| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S87842-5mg促销 |
98.10% | ￥600.00 ￥450.00 |
6 | - | - | - | - |
|
S87842-2mg买3赠1 |
98.10% | ￥500.00 |
5 | - | - | - | - |
|
S87842-10mg促销 |
98.10% | ￥1010.00 ￥800.00 |
6 | - | - | - | - |
|
S87842-25mg买3赠1 |
98.10% | ￥1500.00 |
1 | - | - | - | - |
|
S87842-50mg买3赠1 |
≥98% | ￥2200.00 |
货期：2-3天 | - | - | - | - |
|
S87842-100mg买3赠1 |
≥98% | ￥3400.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | RO1138452 is a potent and selective IP (prostacyclin) receptor antagonist. RO1138452 displays high affinity for IP receptors. In human platelets, pKi is 9.3±0.1; in a recombinant IP receptor system, pKi is 8.7±0.06. | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | Rat I2 Receptor：7 nM (IC50)；Rat I2 Receptor：8.33 (pKi);Rabbit PAF Receptor:52.9 nM (IC50);Human α2A adrenoceptor:724 nM (IC50);Rat α1B adrenoceptor:3280 nM (IC50);Human Muscarinic M4 Receptor:1450 nM (IC50);Human muscarinic M2 Receptor:2220 nM (IC50);Human muscarinic M1 Receptor:2570 nM (IC50)；Human muscarinic M5 Receptor：3110 nM (IC50)；Rat 5-HT1B Receptor：1130 nM (IC50)；pig 5-HT2C Receptor：1190 nM (IC50)；Rat 5-HT2A Receptor：3040 nM (IC50)；Human 5-HT1A Receptor：8580 nM (IC50)；Guinea-pig 5-HT4 Receptor：8910 | ||||||||||||||||||||
| 体内研究： | RO1138452 is a potent and selective antagonist for both human and rat IP receptors and that is possesses analgesic and anti-inflammatory potential. RO1138452 (1-10 mg/kg, i.v.) significantly reduces acetic acid-induced abdominal constrictions. RO1138452 (3-100 mg/kg, p.o.) significantly reduces carrageenan-induced mechanical hyperalgesia and edema formation. One hour after administration of RO1138452 (5 mg/kg, i.v.) to rats, the total plasma concentration is 0.189 μg/mL, whereas the free plasma concentrations is calculated to be 0.009 μg/mL (28 nM) | ||||||||||||||||||||
| 参考文献： | 1. Bley KR, et al. RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br J Pharmacol. 2006 Feb;147(3):335-45. 2. Ayer LM, et al. 4,5-Dihydro-1H-imidazol-2-yl)-[4-(4-isopropoxy-benzyl)-phenyl]-amine (RO1138452) is a selective, pseudo-irreversible orthosteric antagonist at the prostacyclin (IP)-receptor expressed by human airway epithelial cells: IP-receptor-mediated | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO、Ethanol | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
|
||||||||||||||||||||
| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
沪公网安备 31011702002021号
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
