GSK163090 ( —— )

产品货号. M24834 CAS No. 844903-58-8

GSK163090 是一种特异性口服活性 5-HT1A/B/D 受体拮抗剂（5-HT1A/B/D 和多巴胺 D2/D3 的 pK 值：9.4/8.5/9.7 和 6.3/6.7）。

纯度: >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

规格	价格/人民币	库存	数量
5MG	￥1280	有现货
10MG	￥2179	有现货
25MG	￥3669	有现货
50MG	￥5395	有现货
100MG	获取报价	有现货
200MG	获取报价	有现货
500MG	获取报价	有现货
1G	获取报价	有现货

产品询价大包装询价加入购物车

生物学信息

产品名称

GSK163090
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

GSK163090 是一种特异性口服活性 5-HT1A/B/D 受体拮抗剂（5-HT1A/B/D 和多巴胺 D2/D3 的 pK 值：9.4/8.5/9.7 和 6.3/6.7）。
产品描述

GSK163090 is a specific and orally active 5-HT1A/B/D receptor antagonist (pKis: 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3).(In Vitro):GSK163090 (compound 36) is devoid of agonist activity at R1 receptors, but rather it demonstrates a moderate functional antagonismof the phenylephrineinduced contraction of rabbit aorta (pIC50=6.9).At 1 μM concentration, the ratio of the apparent permeabilities measured from basolateral-to-apical (BA) to apical-to-basolateral (AB) indicated that GSK163090 is a moderate P-glycoprotein (P-gp) substrate (BA/AB = 2.8).(In Vivo):In male Sprague-Dawley rats, GSK163090 (compound 36) treatment shows clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg.
体外实验

GSK163090 (compound 36) is devoid of agonist activity at R1 receptors, but rather it demonstrates a moderate functional antagonismof the phenylephrineinduced contraction of rabbit aorta (pIC50=6.9).At 1 μM concentration, the ratio of the apparent permeabilities measured from basolateral-to-apical (BA) to apical-to-basolateral (AB) indicated that GSK163090 is a moderate P-glycoprotein (P-gp) substrate (BA/AB = 2.8).
体内实验

In male Sprague-Dawley rats, GSK163090 (compound 36) treatment shows clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg.
同义词

——
通路

Endocrinology/Hormones
靶点

5-HT Receptor
受体

5-HT1A|5-HT1B|5-HT1D|Dopamine
研究领域

——
适应症

——

化学信息

CAS Number

844903-58-8
分子量

415.53
分子式

C25H29N5O
纯度

>98% (HPLC)
溶解度

DMSO:14.29 mg/mL (34.39 mM; Need ultrasonic)
SMILES

Cc1ccc(c(N2CCN(CCc3cccc(N(CCN4)C4=O)c3)CC2)ccc2)c2n1
化学全称

——

运输与储存

储存条件

(-20℃)
运输条件

With Ice Pack
稳定性

≥ 2 years

参考文献

1.Leslie CP, et al. Discovery of 1-(3-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, selective, and orally active 5-HT1A/B/D receptor antagonist. J Med Chem. 2010 Dec 9;53(23):8228-8240.

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