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Balovaptan

Names

[ CAS No. ]:
1228088-30-9

[ Name ]:
Balovaptan

[Synonym ]:
4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine, 8-chloro-5,6-dihydro-5-methyl-1-[trans-4-(2-pyridinyloxy)cyclohexyl]-
RAX5D5AGV6
8-Chloro-5-methyl-1-[trans-4-(2-pyridinyloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
10298
balovaptan

Biological Activity

[Description]:

Balovaptan is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.

[Related Catalog]:

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

[Target]

Ki: 1 nM (hV1a), 39 nM (mV1a)[1]


[In Vitro]

Balovaptan is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for hV1a and mhV1a, and is used for the research of autism. Balovaptan shows >30000-fold selectivity for hV1a over hV2 receptors, 9891-fold selectivity over hOTR (human oxytocin receptor)[1].

[References]

[1]. Ratni H, et al. Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. J Med Chem. 2015 Mar 12;58(5):2275-89.


[Related Small Molecules]

Tolvaptan | Mozavaptan | Desmopressin Acetate | Lixivaptan | Terlipressin acetate salt | RO5028442 | OPC 21268 | WAY-151932 | (Arg8)-Vasotocin acetate salt

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
597.0±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H24ClN5O

[ Molecular Weight ]:
409.912

[ Flash Point ]:
314.9±32.9 °C

[ Exact Mass ]:
409.166931

[ LogP ]:
3.16

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.702