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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- CAS No.: 378242-00-3
- Formule: C16H14O4S
- Masse moléculaire:302.34
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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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Masse moléculaire 302.34
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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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