| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| N423955-1ml |
1ml |
现货  |
|
| 英文别名 | 433695-36-4 | BRL-50481 | BRL 50481 | N,N,2-trimethyl-5-nitrobenzenesulfonamide | 5-Nitro-2,N,N-trimethylbenzenesulfonamide | N,N,2-Trimethyl-5-nitro-benzenesulfonamide | Benzenesulfonamide, N,N,2-trimethyl-5-nitro- | BRL50481 | CHEMBL484928 | N,N,2-trimethyl-5-nitrobenzen |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | N,N,2-Trimethyl-5-nitrobenzenesulfonamide |
| 生化机理 | BRL 50481 是一种强效、选择性 PDE7 抑制剂（IC50 = 260 nM）。选择性、竞争性 PDE7 抑制剂（对 PDE7A 和 PDE7B 的 IC50 值分别为 0.15 和 12.1 μm）。在体内和体外均有活性。增强 PDE4 抑制剂罗利普仑的抗炎作用 . |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 磷酸二酯酶 7A 抑制剂;磷酸二酯酶 7B 抑制剂 |
| 产品介绍 |
BRL-50481 is a selective inhibitor of phosphodiesterase 7 (PDE 7) that has acceptable selectivity for in vitro studies. Studies suggest that BRL-50481 is used to inhibit the activity of hrPDE7A1 which is usually expressed in baculovirus-infected Spodoptera frugiperda in a competitive manner. In osteoblasts, BRL-50481increases mineralization and bALP as a result of PDE7 silencing which upregulates several osteogenic genes. Further studies show that BRL-50481increases apoptosis in CLL cells via a mitochondrial-dependent process, and is associated with increased cAMP accumulation and down-regulation of the antiapoptotic protein survivin. BRL-50481 is a inhibitor of PDE7A. BRL-50481 is a selective inhibitor of phosphodiesterase 7 (PDE 7) that has acceptable selectivity for in vitro studies. Studies suggest that BRL-50481 is used to inhibit the activity of hrPDE7A1 which is usually expressed in baculovirus-infected Spodoptera frugiperda in a competitive manner. In osteoblasts, BRL-50481increases mineralization and bALP as a result of PDE7 silencing which upregulates several osteogenic genes. Further studies show that BRL-50481increases apoptosis in CLL cells via a mitochondrial-dependent process, and is associated with increased cAMP accumulation and down-regulation of the antiapoptotic protein survivin. BRL-50481 is a inhibitor of PDE7A. |
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| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | N,N,2-trimethyl-5-nitrobenzenesulfonamide |
| INCHI | InChI=1S/C9H12N2O4S/c1-7-4-5-8(11(12)13)6-9(7)16(14,15)10(2)3/h4-6H,1-3H3 |
| InChi Key | IFIUFCJFLGCQPH-UHFFFAOYSA-N |
| Canonical SMILES | CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)C |
| Isomeric SMILES | CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)C |
| WGK Germany | 3 |
| 分子量 | 244.27 |
| Reaxy-Rn | 9999290 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9999290&ln= |
| 敏感性 | 对热敏感 |
|---|---|
| 熔点 | 73 °C |
| 分子量 | 244.270 g/mol |
| XLogP3 | 1.300 |
| 氢键供体数Hydrogen Bond Donor Count | 0 |
| 氢键受体数Hydrogen Bond Acceptor Count | 5 |
| 可旋转键计数Rotatable Bond Count | 2 |
| 精确质量Exact Mass | 244.052 Da |
| 单同位素质量Monoisotopic Mass | 244.052 Da |
| 拓扑极表面积Topological Polar Surface Area | 91.600 Ų |
| 重原子数Heavy Atom Count | 16 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 355.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| WGK Germany | 3 |
|---|---|
| Reaxy-Rn | 9999290 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9999290&ln= |
| 个人防护装备 | Eyeshields， Gloves， type N95 (US)， type P1 (EN143) respirator filter |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Colorless Transparent Liquid) | Pass |
| Record the entire process by video | Conform |
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