378242-00-3
378242-00-3
Chemical Structure
E2072
- CAS. Nr.: 378242-00-3
- Formula:C16H14O4S
- Molecular Weight:302.34
IUPAC Name: 3-(2-mercaptoethyl)-[1,1'-biphenyl]-2,3'-dicarboxylic acid
InChIKey: FIILSNMCZCETMG-UHFFFAOYSA-N
SMILES: O=C(O)C=1C=CC=C(C1)C=2C=CC=C(C2C(=O)O)CCS
Biological Activity: E2072 is a selective, orally active competitive inhibitor of glutamate carboxypeptidase II (GCPII) with a Ki of 10 nM. E2072 alleviates established thermal hyperalgesia in a rat model of chronic constriction injury. E2072 prevents oxaliplatin-induced reductions in nerve conduction velocity and amplitude in mice. E2072 is applicable to research related to neuropathic pain and neuropathy[1][2].
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E2072 | E2072 is a selective, orally active competitive inhibitor of glutamate carboxypeptidase II (GCPII) with a Ki of 10 nM. E2072 alleviates established thermal hyperalgesia in a rat model of chronic constriction injury. E2072 prevents oxaliplatin-induced reductions in nerve conduction velocity and amplitude in mice. E2072 is applicable to research related to neuropathic pain and neuropathy. | |||||||||||||||||||||
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References
- [1]. Wozniak KM, et al. The orally active glutamate carboxypeptidase II inhibitor E2072 exhibits sustained nerve exposure and attenuates peripheral neuropathy. J Pharmacol Exp Ther. 2012;343(3):746-754. [Content Brief]
- [2]. Rais R, et al. Reversible disulfide formation of the glutamate carboxypeptidase II inhibitor E2072 results in prolonged systemic exposures in vivo. Drug Metab Dispos. 2012;40(12):2315-2323. [Content Brief]
