Description
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 . In vivo: Up to now, there is no animal in vivo data reported. Clinical trial: So far, no clinical study has been conducted.
Product information
CAS Number: 152467-47-5
Molecular Weight: 200.24
Formula: C6H4N2O2S2
Chemical Name: methyl thieno[3,2-d][1,2,3]thiadiazole-6-carboxylate
Smiles: COC(=O)C1=CSC2SN=NC=21
InChiKey: FMCBCIKSEQJAGA-UHFFFAOYSA-N
InChi: InChI=1S/C6H4N2O2S2/c1-10-5(9)3-2-11-6-4(3)7-8-12-6/h2H,1H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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