AZD8329 is a potent, selective 11β-HSD1 inhibitor (11β-hydroxysteroid dehydrogenase type 1 inhibitor) with reduced acyl glucuronide liability. AZD8329 demonstrates to have improved technical profile in terms of both solubility and pharmacokinetics. The extent of acyl glucuronidation was reduced through structural optimization of both the carboxylic acid and amide substituents, coupled with a reduction in lipophilicity leading to an overall increase in metabolic stability.
CAS 1048668-70-7 MFCD148668707
化学结构图
SMILES: CC(C)(C)c1c(C(=O)NC2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)cnn1-c1ccc(C(=O)O)cc1
化学属性
| Mol. Weight | 421.53 |
|---|---|
| Appearance | White solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | AZD8329 is a potent, selective 11β-HSD1 inhibitor (11β-hydroxysteroid dehydrogenase type 1 inhibitor) with reduced acyl glucuronide liability. AZD8329 demonstrates to have improved technical profile in terms of both solubility and pharmacokinetics. The extent of acyl glucuronidation was reduced through structural optimization of both the carboxylic acid and amide substituents, coupled with a reduction in lipophilicity leading to an overall increase in metabolic stability. |
|---|---|
| Formula | C25H31N3O3 |
| Synonym | AZD8329; AZD-8329; AZD 8329. 44(2adamantylcarbamoyl)5tertbutylpyrazol1ylbenzoic acid |
| IUPAC Name | 4-(4-((1r,3r,5r,7r)-adamantan-2-ylcarbamoyl)-5-(tert-butyl)-1H-pyrazol-1-yl)benzoic acid |
| InChIKey | XWBXJBSVYVJAMZ-HNDAYGKNSA-N |
| InChI | InChI=1S/C25H31N3O3/c1-25(2,3)22-20(13-26-28(22)19-6-4-16(5-7-19)24(30)31)23(29)27-21-17-9-14-8-15(11-17)12-18(21)10-14/h4-7,13-15,17-18,21H,8-12H2,1-3H3,(H,27,29)(H,30,31)/t14-,15+,17-,18+,21? |
| Canonical SMILES | O=C(O)C1=CC=C(N2N=CC(C(NC3[C@H]4C[C@@H]5C[C@@H](C[C@H]3C5)C4)=O)=C2C(C)(C)C)C=C1 |
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- AZD8329 is a potent, selective 11β-HSD1 inhibitor (11β-hydroxysteroid dehydrogenase type 1 inhibitor) with reduced acyl glucuronide liability. AZD8329 demonstrates to have improved technical profile in terms of both solubility and pharmacokinetics. The extent of acyl glucuronidation was reduced through structural optimization of both the carboxylic acid and amide substituents, coupled with a reduction in lipophilicity leading to an overall increase in metabolic stability.
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