產(chǎn)品目錄

規(guī)格	50mg
CAS	198821-22-6
別名
化學(xué)名	[(3S)-oxolan-3-yl] N-[[3-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoylamino]phenyl]methyl]carbamate
分子式	C23H24N4O6
分子量	452.46
溶解度	≥ 45.2mg/mL in DMSO
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Merimepodib(VX-497) is a novel, noncompetitive and orally bioavailable inhibitor of Inosine monophosphate dehydrogenase (IMPDH) [1]. IMPDH is anenzymethat convertsinosine monophosphatetoxanthosine monophosphate. IMPDH is associated withcell proliferation, making it a possible target forcancerchemotherapy [2].

In vitro: VX-497 (MW 452.5) inhibited the proliferation of primary human, rat, mouse, and dog lymphocytes at concentrations of approximately 100 nM. The inhibitory effect of VX-497 on lymphocytes was reversed in the presence of exogenous guanosine, but not in the presence of adenosine or uridine, confirming that the antilymphocytic activity of VX-497 was specifically due to inhibition of IMPDH[1]. VX-497 was most potent against the first group of viruses on virus replication, which included HBV, HCMV, EMCV, and RSV, with IC50 values of 0.38, 0.80, 1.0, and 1.14 μM, respectively [3].

In vivo: Oral administration of VX-497 dose-dependently inhibited the primary IgM antibody response, with an ED50 value of approximately 30-35 mg/kg in mice. Single daily dosing of VX-497 was as effective as twice-daily dosing in this model of immune activation [1].In the skin transplant study, trunk skin grafts from Balb/c mice were grafted onto C57Bl/6 mice. Administration of VX-497 twice daily until day 10 significantly prolonged graft survival to 13.2 ± 1.2 (p < 0.001, Kaplan Meier Log-Rank test) days in the 50 mg/kg group and 13.9 ± 1.0 (p < 0.001) days in the 85 mg/kg group [4].

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1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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