化合物RS 17053 hydrochloride T16798

Product Introduction
Bioactivity


英文名: RS 17053 hydrochloride

描述: RS 17053 hydrochloride 是有效的、选择性的 α1A 肾上腺素受体 (α1A adrenoceptor) 拮抗剂。RS 17053 hydrochloride 在细胞膜中测得的 pKi 值为 9.1，功能分析的 pA2 值为 9.8。

体外活性: 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 [1].

体内活性: RS 17053 hydrochloride 作用迅速，持续时间超过60分钟。RS-17053（10 mg/kg）显著降低食物摄入量。RS 17053 hydrochloride 预处理显著改变食物摄入量[F(4, 132) = 6.28, p < 0.0001][2]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 125 mg/mL (278.14 mM)


关键字: Beta Receptor | RS17053 | Adrenergic Receptor | inhibit | RS17053 Hydrochloride | RS 17053 Hydrochloride | RS 17053 hydrochloride | RS 17053 | Inhibitor | RS-17053 Hydrochloride

相关产品: Betaxolol | Levobetaxolol hydrochloride | ST 91 | Saterinone | D2343 | LUN42518 HCl 47142-51-8(free base) | Stephanine | Apraclonidine hydrochloride | Synephrine | Salmeterol Xinafoate

相关库: Neurotransmitter Receptor Compound Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | GPCR Compound Library | Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途