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4-phenyl-5-methyl-1,2,3-Thiadiazole

Catalog No.
C4429
CYP2B4 and CYP2E1 inhibitor
Grouped product items
SizePriceStock Qty
1g
$67.00
Ship with 5-10 days
5g
$298.00
Ship with 5-10 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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).

Chemical Properties

StorageStore at -20°C
M.Wt176.2
Cas No.64273-28-5
FormulaC9H8N2S
SynonymsNSC 358739
Solubilityinsoluble in H2O; ≥10.38 mg/mL in EtOH; ≥7.85 mg/mL in DMSO
Chemical Name5-methyl-4-phenyl-1,2,3-thiadiazole
SDFDownload SDF
Canonical SMILESCc1snnc1c1ccccc1
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

4-phenyl-5-methyl-1,2,3-Thiadiazole