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SB-705498是有效，选择性和口服生物利用的TRPV1拮抗剂，抑制TRPV1的Capsaicin，酸和热激活，IC50分别为3 nM， 0.1 nM和6 nM，该作用具有一定的电压依赖性，作用于TRPV1比作用于TRPM8选择性高100倍以上。
靶点信息
| hTRPV1 | hTRPV1 | |||
| 7.6(pKi) | 7.1(pIC50) |
| In vitro | DMSO | 78 mg/mL (181.71 mM) | |
| Water | Insoluble | ||
| Ethanol | 18 mg/mL (41.93 mM) | ||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq 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. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 23.36 mL | 116.82 mL | 233.64 mL |
| 0.5 mM | 4.67 mL | 23.36 mL | 46.73 mL |
| 1 mM | 2.34 mL | 11.68 mL | 23.36 mL |
| 5 mM | 0.47 mL | 2.34 mL | 4.67 mL |
*The above data is based on the productmolecular weight 428.0 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 目录号 | A11143 |
|---|---|
| 作用机制 | Antagonist (拮抗剂) |
| M. Wt | 428.0 |
| Formula | C17H16BrF3N4O |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 501951-42-4 |
| Synonyms | SB705498 |
| SMILES | C1CN(C[C@@H]1NC(=O)NC2=CC=CC=C2Br)C3=NC=C(C=C3)C(F)(F)F |
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