Sulfaphenazole

製品コードS3673 バッチS367302

印刷

化学情報

Chemical Structure Synonyms Depocid, Depotsulfonamide, Plisulfan, Raziosulfa Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C15H14N4O2S
分子量 314.36 CAS No. 526-08-9
Solubility (25°C)* 体外 DMSO 63 mg/mL (200.4 mM)
Ethanol 20 mg/mL (63.62 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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).
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 DU145 cells
濃度 50, 100, 150, 200 μM
反応時間 --
実験の流れ 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.
動物実験 動物モデル wild-type (Wt) and R6/2 mice
投薬量 112, 225, and 400 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Die Optimierung einer Multiplex-Färbung für verschiedene Metastasen des Melanoms [ UNIVERSITY OF APPLIED SCIENCES, 2023, ] PubMed: none
Potential herb-drug interaction risk of thymoquinone and phenytoin [ Chem Biol Interact, 2022, 353:109801] PubMed: 34998822
Potential food-drug interaction risk of thymoquinone with warfarin [ Chem Biol Interact, 2022, 365:110070] PubMed: 35921950

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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