货号 | 5033/10 |
别名 | 2-(3-Mercaptopropyl)pentanedioic acid |
供应商 | Tocris |
生物活性 | Selective glutamate carboxypeptidase II (GCP II) inhibitor (IC50 = 90 nM). Selective for GCP II over NMDA, kainate and AMPA glutamate receptors and MMP-1, -2, -3, -7, -9, ACE and NEP metalloproteases. Antinociceptive in a rat model of neuropathic pain and protects against motor neuron death in familial amyotrophic lateral sclerosis mice. Orally bioavailable. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
计算分子量 | 206.26 |
分子式 | C8H14O4S |
可溶性/溶解性 | Soluble to 100 mM in water and to 100 mM in DMSO |
参考文献 | Vornovet al (2013) Pharmacokinetics and pharmacodynamics of the glutamate carboxypeptidase II inhibitor 2-MPPA show prolonged alleviation of neuropathic pain through an indirect mechanism. J.Pharmacol.Exp.Ther. 346 406. PMID: 23776202. Ghadgeet al (2003) Glutamate carboxypeptidase II inhibition protects motor neurons from death in familial amyotrophic lateral sclerosis models. Proc.Natl.Acad.Sci.U.S.A. 100 9554. PMID: 12876198. Majeret al (2003) Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor. J.Med.Chem. 46 1989. PMID: 12723961. |