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Rec 15/2615 (hydrochloride) Sale

(Synonyms: SB 216469) 目录号 : GC46212

An α1B-AR antagonist

Rec 15/2615 (hydrochloride) Chemical Structure

Cas No.:1782573-48-1

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产品描述

Rec 15/2615 is an antagonist of α1B-adrenergic receptors (α1B-ARs; Ki = 0.45 nM for the recombinant human receptor).1 It selectively inhibits α1B-ARs over α1A-, α1D-, and α1L-ARs (Kis = 7.59, 10.23, and 49 nM, respectively). Rec 15/2615 inhibits norepinephrine-induced contractions of isolated rabbit prostate and urethral strips (Kis = 100 and 316.2 nM, respectively), as well as reduces norepinephrine-induced contractions of chloroethylclonidine-precontracted isolated rabbit aortic rings (Ki = 50 nM).2 It decreases diastolic blood pressure (ED25 = 183 μg/kg, i.v.) and increases intracavernous pressure in anesthetized dogs when administered intracavernously at doses ranging from 30 and 1,000 μg/kg.1,2

|1. Sironi, G., Colombo, D., Poggesi, E., et al. Effects of intracavernous administration of selective antagonists of α1-adrenoceptor subtypes on erection in anesthetized rats and dogs. J. Pharmacol. Exp. Ther. 292(3), 974-981 (2000).|2. Testa, R., Guarneri, L., Angelico, P., et al. Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15/2739 (SB 216469): Role of the alpha-1L adrenoceptor in tissue selectivity, part II. J. Pharmacol. Exp. Ther. 281(3), 1284-1293 (1997).

Chemical Properties

Cas No. 1782573-48-1 SDF
别名 SB 216469
Canonical SMILES COC1=CC2=C(C(N)=NC(N3CCN(C(COC4=C(C(C)C)C=CC=C4OC)=O)CC3)=N2)C=C1OC.Cl.Cl
分子式 C26H33N5O5 • 2HCl 分子量 568.5
溶解度 DMSO: 100 mM 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 1.759 mL 8.7951 mL 17.5901 mL
5 mM 0.3518 mL 1.759 mL 3.518 mL
10 mM 0.1759 mL 0.8795 mL 1.759 mL
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Research Update

Gateways to clinical trials

Methods Find Exp Clin Pharmacol 2007 Nov;29(9):625-55.PMID:18193114doi

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