| 產(chǎn)品編號(hào) | D51227 |
| 英文名稱 | RS-127445 |
| 中文名稱 | |
| 別 名 | 5-HT2B受體拮抗劑 |
| 克 隆 號(hào) | |
| CAS | 199864-87-4 |
| 理論分子量 | 281.33 kDa |
| 檢測分子量 | |
| 性 狀 | Lyophilized |
| 保存條件 | Store in dry, dark place for one year. |
| 注意事項(xiàng) | This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications. |
| 產(chǎn)品介紹 |
RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi = 9.5+/-0.1) and 1, 000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pK(B) = 9.5+/-0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4+/-0.1). RS-127445 also blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5+/-1.1) and (+/-)alpha-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9+/-0.3). |
