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

E2072 是一种选择性具有口服活性的谷氨酸羧肽酶 II (GCPII) 竞争性抑制剂，Ki 为 10 nM。E2072 可减轻大鼠慢性压迫损伤模型中已形成的热痛觉过敏。E2072 可预防小鼠中 Oxaliplatin 诱导的神经传导速度和波幅降低。E2072 可用于神经性疼痛、神经病变的相关研究。

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E2072

E2072 Chemical Structure

CAS No. : 378242-00-3

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E2072 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

E2072 (50-200 nM) 可强效且竞争性地抑制重组人 GCPII，其 Ki 值为 10 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

E2072 相关抗体:
药代动力学
(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 % / / / /
体内研究
(In Vivo)

E2072 (0.01-10 mg/kg，灌胃，每日，连续至多 11 天) 可减轻神经病理性疼痛大鼠慢性压迫损伤模型中已形成的热痛觉过敏[1]。
E2072 (灌胃，每日 1 次，连续 4 周，剂量 0.01-1.0 mg/kg) 可预防雌性 BALB/c 小鼠中 Oxaliplatin (HY-17371) 诱导的神经传导速度和波幅降低[1]。

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.
分子量

302.34

Formula

C16H14O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

E2072 相关分类

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  • 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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