Sulfaphenazole

Synonyms: Depocid, Depotsulfonamide, Plisulfan, Raziosulfa

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 Chemical Structure

Sulfaphenazole Chemical Structure

CAS No. 526-08-9

Purity & Quality Control

Sulfaphenazole Related Products

Biological Activity

Description 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).
Targets
CYP2C9 [1]
(Cell-free assay)
0.3 μM(Ki)
In vitro
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].
Cell Research Cell lines DU145 cells
Concentrations 50, 100, 150, 200 μM
Incubation Time --
Method The cells (2×106) are labeled with BP at 1 mM or amine compounds (0 to 1.0 mM) in serum-free medium for 1h prior to harvesting. After washing twice with PBS, the cells are suspended in PBS containing protease inhibitors and sonicated (2 s pulse/2 s pause×5, 20% amplitude). The homogenate is centrifuged for 10 min at 20,000g at 4℃. The cell extract(0.2 mg/ml, 50 μl/well) is coated in the wells of a 96-well microtiter plate for 12 h at 4℃. The wells are then overcoated with 5% BSA in PBS for 1 h at room temperature. After washing three times with PBST, BP incorporated into the cellular proteins is assessed as performed in microtiter plate assays.
In Vivo
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].
Animal Research Animal Models wild-type (Wt) and R6/2 mice
Dosages 112, 225, and 400 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 314.36 Formula

C15H14N4O2S

CAS No. 526-08-9 SDF Download Sulfaphenazole SDF
Smiles C1=CC=C(C=C1)N2C(=CC=N2)NS(=O)(=O)C3=CC=C(C=C3)N
Storage (From the date of receipt)

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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Sulfaphenazole | Sulfaphenazole supplier | purchase Sulfaphenazole | Sulfaphenazole cost | Sulfaphenazole manufacturer | order Sulfaphenazole | Sulfaphenazole distributor