BRL-54443, 5-HT 1e 受体激动剂;5-HT 1F 受体激动剂

5-HT1 Selective Inhibitors | Agonists | Antagonists | Modulators

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货号 (SKU)	包装规格	是否现货	价格	数量
B409219-1ml	1ml	现货

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Compound libraries (12332)

基本描述

英文别名	1H-Indol-5-ol, 3-(1-methyl-4-piperidinyl)-
规格或纯度	Moligand™, 10mM in DMSO
英文名称	BRL-54443
生化机理	BRL 54443 是一种 5-HT1E 和 5-HT1F 受体激动剂，_pKi分别为 8.7 和 9.25，与 5-HT1A、5-HT1B、5-HT1D 受体的结合亲和力较弱。
储存温度	-80℃储存
运输条件	超低温冰袋运输
作用类型	激动剂
作用机制	5-HT 1e 受体激动剂;5-HT 1F 受体激动剂
产品介绍	BRL-54443是一种5-HT1E和5-HT1F受体激动剂，pKi分别为8.7和9.25，对5-HT1A， 5-HT1B， 5-HT1D受体具有弱的结合亲和力。A potent agonist at SR-1E and SR-1F. Information BRL 54443 is a5-HT1Eand5-HT1Freceptor agonist withpKiof 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors. In vitro BRL 54443 has also measurable affinity for the 5-HT_2A receptor. BRL 54443 induces contraction with a −logEC50 of 6.52. Contraction caused by BRL 54443 is likely mediated through stimulation of 5-HT5-HT_2A receptors. In vivo BRL 54443 induces an immediate dose-dependent maximal intragastric volume increase vs. saline. Cell Data cell lines：Renca or 786-O cells, mouse endothelial cells and splenic CD11b⁺/c^-myeloid cells, HUVECs Concentrations： Incubation Time： Powder Purity:≥99%

Ki Data	5-HT1B, pKi: 6.9; 5-HT1D, pKi: 7.2; 5-HT1A, pKi: 7.2; 5-HT1F, pKi: 9.25; 5-HT1E, pKi: 8.7
ALogP	2.572
HBD Count	2
Rotatable Bond	1

HTR1E Tchem 5-羟色胺受体 1E(5-hydroxytryptamine receptor 1E) (1 活性数据)

点击查看靶蛋白信息： HTR1E

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

HTR1F Tclin 5-羟色胺受体 1F(5-hydroxytryptamine receptor 1F) (1 活性数据)

点击查看靶蛋白信息： HTR1F

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

Canonical SMILES	CN1CCC(CC1)C2=C[NH]C3=C2C=C(O)C=C3
分子量	230.31
Reaxy-Rn	749183
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=749183&ln=

溶解性	Solubility (25°C) In vitro DMSO: 38 mg/mL (204.04 mM); Ethanol: 15 mg/mL (80.54 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility	46
DMSO(mM) Max Solubility	199.73
Water(mg / mL) Max Solubility	<1