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WAY-151932

Names

[ CAS No. ]:
220460-92-4

[ Name ]:
WAY-151932

[Synonym ]:
VNA932
[2-Chloro-4-(3-methyl-1H-pyrazol-1-yl)phenyl](5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-yl)methanone
Methanone, [2-chloro-4-(3-methyl-1H-pyrazol-1-yl)phenyl]-5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-yl-

Biological Activity

[Description]:

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.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Vasopressin Receptor
Research Areas >> Metabolic Disease

[Target]

IC50: 80.3 nM (human-V2 binding), 778 nM (human-V1a binding)[1]


[In Vitro]

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].

[In Vivo]

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].

[References]

[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.


[Related Small Molecules]

Tolvaptan | Mozavaptan | Desmopressin Acetate | Lixivaptan | Terlipressin acetate salt | RO5028442 | OPC 21268 | Balovaptan | (Arg8)-Vasotocin acetate salt

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
630.6±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C23H19ClN4O

[ Molecular Weight ]:
402.876

[ Flash Point ]:
335.1±31.5 °C

[ Exact Mass ]:
402.124725

[ LogP ]:
5.50

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.692

[ Storage condition ]:
2-8℃


Related Compounds