1. Metabolic Enzyme/Protease Neuronal Signaling
  2. Carboxylesterase (CES) Cholinesterase (ChE)
  3. Heptenophos

Heptenophos 是一种 AChE血浆羧酸酯酶 (CES) 抑制剂。Heptenophos 通过抑制 AChE 活性,导致乙酰胆碱在胆碱能突触处蓄积,从而引发典型的有机磷中毒症状。Heptenophos 对雄性白化小鼠具有迅速的致死毒性,但其毒性作用可被双复磷有效拮抗,且 Memantine (HY-B0591) 能进一步增强双复磷的解毒效果。因此,Heptenophos 常被用于有机磷中毒机制及解毒策略的相关研究。

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Heptenophos

Heptenophos Chemical Structure

CAS No. : 23560-59-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Heptenophos is an inhibitor of AChE and plasma carboxylesterase (CES). By inhibiting AChE activity, Heptenophos causes the accumulation of acetylcholine at cholinergic synapses, thereby triggering typical symptoms of organophosphate poisoning. Heptenophos exhibits rapid lethal toxicity in male albino mice, but its toxic effects are effectively antagonized by obidoxime, and Memantine (HY-B0591) further enhances the detoxification efficacy of obidoxime. Therefore, Heptenophos is commonly used in studies related to the mechanism of organophosphate poisoning and detoxification strategies[1][2].

IC50 & Target

AChE

 

体内研究
(In Vivo)

Heptenophos (1.3 LD50;静脉注射;单次给药) 会对雄性白化病小鼠的中枢、外周及红细胞 AChE 以及血浆 CES 产生强烈抑制作用,其静脉注射 LD50 为 196.68 μmol/kg;而 Trimedoxime (HY-165600A) 对 Heptenophos 中毒小鼠具有时间依赖性的保护效力,ED50 为 14.66 μmol/kg,还可重新激活脑、膈肌 AChE 及血浆 CES[1]
Heptenophos (1.3 LD50;静脉注射;单次给药) 在雄性白化小鼠中的静脉注射 LD50 为 196.68 μmol/kg,联合给药时需使用 ED50 为 21.56 μmol/kg 的双复磷 (HY-W011108) 才能达到 50% 的存活率[2]

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

Animal Model: albino mice (male, 18-24 g)[1]
Dosage: 1.3 LD50; 196.68 μmol/kg (LD50)
Administration: i.v.; single dose
Result: Induced severe inhibition of central, peripheral, and erythrocyte AChE as well as plasma carboxylesterase, leaving 3.33% of erythrocyte AChE, 3.37% of brain AChE, 13.05% of diaphragmal AChE, and 7.3% of plasma carboxylesterase activity uninhibited.
Reached an intravenous LD50 of 196.68 μmol/kg (95% confidence interval: 163.72-208.41).
Animal Model: Albino mice (male, 18-24 g)[2]
Dosage: 1.3 LD50 (toxic challenge); 196.68 μmol/kg (LD50 determination)
Administration: i.v.; single dose
Result: Determined an intravenous LD50 of 196.68 μmol/kg (95% confidence interval: 163.72-208.41 μmol/kg).
Required an obidoxime ED50 of 21.56 μmol/kg to achieve 50% survival when administered concurrently with 1.3 LD50 heptenophos.
分子量

250.61

Formula

C9H12ClO4P

CAS 号
中文名称

庚烯磷

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
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Heptenophos
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