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.
For research use only. We do not sell to patients.
- CAS No.: 378242-00-3
- Formula: C16H14O4S
- Molecular Weight:302.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
E2072 (50-200 nM) potently and competitively inhibits recombinant human GCPII with a Ki of 10 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Tmax | AUCinf | Clearance (CL) | Vd | T1/2 | CL/F | Vd/F | F | AUC0-inf | T1/2 (Absorption) | T1/2 (Elimination) | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.v. | 57226 ng/mL | 0.11 h | / | / | / | / | / | / | / | 86973 ng·h/mL | 0.87 h | 105 h | 38 % |
| Monkey[2] | 5 mg/kg | i.v. | 68013.3 ng/mL | 0.08 h | 63622.1 ng·h/mL | 0.022 L/h/kg | 0.72 L/kg | 23 h | / | / | / | / | / | / | / |
| Monkey[2] | 5 mg/kg | p.o. | 10454.3 ng/mL | 0.42 h | 24935.6 ng·h/mL | / | / | 9.57 h | 0.057 L/h/kg | 0.79 L/kg | 39.1 % | / | / | / | / |
E2072 (administered via oral gavage, once daily for 4 consecutive weeks at doses of 0.01-1.0 mg/kg) prevents oxaliplatin (HY-17371)-induced reductions in nerve conduction velocity and amplitude in female BALB/c mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 200-250 g, chronic constrictive injury model)[1]
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Dosage:10 mg/kg; 1 mg/kg; 0.1 mg/kg; 0.01 mg/kg
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Administration:p.o.; daily; up to 11 consecutive days
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Result:Significantly attenuated pre-existing thermal hyperalgesia with 10, 1, or 0.1 mg/kg doses, with significant reductions observed from the eighth day of treatment.
Prolonged analgesic effect for up to 7 days after cessation of 10 mg/kg treatment.
Showed no effect on hyperalgesia at 0.01 mg/kg dose.
Did not alter normal thermal sensitivity in nonligated paws.
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Animal Model:BALB/c (female, ~20 g, oxaliplatin-induced model)[1]
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Dosage:1 mg/kg; 0.1 mg/kg; 0.01 mg/kg
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Administration:p.o.; daily; 4 weeks
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Result:Significantly prevented oxaliplatin-induced caudal nerve conduction velocity deficits at 0.01, 0.1, and 1.0 mg/kg doses (Oxaliplatin alone reduced caudal NCV to 88% of control).
Significantly prevented oxaliplatin-induced digital nerve conduction velocity deficits at 0.1 and 1.0 mg/kg doses (Oxaliplatin alone reduced digital NCV to 90.58% of control).
Prevented oxaliplatin-induced caudal and digital amplitude deficits at 0.1 and 1.0 mg/kg doses (Oxaliplatin alone reduced caudal amplitude to 83 % of control and digital amplitude to 79% of control).
Did not prevent digital velocity or amplitude deficits at 0.01 mg/kg dose.
Chemical Information
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CAS No. 378242-00-3
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Molecular Weight 302.34
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Formula C16H14O4S
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SMILES
O=C(O)C=1C=CC=C(C1)C=2C=CC=C(C2C(=O)O)CCS
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
E2072 Related Classifications
HY-165571 Related Classifications
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