Zaragozic Acid A是一种角鲨烯合成酶抑制剂和真菌代谢产物，含有新颖的4,6,7-三羟基-2,8-二氧代双环[3.2.1]辛烷-3,4,5-三羧酸核。角鲨烯合酶催化胆固醇合成的第一步，介导法呢基焦磷酸的还原二聚化以产生角鲨烯。Zaragozic Acid A是一种真菌代谢产物，可作为角鲨烯合酶的可逆竞争性抑制剂（体外Ki = 78 pM）。Zaragozic Acid A剂量依赖性地降低HepG2细胞中的胆固醇合成（IC50 = 6 µM）并抑制小鼠的肝胆固醇合成（ED50 = 0.2 mg/kg). Zaragozic Acid A is a squalene synthetase inhibitor and fungal metabolite containing a novel 4,6,7-trihydroxy-2,8-dioxobicyclo[3.2.1]octane-3,4,5-tricarboxylic acid core. Squalene synthase catalyzes the first committed step in cholesterol synthesis, mediating the reductive dimerization of farnesyl pyrophosphate to produce squalene. Zaragozic Acid A is a fungal metabolite that acts as a reversible competitive inhibitor of squalene synthase (Ki = 78 pM in vitro). Zaragozic Acid A dose-dependently reduces cholesterol synthesis in HepG2 cells (IC50 = 6 μM) and inhibits hepatic cholesterol synthesis in mice (ED50 = 0.2 mg/kg).
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Zaragozic Acid A
Dangerous GoodsCAS number：142561-96-4 molecular formula：C35H46O14
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Specs
| Chinese alias | - | ||
| English alias | J-007666 | Zaragozic acid A | (1S,3S,4S,5R,6R,7R)-1-((4S,5R)-4-Acetoxy-5-methyl-3-methylene-6-phenyl-hexyl)-4,7-dihydroxy-6-((S)-6-methyl-4-methyl-oct-2-enoyloxy)-2,8-dioxa-bicyclo[3.2.1]octane-3,4,5-tricarboxylic acid | 3vjc | GTPL3057 | Ibacitabin | SQU | ||
| CAS number | 142561-96-4 | molecular formula | C35H46O14 |
| molecular weight | 690.73 g/mol | Exact mass | - |
| PSA | 223.000 Ų | logp | 4.900 |
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WGK Germany：
3
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