VX-148 is a novel, uncompetitive IMPDH inhibitor with a K(i) value of 6 nM against IMPDH type II enzyme. VX-148 is slightly more potent than mycophenolic acid and VX-497 in inhibiting the proliferation of mitogen-stimulated primary human lymphocytes (IC(50) value of ~80 nM). The inhibitory activity of VX-148 is alleviated in the presence of exogenous guanosine. VX-148 does not inhibit proliferation of nonlymphoid cell types such as fibroblasts, indicating selectivity for inhibition of IMPDH activity. VX-148 is orally bioavailable in rats and mice; orally bioavailable administration of VX-148 inhibits primary antibody response in mice in a dose-dependent manner with an ED(50) value of 38 mg/kg b.i.d. VX-148 significantly prolongs skin graft survival at 100 mg/kg b.i.d. in mice. References: Dunkern T, Chavan S, Bankar D, Patil A, Kulkarni P, Kharkar PS, Prabhu A, Goebel H, Rolser E, Burckhard-Boer W, Arumugam P, Makhija MT. Design, synthesis and biological evaluation of novel inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors. J Enzyme Inhib Med Chem. 2013 May 10. [Epub ahead of print] PubMed PMID: 23663081.

纯度：≥98%

CAS：297730-05-3