrosis, in a rat model of pulmonary hypertension induced by monocrotaline .2 It increases survival and reduces neurological deficits in a mouse model of cerebral ischemia induced by middle cerebral artery occlusion (MCAO) when administered at the same dose.3
1.Wan, Y., Wallinder, C., Plouffe, B., et al.Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonistJ. Med. Chem.47(24)5995-6008(2004) 2.Bruce, E., Shenoy, V., Rathinasabapathy, A., et al.Selective activation of angiotensin AT2 receptors attenuates progression of pulmonary hypertension and inhibits cardiopulmonary fibrosisBr. J. Pharmacol.172(9)2219-2231(2004) 3.Schwengel, K., Namsolleck, P., Lucht, K., et al.Angiotensin AT2-receptor stimulation improves survival and neurological outcome after experimental stroke in miceJ. Mol. Med. (Berl.)94(8)957-966(2016)
| Cas No. | 477775-14-7 | SDF | |
| 别名 | AT2 receptor agonist C21 | ||
| Canonical SMILES | O=C(OCCCC)NS(=O)(C1=C(C2=CC=C(CN3C=CN=C3)C=C2)C=C(CC(C)C)S1)=O | ||
| 分子式 | C23H29N3O4S2 | 分子量 | 475.62 |
| 溶解度 | DMSO: 5 mg/mL (10.51 mM) | 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 | 2.1025 mL | 10.5126 mL | 21.0252 mL |
| 5 mM | 0.4205 mL | 2.1025 mL | 4.205 mL |
| 10 mM | 0.2103 mL | 1.0513 mL | 2.1025 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。
Interconversion of Functional Activity by Minor Structural Alterations in Nonpeptide AT2 Receptor Ligands
ACS Med Chem Lett 2014 Dec 8;6(2):178-82.PMID:25699147DOI:10.1021/ml500427r.
Migration of the methylene imidazole side chain in the first reported selective drug-like AT2 receptor agonist C21/M024 (1) delivered the AT2 receptor antagonist C38/M132 (2). We now report that the AT2 receptor antagonist compound 4, a biphenyl derivative that is structurally related to 2, is transformed to the agonist 6 by migration of the isobutyl group. The importance of the relative position of the methylene imidazole and the isobutyl substituent is highlighted herein.