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甲吡唑 /Fomepizole {[allProObj[0].p_purity_real_show]}

货号:A195940 同义名: 4-甲基吡唑 / 4-Methylpyrazole;Antizol

Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase which plays a key role in the metabolism of ethylene glycol and methanol.

Fomepizole 化学结构 CAS号:7554-65-6
Fomepizole 化学结构
CAS号:7554-65-6
Fomepizole 3D分子结构
CAS号:7554-65-6
Fomepizole 化学结构 CAS号:7554-65-6
Fomepizole 3D分子结构 CAS号:7554-65-6
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Fomepizole 纯度/质量文件 产品仅供科研

货号:A195940 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Dehydrogenase 其他靶点 纯度
Trilostane 99+%
AGI-6780 +++

IDH2 R140Q mutant, IC50: 23 nM

99%+
Gimeracil 98%
AGI-5198 ++

R132C-IDH1, IC50: 0.16 μM

R132H-IDH1, IC50: 70 nM

99%+
SW033291 ++++

15-PGDH, IC50: 1.5 nM

15-PGDH, Ki: 0.1 nM

99%+
Mycophenolic acid 99+%
Fomepizole 98%
Leflunomide 98%
3-Nitropropanoic acid 99%+
Isovaleramide 98%
Mycophenolate Mofetil +++

Inosine monophosphate dehydrogenase I, IC50: 39 nM

Inosine monophosphate dehydrogenase II, IC50: 27 nM

98%
MK-8245 ++++

SCD1 (mouse), IC50: 1 nM

SCD1 (rat), IC50: 3 nM

99%+
Vidofludimus ++

Human DHODH, IC50: 134 nM

99%+
Emodin 98%
Ivosidenib 98%
NCT-501 ++

ALDH1A1, IC50: 40 nM

98%
Gossypol 99%+
Devimistat 98%
Disulfiram 98%+
Enasidenib ++++

IDH2, IC50: 12 nM

98%
PluriSIn 1 99%+
ML390 +

DHODH, IC50: 0.56 μM

99%+
Teriflunomide 99%+
Daidzin +++

ALDH-Ⅰ, Ki: 20 nM

98+%
18β-Glycyrrhetinic acid 99%
RRx-001 95%
NCT-503 +

PHGDH, IC50: 2.5 μM

99%+
Vorasidenib 99%+
Ammonium Glycyrrhizinate(x:1) 98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Fomepizole 生物活性

靶点
  • Dehydrogenase

描述 Fomepizole, 4-methylpyrazole (4-MP), is a competitive antagonist of alcohol dehydrogenase with a binding affinity >8000 times that of ethanol. Fomepizole's wide therapeutic dose range and safety profile confer several advantages over standard ethanol therapy for the treatment of toxic alcohol exposures, including the lack of ethanol-associated side effects[3]. Fomepizole is a safe and effective antidote in the treatment of ethylene glycol poisoning[4]. Male and pregnant Sprague-Dawley rats, which were obtained at 19 days gestation, were administered fomepizole 15 mg/kg intraperitoneally. Elevated concentrations of fomepizole were detected in the fetus following maternal administration. Fetal fomepizole concentrations were fivefold higher than maternal serum concentrations. The zero order elimination rate of fomepizole from maternal serum was 7.6 mol/L/h, which was slightly slower than the elimination rate in male rats (12.9 mol/L/h) [5]. 1 dose of fomepizole for severe DERs with hypotension unresponsive to fluid resuscitation or for angioedema unresponsive to antihistamines be administered[6]. Fomepizole may precipitate bradycardia and/or hypotension during hemodialysis. Monitor vital signs closely during and immediately after infusion[7].

Fomepizole 参考文献

[1]Lepik KJ, Levy AR, 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.

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

[3]Bestic M, Blackford M, Reed M. Fomepizole: a critical assessment of current dosing recommendations. J Clin Pharmacol. 2009 Feb;49(2):130-7

[4]Battistella M. Fomepizole as an antidote for ethylene glycol poisoning. Ann Pharmacother. 2002 Jun;36(6):1085-9

[5]Gracia R, Latimer B, McMartin KE. Kinetics of fomepizole in pregnant rats. Clin Toxicol (Phila). 2012 Sep;50(8):743-8

[6]Sande M, Thompson D, Monte AA. Fomepizole for severe disulfiram-ethanol reactions. Am J Emerg Med. 2012 Jan;30(1):262.e3-5

[7]Lepik KJ, Brubacher JR, DeWitt CR, Lam GS, Lawson EJ, Erhardt GD, Purssell RA, Kennedy JR, Brignall JL. Bradycardia and hypotension associated with fomepizole infusion during hemodialysis. Clin Toxicol (Phila). 2008 Jul;46(6):570-3

Fomepizole 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

12.18mL

2.44mL

1.22mL

60.90mL

12.18mL

6.09mL

121.80mL

24.36mL

12.18mL

Fomepizole 技术信息

CAS号7554-65-6
分子式C4H6N2
分子量 82.104
别名 4-甲基吡唑 ;4-Methylpyrazole;Antizol;Fomepizolum;Antizol-Vet
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(1278.87 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(1217.97 mM),配合低频超声助溶

动物实验配方
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