WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406727
Description: 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; oral 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.
MedKoo Cat#: 406727
Chemical Formula: C23H25N5O4
Exact Mass: 435.19065
Molecular Weight: 435.48
Elemental Analysis: C, 63.44; H, 5.79; N, 16.08; O, 14.70
VX-148 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to email@example.com to inquire quote.
Synonym: VX148, VX-148, VX 148
IUPAC/Chemical Name: (R)-1-cyanobutan-2-yl ((S)-1-(3-(3-(4-cyano-3-methoxyphenyl)ureido)phenyl)ethyl)carbamate
InChi Key: PJFQWSNOXLEDDZ-MGPUTAFESA-N
InChi Code: InChI=1S/C23H25N5O4/c1-4-20(10-11-24)32-23(30)26-15(2)16-6-5-7-18(12-16)27-22(29)28-19-9-8-17(14-25)21(13-19)31-3/h5-9,12-13,15,20H,4,10H2,1-3H3,(H,26,30)(H2,27,28,29)/t15-,20+/m0/s1
SMILES Code: O=C(O[C@H](CC)CC#N)N[C@H](C1=CC=CC(NC(NC2=CC=C(C#N)C(OC)=C2)=O)=C1)C
The following data is based on the product molecular weight 435.48 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: 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.
2: Jain J, Almquist SJ, Heiser AD, Shlyakhter D, Leon E, Memmott C, Moody CS, Nimmesgern E, Decker C. Characterization of pharmacological efficacy of VX-148, a new, potent immunosuppressive inosine 5'-monophosphate dehydrogenase inhibitor. J Pharmacol Exp Ther. 2002 Sep;302(3):1272-7. PubMed PMID: 12183689.