Fomepizole (Synonyms: 甲吡唑; 4-Methylpyrazole)

Fomepizole (4-Methylpyrazole) 是一种有效的细胞色素 P450 (CYP2E1) 抑制剂。Fomepizole 是竞争性的乙醇脱氢酶 (alcohol dehydrogenase) 抑制剂。Fomepizole 可以阻止甲醇和乙二醇进一步转化为有毒代谢产物。Fomepizole 有潜力用作乙二醇或甲醇中毒的解毒剂。

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生物活性

Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning^[1]^[2]^[3].

IC₅₀ & Target^[3]

CYP2E1

体内研究 (In Vivo)	Pretreatment with Fomepizole (4-Methylpyrazole; 25 mg/kg; IP) prolongs ethanol neurobehavioral toxicity in CD-1 mice^[4]

分子量

82.10

性状

<13°C 固体,>13°C 液体

Formula

C₄H₆N₂

CAS 号

7554-65-6

中文名称

甲吡唑；4-甲基吡唑

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (1218.03 mM)

H₂O : 100 mg/mL (1218.03 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	12.1803 mL	60.9013 mL	121.8027 mL
5 mM	2.4361 mL	12.1803 mL	24.3605 mL
10 mM	1.2180 mL	6.0901 mL	12.1803 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS

Solubility: 140 mg/mL (1705.24 mM); Clear solution; Need ultrasonic
2.
请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (30.45 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (30.45 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
3.
请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (30.45 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (30.45 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
4.
请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (30.45 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (30.45 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

参考文献	[1]. Casavant MJ. Fomepizole in the treatment of poisoning. Pediatrics. 2001 Jan;107(1):170. [Content Brief] [2]. Lepik KJ, et al. Adverse drug events associated with the antidotes for methanol and ethylene glycol poisoning: a comparison of ethanol and fomepizole. Ann Emerg Med. 2009 Apr;53(4):439-450.e10. [Content Brief] [3]. Garrett Rampon, et al. Use of fomepizole as an adjunct in the treatment of acetaminophen overdose: a case series. Toxicology Communications. Volume 4, 2020 - Issue 1. [4]. Páez AM, et al. Effects of 4-methylpyrazole on ethanol neurobehavioral toxicity in CD-1 mice. Acad Emerg Med. 2004 Aug;11(8):820-6. [Content Brief]

参考文献

[1]. Casavant MJ. Fomepizole in the treatment of poisoning. Pediatrics. 2001 Jan;107(1):170.  [Content Brief]

[2]. Lepik KJ, et al. Adverse drug events associated with the antidotes for methanol and ethylene glycol poisoning: a comparison of ethanol and fomepizole. Ann Emerg Med. 2009 Apr;53(4):439-450.e10.  [Content Brief]

[3]. Garrett Rampon, et al. Use of fomepizole as an adjunct in the treatment of acetaminophen overdose: a case series. Toxicology Communications. Volume 4, 2020 - Issue 1.

[4]. Páez AM, et al. Effects of 4-methylpyrazole on ethanol neurobehavioral toxicity in CD-1 mice. Acad Emerg Med. 2004 Aug;11(8):820-6.  [Content Brief]

该产品被引用文献

参考文献	[1]. Casavant MJ. Fomepizole in the treatment of poisoning. Pediatrics. 2001 Jan;107(1):170. [Content Brief] [2]. Lepik KJ, et al. Adverse drug events associated with the antidotes for methanol and ethylene glycol poisoning: a comparison of ethanol and fomepizole. Ann Emerg Med. 2009 Apr;53(4):439-450.e10. [Content Brief] [3]. Garrett Rampon, et al. Use of fomepizole as an adjunct in the treatment of acetaminophen overdose: a case series. Toxicology Communications. Volume 4, 2020 - Issue 1. [4]. Páez AM, et al. Effects of 4-methylpyrazole on ethanol neurobehavioral toxicity in CD-1 mice. Acad Emerg Med. 2004 Aug;11(8):820-6. [Content Brief]

参考文献