CAS 209481-24-3; sb-271046a

CAS:

209481-24-3

分子式:

C₂₀H₂₂ClN₃O₃S₂·HCl

分子量:

488.45

英文名称:

sb-271046a

5-chloro-n-(4-methoxy-3-piperazin-1-yl-phenyl)-3-methyl-2-benzo-thiophenesulfonamide hydrochloride

用途:

SB271046是一种口服生物有效的，选择性的5-HT6受体拮抗剂，pKi为8.9，比作用于其他5-HT受体亚型选择性高200倍。SB-271046作用于大鼠和猪纹状体和人类尾壳膜，有效取代[125I]-SB-258585，pKi分别为9.02, 8.55 和8.81。SB-271046竞争性拮抗5-HT诱导的腺苷酸环化酶活性刺激，pA2为8.71。[1] 在功能性腺苷酸环化酶测定中，SB-271046是一种竞争性拮抗剂，pA2为8.7，这与其结合亲和力较好相一致。SB-271046对大部分人类P450酶没有显著的抑制活性。[2]

推荐供应商

货号

品牌

产品名称

规格

包装、参考价格

S792429

MACKLIN

SB 271046 hydrochloride

10mM in DMSO

825元/1ml;

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储存：-20°C

S873254

MACKLIN

SB 271046 hydrochloride

99%

143元/1mg;

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储存：-20℃
状态：粉末

S5326

Sigma-Aldrich

SB-271046A

≥98% (HPLC)

1515.08元/5 MG; 7559.72元/25 MG;

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产品说明

包装

5, 25 mg in glass bottle

生化/生理作用

The first potent and selective 5-HT₆ antagonist. Training in cognitive tasks, as well as administration SB-271046, induces an increase in pERK1/2 and pCREB1 levels, while CREB2 levels are significantly reduced; cognition-enhancing properties of SB-271046 are attributed to the effect on pERK1/2, not pCREB1/2. SB-271046 reverses MK-801-induced, but not scopolamine-induced, learning impairments. However, with coadministration of galanthamine, both types of learning impairments were ameliorated.

特点和优势

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

基本信息

经验(实验)分子式	C₂₀H₂₂ClN₃O₃S₂· HCl
分子量	488.45
MDL编号	MFCD10565914
PubChem化学物质编号	329824453
NACRES	NA.77

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
溶解性	DMSO: >20 mg/mL
创始人	GlaxoSmithKline
储存温度	2-8℃
SMILES string	Cl.COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N4CCNCC4
InChI	1S/C20H22ClN3O3S2.ClH/c1-13-16-11-14(21)3-6-19(16)28-20(13)29(25,26)23-15-4-5-18(27-2)17(12-15)24-9-7-22-8-10-24;/h3-6,11-12,22-23H,7-10H2,1-2H3;1H
InChI key	RMXZRJYGJMSDQK-UHFFFAOYSA-N

安全信息

储存分类代码	11 - Combustible Solids
WGK	nwg
闪点(F)	Not applicable
闪点(C)	Not applicable