Leflunomide
(Synonyms: 来氟米特; HWA486; RS-34821; SU101) 目录号 : GC17904A prodrug form of A-771726
Cas No.:75706-12-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | DHODase activity is measured by the DCIP colorimetric assay. This is a coupled assay in which oxidation of DHO and subsequent reduction of ubiquinone are stoichiometrically equivalent to the reduction of DCIP. Reduction of DCIP is accompanied by a loss of absorbance at 610 nm (ε=21500 M/cm). The assay is performed in a 96-well microtiter plate at ambient temperature (ca. 25°C). Stock solutions of 10 mM leflunomide and A771726 are prepared in dimethyl sulfoxide (DMSO) and these are diluted with reaction buffer (100 mM Tris and 0.1 % Triton X-100, pH 8.0) to prepare working stocks of the inhibitors at varying concentrations. For each reaction, the well contained 10 nM DHODase, 68 μM DCIP, 0.16 mg/mL gelatin, the stated concentration of ubiquinone, 10 μL of an inhibitor working stock to give the stated final concentration, and reaction buffer. After a 5-min equilibration period, the reaction is initiated by addition of DHO to the stated final concentrations. The total volume of reaction mixture for each assay is 150 μL, and the final DMSO concentration is ≤ 0.01% (v/v). The reaction progress is followed by recording the loss of absorbance at 610 nm over a 10-min period (during which the velocity remained linear). Velocities are reported as the change in absorbance at 610 nm per minute, and each reported value is the average of three replicates. In experiments where the DHO or ubiquinone concentration is varied, the other substrate is held constant at 200 μM. To determine the inhibitor potency of leflunomide and A771726, the effects of varying concentrations of the two compounds on the initial velocity of the DHODase reaction is measured over a concentration range of 0.01−1.0 μM. In these experiments the DHO and ubiquinone concentrations are held constant at 200 and 100 μM, respectively. |
References: [1]. Davis JP, et al. The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase. Biochemistry. 1996 Jan 30;35(4):1270-3. |
Leflunomide is an agonist of aryl hydrocarbon receptor (AHR) [1]. As an immunoregulatory agent, Leflunomide can be administrated orally. A771726 (teriflunomide) is an active drug formed non-enzymatically from leflunomide [2].
Leflunomide has been demonstrated to expand Tregs levels in peripheral blood and stem cells subsets as well as to increase the migration of these cells into the injured kidney. Leflunomide has been displayed to increase cells expressed IL-10 and reduce cells expressed IL-17- and IL-23 in ischemic-reperfused kidney [1].
Leflunomide has shown to significantly lower the lipid peroxidation in male Wistar albino rats of sepsis. Meanwhile, leflunomide successfully inhibited the protein carbonyl rise and NO rise in bowel [2]. Leflunomide has shown to reduce cell proliferation, inhibit tumor marker expression, as well as down-regulate neuroendocrine marker ASCL1 protein expression in a dose- and time-dependent manner in human MTC-TT cells [3].
References:
[1] Baban B1, Liu JY, Mozaffari MS. Aryl hydrocarbon receptor agonist, leflunomide, protects the ischemic-reperfused kidney: role of Tregs and stem cells. Am J Physiol Regul Integr Comp Physiol. 2012 Dec;303(11):R1136-46.
[2] Ozturk E1, Surucu M2, Karaman A3, Samdancı E4, Fadillioglu E5. Protective effect of leflunomide against oxidative intestinal injury in a rodent model of sepsis. J Surg Res. 2014 Apr;187(2):610-5.
[3] Alhefdhi A1, Burke JF, Redlich A, Kunnimalaiyaan M, Chen H. Leflunomide suppresses growth in human medullary thyroid cancer cells. J Surg Res. 2013 Nov;185(1):212-6.
Cas No. | 75706-12-6 | SDF | |
别名 | 来氟米特; HWA486; RS-34821; SU101 | ||
化学名 | 5-methyl-N-[4-(trifluoromethyl)phenyl]-1,2-oxazole-4-carboxamide | ||
Canonical SMILES | CC1=C(C=NO1)C(=O)NC2=CC=C(C=C2)C(F)(F)F | ||
分子式 | C12H9F3N2O2 | 分子量 | 270.21 |
溶解度 | ≥ 83.3mg/mL in DMSO | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.7008 mL | 18.5041 mL | 37.0083 mL |
5 mM | 0.7402 mL | 3.7008 mL | 7.4017 mL |
10 mM | 0.3701 mL | 1.8504 mL | 3.7008 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。