2. Metabolic Enzyme/Protease
  3. Carboxypeptidase
  4. 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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E2072

E2072 Chemical Structure

CAS No. : 378242-00-3

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E2072 Related Antibodies

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Description

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].

In Vitro

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.

E2072 Related Antibodies
Parmacokinetics
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 % / / / /
In Vivo

E2072 (0.01-10 mg/kg, p.o., once daily, for up to 11 consecutive days) alleviates established thermal hyperalgesia in a rat chronic constriction injury model of neuropathic pain[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.

Animal Model: Sprague-Dawley (male, 200-250 g, chronic constrictive injury model)[1]
Dosage: 10 mg/kg; 1 mg/kg; 0.1 mg/kg; 0.01 mg/kg
Administration: p.o.; daily; up to 11 consecutive days
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.
Animal Model: BALB/c (female, ~20 g, oxaliplatin-induced model)[1]
Dosage: 1 mg/kg; 0.1 mg/kg; 0.01 mg/kg
Administration: p.o.; daily; 4 weeks
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.
Molecular Weight

302.34

Formula

C16H14O4S
CAS No.
SMILES

O=C(O)C=1C=CC=C(C1)C=2C=CC=C(C2C(=O)O)CCS
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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E2072 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

E2072378242-00-3E 2072E-2072CarboxypeptidaseGCPII InhibitorBALB/c miceSprague-Dawleyratneuropathic painneuropathyInhibitorinhibitorinhibit

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