4-phenyl-5-methyl-1,2,3-Thiadiazole (Synonyms: NSC 358739) |
| カタログ番号GC11758 |
CYP2B4およびCYP2E1阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 64273-28-5
Sample solution is provided at 25 µL, 10mM.
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4-phenyl-5-methyl-1,2,3-Thiadiazole is a CYP2B4 and CYP2E1 inhibitor.
Cytochrome P450 (CYP450) enzymes, a superfamily of oxidative catalysts, are important in the biosynthesis and metabolism of a wide range of endogenous molecules and the metabolism of xenobiotics. CYP2B4 can metabolize substituted amines, while CYP2E1 metabolizes various alcohols and halogenated alkenes.
In vitro: 4-phenyl-5-methyl-1,2,3-Thiadiazole (PMT) was found to be slightly more inhibitory to P450s 2E1 and 1A2 than its close analog, 4,5-diphenyl-1,2,3-thiadiazole (DPT). By contrast, 4-phenyl-5-hydrogen-1,2,3-Thiadiazole (PT), a weaker inhibitor than DPT and PMT with P450s 2E1 and 2B4, was comparable to PMT and more effective than DPT with P450 1A2. Moreover, PMT, DPT, as well as PT showed no inactivation of either P450 2E1 or 2B4, though they were fairly effective inhibitors, and the thiadiazole ring could be oxidized by the P450 system. Furthremore, the lack of inactivation of the P450 isoforms by PMT, DPT, and PT suggested that a transient reactive intermediate was not formed on oxidation of the thiadiazole ring. In additioin, the 1,2,3-thiadiazole ring could be oxidized by the P450 system [1].
In vivo: Up to now, there is no animla 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. | 64273-28-5 | SDF | |
| 同義語 | NSC 358739 | ||
| Chemical Name | 5-methyl-4-phenyl-1,2,3-thiadiazole | ||
| Canonical SMILES | Cc1snnc1c1ccccc1 | ||
| Formula | C9H8N2S | M.Wt | 176.2 |
| 溶解度 | ≥ 7.85mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.6754 mL | 28.3768 mL | 56.7537 mL |
| 5 mM | 1.1351 mL | 5.6754 mL | 11.3507 mL |
| 10 mM | 0.5675 mL | 2.8377 mL | 5.6754 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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