RG7713(RO5028442)是一种高效且有选择性的脑-渗透加压素1a(V1a)受体拮抗剂，其Ki值为1nM(hV1a)和39nM(mV1a)。
CAS：920022-47-5
分子式：C25H28ClN3O2
分子量：437.96
纯度：98%
存储：Store at -20°C

Background:

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).

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].

[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.