| Bioactivity | RG7713 (RO5028442) is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a). | ||||||||||||
| Target | Ki: 1 nM (hV1a receptor), 39 nM (mV1a receptor) | ||||||||||||
| Invitro | RG7713 (RO5028442) (compound 8) has excellent binding in and functional affinity for hV1a, moderate mouse affinity, and excellent selectivity versus human V2 (hV2) and human oxytocin (hOT) receptors. RG7713 (RO5028442) shows high solubility. RG7713 (RO5028442) is found to be highly selective against a panel of 89 targets. Finally, RG7713 (RO5028442) is identified as a suitable compound for clinical studies[1]. | ||||||||||||
| Name | RG7713 | ||||||||||||
| CAS | 920022-47-5 | ||||||||||||
| Formula | C25H28ClN3O2 | ||||||||||||
| Molar Mass | 437.96 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |