Home Metabolism P450 (e.g. CYP17) inhibitor Sulfaphenazole

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Sulfaphenazole P450 (e.g. CYP17) inhibitor

Cat.No.S3673

Sulfaphenazole (Depocid, Depotsulfonamide, Plisulfan, Raziosulfa) is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).
Sulfaphenazole P450 (e.g. CYP17) inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 314.36

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Chemical Information, Storage & Stability

Molecular Weight 314.36 Formula

C15H14N4O2S

 Storage (From the date of receipt)
CAS No. 526-08-9 Download SDF Storage of Stock Solutions

Synonyms Depocid, Depotsulfonamide, Plisulfan, Raziosulfa Smiles C1=CC=C(C=C1)N2C(=CC=N2)NS(=O)(=O)C3=CC=C(C=C3)N

Solubility

In vitro
Batch:

DMSO : 63 mg/mL ( (200.4 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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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.

Mechanism of Action

Targets/IC50/Ki
CYP2C9 [1]
(Cell-free assay)
0.3 μM(Ki)
In vitro
Cystamine is a transglutaminase (TGase) inhibitor. In addition to TGase inhibition, cystamine is able to replenish glutathione and to inhibit caspase activity. The inhibitory capacity of cystamine in vitro is largely affected by the extent of the reduced form of the molecule. Nonetheless, cystamine inhibits in situ TGase activity decidedly stronger than cysteamine[1].
In vivo
Treatment with cystamine results in prolonged survival and decreased abnormal movements in a murine model of HD（Huntington's disease）. Cystamine does not cross the blood brain barrier[1]. Cystamine treatment normalizes transglutaminase and GGEL levels in R6/2 mice. cystamine has significant efficacy in improving the neurological and neuropathological phenotype observed in the R6/2 transgenic model of HD and strongly suggests that Tgase plays a role in HD[2].
References

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