4-Carboxypyrazole
(Synonyms: 1H-吡唑-4-甲酸) 目录号 : GC60512
4-Carboxypyrazole是一种内源性代谢产物。
Cas No.:37718-11-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
4-Carboxypyrazole is an endogenous metabolite.
| Cas No. | 37718-11-9 | SDF | |
| 别名 | 1H-吡唑-4-甲酸 | ||
| Canonical SMILES | O=C(C1=CNN=C1)O | ||
| 分子式 | C4H4N2O2 | 分子量 | 112.09 |
| 溶解度 | DMSO : 100 mg/mL (892.14 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 8.9214 mL | 44.607 mL | 89.214 mL |
| 5 mM | 1.7843 mL | 8.9214 mL | 17.8428 mL |
| 10 mM | 0.8921 mL | 4.4607 mL | 8.9214 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Kinetic interactions between 4-methylpyrazole and ethanol in healthy humans
Alcohol Clin Exp Res 1996 Aug;20(5):804-9.PMID:8865952DOI:10.1111/j.1530-0277.1996.tb05255.x.
4-Methylpyrazole (4-MP), a potent inhibitor of alcohol dehydrogenase activity, is a candidate to replace ethanol as the antidote for methanol and ethylene glycol intoxications, because it has a longer duration of action and apparently fewer adverse effects. To study a probable mutual inhibitory effect between ethanol and 4-MP on their elimination, two studies were performed in healthy human volunteers using double-blind crossover designs. In study A1 4-MP in the presumed therapeutic dose range of 10 to 20 mg/kg caused a 40% reduction in the rate of elimination of ethanol in 12 subjects given 0.5 to 0.7 g/kg of ethanol. These data suggest that such doses of 4-MP inhibit alcohol dehydrogenase activity in humans in vivo and would be effective at blocking methanol or ethylene glycol metabolism. In study B, ethanol (0.6 g/kg followed by 0.2 g/kg twice) significantly decreased the rate of elimination of 4-MP (5 mg/kg, given intravenously to four subjects). These moderate doses of ethanol also inhibited the rate of urinary excretion of 4-Carboxypyrazole, the primary metabolite of 4-MP in humans. Data suggest that ethanol inhibits 4-MP metabolism, thereby increasing the duration of therapeutic blood levels of 4-MP in the body. This mutual interaction may have clinical implications, because most self-poisoned patients have also ingested ethanol. Theoretically, methanol and ethylene glycol might also show such interactions with 4-MP.
A stable zinc-4-carboxypyrazole framework with high uptake and selectivity of light hydrocarbons
Dalton Trans 2015 Feb 14;44(6):2893-6.PMID:25564046DOI:10.1039/c4dt03594a.
A special organic ligand, 4-Carboxypyrazole (4-cpz), is chosen to synthesize a highly stable metal-organic framework (MOF) for selective sorption of light hydrocarbons. The new MOF, (H(3)O)[Zn(3)(OH)(4-cpz)3]·2(DEF)·H(2)O (FIR-51, DEF = N,N-diethylformamide), was synthesized solvothermally and shows unusual chemical stability. This compound exhibits high storage capacity for light hydrocarbons and high selectivity for C3 and C2 over methane at 273 and 294 K.
Kinetics and metabolism of fomepizole in healthy humans
Clin Toxicol (Phila) 2012 Jun;50(5):375-83.PMID:22554311DOI:10.3109/15563650.2012.683197.
Context/objective: Fomepizole, a potent inhibitor of alcohol dehydrogenase, has replaced ethanol as antidote for methanol and ethylene glycol intoxications because of a longer duration of action and fewer adverse effects. Prior human studies have indicated that single doses of fomepizole are eliminated by Michaelis-Menten kinetics, but two studies in poisoned patients have suggested that first order elimination occurs after multiple doses. Because of the contrast in fomepizole kinetics among existing studies and the lack of information regarding its metabolism in humans, kinetic and metabolic studies were conducted after single doses and after multiple oral doses in healthy human subjects. Materials/methods: In a single-dose, crossover study, healthy humans received fomepizole IV or orally (7 mg/kg). Also to define the metabolism and kinetics of fomepizole when administered over the presumed antidotal period, subjects were divided into three groups, which were given oral loading doses of 10-15 mg/kg, followed by supplemental doses of 3-10 mg/kg/12 h through 96 hours. Results: The single dose study confirmed that fomepizole was eliminated by saturable, nonlinear kinetics, primarily by metabolism, and subsequent renal excretion of the metabolite 4-Carboxypyrazole (4-CP). In the multi-dose study, the zero order elimination rate of fomepizole increased with increasing duration of treatment (from mean of 3 μmol/L/h after first dose to 14 μmol/L/h after 72 hours). Consistent with the enhanced elimination of fomepizole, the rate of urinary excretion of 4-CP increased with time. After 96 hours, fomepizole elimination apparently changed to first order kinetics with a t(½) of 1.5-2 hours. Discussion/conclusion: The results suggest that fomepizole induces its own metabolism via cytochrome P-450, leading to enhanced fomepizole elimination and 4-CP excretion. Thus, to maintain relatively constant plasma levels of fomepizole during therapy, increased supplemental doses at about 36-48 hours are needed to overcome the increased elimination of fomepizole. As such, these kinetic evaluations in healthy humans support the current dosing recommendations for fomepizole.