Merimepodib-VI-21497-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMerimepodibCat. No.: HY-13986CAS No.: 198821-22-6Synonyms: VI-21497; VX-497; MMP分式: CHNO分量: 452.46作靶點(diǎn): HBV; HCV作通路: Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 31 mg/mL (6

2、8.51 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.2101 mL 11.0507 mL 22.1014 mL5 mM 0.4420 mL 2.2101 mL 4.4203 mL10 mM 0.2210 mL 1.1051 mL 2.2101 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Merimepodib競(jìng)爭(zhēng)型，有服活性的肌苷磷酸脫氫酶 (IMPDH

3、) 抑制劑，具有譜抗病毒活性。體外研究VX-497 has antiproliferative effect on lymphoid and keratinocyte cells. The antiproliferative effect of VX-497in cells is reversed within 48 h of its removal 1. VX-497 has intermediate antiviral activity against a secondgroup of viruses, which includes HSV-1, parainfluenza-3 virus

4、, BVDV, VEEV, and dengue virus, with IC50s1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEranging from 6 to 19 M. VX-497 is 100-fold more potent, with an IC50 of 380 nM and a corresponding CC50of 5.2 M, for a therapeutic index of 14. The antiviral activity of VX-497 in HepG5 cells is reversedthreef

5、old by the addition of guanosine 2.體內(nèi)研究 Oral administration of VX-497 inhibits the primary IgM antibody response in a dose-dependent manner, withan ED50 value of appr 30-35 mg/kg in mice. Single daily dosing of VX-497 is observed to be as effective astwice-daily dosing in this model of immune activa

6、tion 1. GVHD developed in the vehicle-treated allograftedF1 mice and treatment with VX-497 improved all manifestations of the disease significantly. The 2.9-foldincrease in spleen weight in allografted animals is reduced to a 1.6-fold increase in the VX-497-treated mice.Serum IFN-gamma levels are in

7、creased 54-fold in the vehicle group while there is a 7.4-fold increase in VX-497-treated animals 3.PROTOCOLCell Assay 2 The murine fibroblast L929 cell line is cultured in Eagle minimal essential medium supplemented with 10%fetal bovine serum, nonessential amino acids, 50 U of penicillin per mL, 50

8、 g of streptomycin per mL, and 2mM l-glutamine. EMCV is infected at 500 PFU/107 L929 cells. Cells are left untreated or are treated withdifferent concentrations of murine IFN- alone, VX-497 alone, or combinations thereof.MCE has not independently confirmed the accuracy of these methods. They are for

9、 reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Mol Immunol. 2019 Aug. Antiviral Res. 2018 Jan;149:34-40.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Jain J, et al. VX-497: a novel, selective IMPDH inhibitor and immunosuppressive agent. J Pharm Sci. 2001 May;90(5):625-37.2. Markland W, et

10、al. Broad-spectrum antiviral activity of the IMP dehydrogenase inhibitor VX-497: a comparison with ribavirin anddemonstration of antiviral additivity with alpha interferon. Antimicrob Agents Chemother. 2000 Apr;44(4):859-66.3. Decker CJ, et al. The novel IMPDH inhibitor VX-497 prolongs skin graft survival and improves graft versus host disease in mice. DrugsExp Clin Res. 2001;27(3):89-95.McePdfHeightCaution: Product has not been fully