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RS-127445
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RS-127445图片
CAS NO:199864-87-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
RS-127445 是一种有效的,具有口服活性的,高亲和力选择性5-HT2B受体拮抗剂,pKi为 9.5,比作用于其他受体和离子通道的选择性高 1000 倍。
生物活性

RS-127445 is a selective, high affinity, orally bioavailable5-HT2Breceptorantagonist with apKiof 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites[1].

IC50& Target[1]

5-HT2BReceptor

9.5 nM (pKi)

体外研究
(In Vitro)

RS-127445 is found to has nanomolar affinity for the 5-HT2Breceptor (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 displaces [3H]-5-HT from human recombinant 5-HT2Breceptors expressed in CHO-K1 cells. The affinity (pKivalue) of RS-127445 for the 5-HT2Breceptor is 9.5±0.1 (n=9). RS-127445 is selective for the 5-HT2Breceptor, having approximately 1000 fold lower affinity for the human recombinant 5-HT2A, 5-HT2C, 5-HT5, 5-HT6and 5-HT7receptors, a 5-HT1Areceptor in rat brain membranes, a 5-HT1B/Dreceptor in bovine caudate, and a monoamine uptake site in rabbit platelets. RS-127445 potently blocks the 5-HT (10 nM) evoked increases in intracellular calcium concentrations in the HEK-293 cells expressing the 5-HT2Breceptor (pIC50of 10.4±0.1). In cells expressing human recombinant 5-HT2Breceptors, RS-127445 potently antagonizes 5-HT-evoked formation of inositol phosphates (pKB=9.5±0.1) and 5-HT-evoked increases in intracellular calcium (pIC10=10.4±0.1). RS-127445 also blocks 5-HT-evoked contraction of rat isolated stomach fundus (pA2B=9.5±1.1) and (±)α-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2=9.9±0.3)[1].

体内研究
(In Vivo)

In rats, the fraction of RS-127445 that is bioavailable via the oral or intraperitoneal routes is 14 and 60% respectively. Intraperitoneal administration of RS-127445 (5 mg/kg) produced plasma concentrations predicted to fully saturate accessible 5-HT2Breceptors for at least 4 h.RS-127445 (5 mg/kg) is administered to rats by oral, intraperitoneal and intravenous routes. Peak plasma concentrations are rapidly achieved with the highest concentrations being found at the first time-point measured following intravenous and intraperitonael administration (0.08 h) and by 0.25 h following dosing by the oral route of administration. RS-127445 is cleared from plasma with an estimated terminal elimination half-life of approximately 1.7 h. The bioavailability of RS-127445, when administered by the oral and intraperitoneal routes is approximately 14 and 62% of that obtained by intravenous administration. Approximately 60% of an intraperitoneal dose and 14% of the oral dose of RS-127445 (5 mg/kg) is bioavailable[1]. RS-127445 (1-30 mg/kg), dose-dependently reduces faecal output, reaching significance at 10 and 30 mg/kg (n=6-11). In blood and brain, >98% of RS-127445 is protein-bound[2].

分子量

281.33

Formula

C17H16FN3

CAS 号

199864-87-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.