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WAY-151932 (VNA-932) Sale

(Synonyms: VNA-932; WAY-VNA 932) 目录号 : GC31475

WAY-151932 (VNA-932) 是一种加压素 V2 受体激动剂,在人 V2 结合和 V1a 结合试验中的 IC50 分别为 80.3 nM 和 778 nM。

WAY-151932 (VNA-932) Chemical Structure

Cas No.:220460-92-4

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产品描述

WAY-151932 is a vasopressin V2-receptor agonist with IC50 of 80.3 nM and 778 nM in human-V2 binding and V1a binding assay.

WAY-151932 (VNA-932) stimulates cAMP formation in LV2 cells expressing the hV2 receptors in a dose-dependent manner with an EC50 of 0.74±0.07 nM[2].

Oral administration of WAY-151932 (VNA-932) to water-loaded conscious rats produces a dose-dependent decrease in urine volume (ED50=0.14 mg/kg, 2.5% starch in water vehicle) and a corresponding increase in osmolality without altering the urine electrolyte excretion profile[2].

[1]. Molinari AJ, et al. Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5796-800. [2]. Failli AA, et al. Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists. Bioorg Med Chem Lett. 2006 Feb 15;16(4):954-9.

Chemical Properties

Cas No. 220460-92-4 SDF
别名 VNA-932; WAY-VNA 932
Canonical SMILES O=C(C1=CC=C(N2N=C(C)C=C2)C=C1Cl)N3CC4=CC=CN4CC5=CC=CC=C53
分子式 C23H19ClN4O 分子量 402.88
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 2.4821 mL 12.4106 mL 24.8213 mL
5 mM 0.4964 mL 2.4821 mL 4.9643 mL
10 mM 0.2482 mL 1.2411 mL 2.4821 mL
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Research Update

Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists

Our efforts in seeking low molecular weight agonists of the antidiuretic peptide hormone arginine vasopressin (AVP) have led to the identification of the clinical candidate WAY-151932 (VNA-932). Further exploration of the structural requirements for agonist activity has provided another class of potent, orally active, non-peptidic vasopressin V2 receptor selective agonists exemplified by the 5,11-dihydro-pyrido[2,3-b][1,5]benzodiazepine as a candidate for further development.

Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan

Small molecule agonists and antagonists of the V(2)-vasopressin receptor have been discovered and have undergone clinical trials. In conjunction with these discovery programs, the synthesis and biological testing of various metabolites associated with these clinical targets were actively pursued. We now report the results of our synthetic efforts and the corresponding biological data generated for several of the metabolites of WAY-151932 and CL-347985 (Lixivaptan).