A reversible competitive inhibitor of squalene synthase (Ki = 78 pM in vitro); reduces cholesterol synthesis in HepG2 cells (IC50 = 6 µM) and inhibits hepatic cholesterol synthesis in mice (ED50 = 0.2 mg/kg); also inhibits FPTase and GGTase-I (IC50s = 216 and 50 nM

Zaragozic Acid A – 1 mg

Brand:
Cayman
CAS:
142561-96-4
Storage:
-20
UN-No:
Non-Hazardous - /

Squalene synthase catalyzes the first committed step in cholesterol synthesis, mediating the reductive dimerization of farnesyl pyrophosphate (Item No. 63250) to produce squalene.{15286} Zaragozic acid A is a fungal metabolite that acts as a reversible competitive inhibitor of squalene synthase (Ki = 78 pM in vitro).{28249} It dose-dependently reduces cholesterol synthesis in HepG2 cells (IC50 = 6 µM) and inhibits hepatic cholesterol synthesis in mice (ED50 = 0.2 mg/kg).{28249} Zaragozic acid A also inhibits farnesy transferase (FTase) and geranylgeranyl transferase type I (GGTase I) (IC50s = 216 and 50 nM, respectively).{1196}  

 

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Description

A reversible competitive inhibitor of squalene synthase (Ki = 78 pM in vitro); reduces cholesterol synthesis in HepG2 cells (IC50 = 6 µM) and inhibits hepatic cholesterol synthesis in mice (ED50 = 0.2 mg/kg); also inhibits FPTase and GGTase-I (IC50s = 216 and 50 nM, respectively)

Formal name: (7S)-11-acetate 5-[(2E,4S,6S)-4,6-dimethyl-2-octenoate]-2,7-anhydro-3,4-di-C-carboxy-8,9,10,12,13-pentadeoxy-10-methylene-12-(phenylmethyl)-L-erythro-L-glycero-D-altro-7-trideculo-7,4-furanosonic acid

Synonyms:  L-694,599|Squalestatin S1

Molecular weight: 690.7

CAS: 142561-96-4

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Natural Products|Microbial Metabolites||Product Type|Biochemicals|Small Molecule Inhibitors|Sterol Biosynthesis||Research Area

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