64273-28-5 Usage
Uses
Used in Pharmaceutical Industry:
5-METHYL-4-PHENYL-1,2,3-THIADIAZOLE is used as a selective, mechanism-based inhibitor for [application reason] targeting specific cytochrome P450 enzymes, CYP2B4 and CYP2E1. This selective inhibition can be beneficial in the development of drugs that require precise control over metabolic pathways, potentially leading to more effective and safer medications.
5-METHYL-4-PHENYL-1,2,3-THIADIAZOLE's ability to inhibit specific cytochrome P450 enzymes makes it a valuable tool in the pharmaceutical industry for drug development and understanding the metabolic processes of various medications. By selectively targeting these enzymes, 5-METHYL-4-PHENYL-1,2,3-THIADIAZOLE can help researchers and pharmaceutical companies optimize drug interactions and minimize potential side effects or toxicities associated with certain metabolic pathways.
Biological Activity
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].
references
[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).
Check Digit Verification of cas no
The CAS Registry Mumber 64273-28-5 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 6,4,2,7 and 3 respectively; the second part has 2 digits, 2 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 64273-28:
(7*6)+(6*4)+(5*2)+(4*7)+(3*3)+(2*2)+(1*8)=125
125 % 10 = 5
So 64273-28-5 is a valid CAS Registry Number.
InChI:InChI=1/C9H8N2S/c1-7-9(10-11-12-7)8-5-3-2-4-6-8/h2-6H,1H3
64273-28-5Relevant academic research and scientific papers
ARYL GPR120 RECEPTOR AGONISTS AND USES THEREOF
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Page/Page column 68, (2010/05/13)
Aryl GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
