2,3-dihydrothieno-Thiadiazole Carboxylate
(Synonyms: MTCC) 目录号 : GC13836
Selective CYP450 inhibitor
Cas No.:152467-47-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
2,3-dihydrothieno-Thiadiazole Carboxylate is a CYP450 (CYP2E1 and CYP2B4) inhibitor.
The cytochrome P450 (CYP) enzymes are a superfamily of oxidative catalysts critical in the biosynthesis and metabolism of various endobiotics such as steroids and steroid hormones, the neurotransmitter nitric oxide, and vitamins A and D. The cytochrome P450 enzymes are also involved in the metabolism of xenobiotics including natural products, drugs, and other organic chemicals.
In vitro: As a 1,2,3-thiadiazole analog, 2,3-dihydrothieno-thiadiazole carboxylate could both inhibit and inactivate certain microsomal CYP450 enzymes (CYP2E1 and CYP2B4) at 100 μM, but not others (CYP1A2). Moreover, P450 2E1 was significantly more sensitive than P450 2B4 to mechanism-based inactivation by 2,3-dihydrothieno-thiadiazole carboxylate when compared by the difference in partition numbers and inactivation rate constants. Inactivation rate constants (kinact) determined from plots of 1/kobs versus 1/[I] were 0.08 for 2E1 and 0.04 min-1 for P450 2B4, with Kis of 0.1 and 2.0 mM, respectively. The difference in the oxidation of the monocyclic and bicyclic thaidiazoles might account for the ability of 2,3-dihydrothieno-thiadiazole carboxylate to function as a mechanism-based inactivator [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Babu, B. R. and Vaz, A.D.N. 1,2,3-thiadiazole: A novel heterocyclic heme ligand for the design of cytochrome P450 inhibitors. Biochemistry 36, 7209-7216 (1997).
| Cas No. | 152467-47-5 | SDF | |
| 别名 | MTCC | ||
| 化学名 | methylthieno[3,2-d][1,2,3]thiadiazole-6-carboxylate | ||
| Canonical SMILES | O=C(OC)C1=CSC2=C1N=NS2 | ||
| 分子式 | C6H4N2O2S2 | 分子量 | 200.2 |
| 溶解度 | ≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 4.995 mL | 24.975 mL | 49.95 mL |
| 5 mM | 0.999 mL | 4.995 mL | 9.99 mL |
| 10 mM | 0.4995 mL | 2.4975 mL | 4.995 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。