Merimepodib
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Merimepodib(VX-497)是一种新型、非竞争性和口服生物可利用的肌苷单磷酸脱氢酶(IMPDH)抑制剂[1]。IMPDH将肌苷单磷酸转化为单磷酸黄苷。IMPDH与细胞增殖相关,使其成为癌症化疗的潜在靶标[2]。
体外实验:约100 nM浓度的VX-497(MW 452.5)抑制原代人、大鼠、小鼠和狗淋巴细胞的增殖。外源性鸟苷可以逆转VX-497对淋巴细胞的抑制作用,但腺苷或尿苷没有这种逆转作用,证实了VX-497的抗淋巴细胞活性是由于特异性地抑制IMPDH [1]。VX-497对第一组病毒的病毒复制最有效,包括HBV、HCMV、EMCV和RSV,IC50值分别为0.38、0.80、1.0和1.14 μM[3]。
在体实验:口服给药VX-497以剂量依赖性的方式抑制初级IgM抗体应答,小鼠中ED50值约为30-35 mg/kg。在免疫激活模型中,单次每日给药VX-497与每日两次给药效果相当[1]。在皮肤移植研究中,将来自Balb/c小鼠的躯干皮肤移植物移植到C57Bl/6小鼠上。50 mg/kg VX-497每日给药两次直到第10天显著延长移植物存活至13.2 ± 1.2天(p < 0.001,Kaplan Meier对数秩检验),85 mg/kg组中为13.9 ± 1.0天[4]。
参考文献:
[1]. Jain J1,Almquist SJ,Shlyakhter D,Harding MW. VX-497: a novel, selective IMPDH inhibitor and immunosuppressive agent. J Pharm Sci.2001 May;90(5):625-37.
[2]. Pimkin M1,Markham GD. Inosine 5'-monophosphate dehydrogenase. Adv Enzymol Relat Areas Mol Biol.2009;76:1-53.
[3]. Markland W1,McQuaid TJ,Jain J,Kwong AD. Broad-spectrum antiviral activity of the IMP dehydrogenase inhibitor VX-497: a comparison with ribavirin and demonstration of antiviral additivity with alpha interferon. Antimicrob Agents Chemother.2000 Apr;44(4):859-66.
[4]. Decker CJ1,Heiser AD,Chaturvedi PR,Faust TJ,Ku G,Moseley S,Nimmesgern E. The novel IMPDH inhibitor VX-497 prolongs skin graft survival and improves graft versus host disease in mice. Drugs Exp Clin Res.2001;27(3):89-95.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 452.46 |
Cas No. | 198821-22-6 |
Formula | C23H24N4O6 |
Solubility | ≥45.2 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | [(3S)-oxolan-3-yl] N-[[3-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoylamino]phenyl]methyl]carbamate |
SDF | Download SDF |
Canonical SMILES | COC1=C(C=CC(=C1)NC(=O)NC2=CC=CC(=C2)CNC(=O)OC3CCOC3)C4=CN=CO4 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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