磺胺苯吡唑
货号：
IS2360
品牌：
Jinpan
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产品简介
| 有效期 | 2年 |
| MDL | MFCD00057226 |
| EC | EINECS 208-384-3 |
| InChIKey | QWCJHSGMANYXCW-UHFFFAOYSA-N |
| InChI | InChI=1S/C15H14N4O2S/c16-12-6-8-14(9-7-12)22(20,21)18-15-10-11-17-19(15)13-4-2-1-3-5-13/h1-11,18H,16H2 |
| PubChem CID | 5335 |
| 别名 | 苯磺酰胺 |
| 英文名称 | Sulfaphenazole |
| CAS | 526-08-9 |
| 分子式 | C15H14N4O2S |
| 分子量 | 314.36 |
| 储存条件 | 2-8℃ |
| 纯度 | ≥98% |
| 外观（性状） | White to pale yellow Powder |
| 单位 | 瓶 |
| 生物活性 | 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).[1-2] |
| 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]. |
| SMILES | O=S(C1=CC=C(N)C=C1)(NC2=CC=NN2C3=CC=CC=C3)=O |
| 靶点 | CYP2C9 |
| 动物实验 | 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.[1] |
| 细胞实验 | Animal Models: wild-type (Wt) and R6/2 mice; Dosages: 112, 225, and 400 mg/kg; Administration: i.p.[2] |
| 数据来源文献 | [1] Jeon JH, et al. Exp Mol Med. 2004, 36(6):576-81. [2] Dedeoglu A, et al. J Neurosci. 2002, 22(20):8942-50. |
| 规格 | 50mg 100mg |
是CYP2C9的特异性抑制剂。
