RS 17053 hydrochloride ( RS-17053 )

产品货号. M26811 CAS No. 169505-93-5

RS 17053 盐酸盐是一种有效的选择性 α1A 肾上腺素受体拮抗剂，功能测定中的 pA2 为 9.8，天然细胞膜中的 pKi 为 9.1。

纯度: >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

规格	价格/人民币	库存	数量
2MG	￥275	有现货
5MG	￥446	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

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生物学信息

产品名称

RS 17053 hydrochloride
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

RS 17053 盐酸盐是一种有效的选择性 α1A 肾上腺素受体拮抗剂，功能测定中的 pA2 为 9.8，天然细胞膜中的 pKi 为 9.1。
产品描述

RS 17053 hydrochloride is an effective and selective antagonist of α1A-adrenergic receptor with pA2 of 9.8 in functional assays and pKi of 9.1 in the native cell membrane.(In Vitro):RS 17053 hydrochloride antagonizes responses to NE only at high concentrations in isolated smooth muscle preparations from human LUT tissues. RS 17053 hydrochloride displays a high affinity for the α1A-adrenoceptor (pKi and pA2 estimates of 9.1-9.9) and a 30-100-fold selectivity over the α1 B and the α1 D-adrenoceptor subtypes (pKi and pA2 estimates of 7.7-7.8) in several tissues from rat and cloned adrenoceptors .(In Vivo):RS 17053 hydrochloride has a rapid onset of action and a duration of action exceeding 60 min. RS-17053 (10 mg/kg ) significantly suppresses food intake. RS 17053 hydrochloride pretreatment obviously alters food intake .
体外实验

In several tissues from rat and cloned adrenoceptors, RS 17053 hydrochloride displays high affinity for the α1A-adrenoceptor (pKi and pA2 estimates of 9.1-9.9) and a 30-100-fold selectivity over the α1 B and the α1 D-adrenoceptor subtypes (pKi and pA2 estimates of 7.7-7.8). However, in isolated smooth muscle preparations from human LUT tissues, RS 17053 hydrochloride antagonizes responses to NE only at high concentrations. Estimates of affinity (pA2) at α1-adrenoceptors mediating NE-induced contractions are 7.5 in prostatic periurethral longitudinal smooth muscle (compared with 8.6 for prazosin), 6.9 in anterior fibromuscular stroma (prazosin, 8.9), and 7.1 in bladder neck (prazosin, 8.5).
体内实验

RS 17053 hydrochloride has a rapid onset of action, and a duration of action exceeding 60 min. RS 17053 hydrochloride pretreatment significantly alteres food intake [F(4, 132) 5 6.28, p , 0.0001]. 10 mg/kg RS-17053 significantly suppresses food intake.
同义词

RS-17053
通路

Others
靶点

Other Targets
受体

Proton pump
研究领域

——
适应症

——

化学信息

CAS Number

169505-93-5
分子量

449.42
分子式

C24H30Cl2N2O2
纯度

>98% (HPLC)
溶解度

In Vitro:?DMSO : 100 mg/mL (222.51 mM)
SMILES

Cl.CC(C)(Cc1c[nH]c2ccc(Cl)cc12)NCCOc1ccccc1OCC1CC1
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.Masaoka T, et al. Pathophysiology of Potassium-competitive Acid Blocker-refractory Gastroesophageal Reflux and the Potential of Potassium-competitive Acid Blocker Test. J Neurogastroenterol Motil. 2018 Oct 1;24(4):577-583.

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