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Zaragozic Acid A

Cat. No. M11347
Zaragozic Acid A Structure
Size Price Availability
1mg USD 500  USD500 1-2 Weeks
5mg USD 1200  USD1200 1-2 Weeks
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Quality Control & Documentation
Biological Activity

Zaragozic acid A is an inhibitor of acute liver cholsterol synthesis (50% inhibition dose 200 μg/ kg) with Ki value of 78pM. It inhibited cholesterol synthesis in Hep G2 cells.

Chemical Information
Molecular Weight 690.73
Formula C35H46O14
CAS Number 142561-96-4
Storage -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Nicholas Liu, et al. Org Lett. Identification and Heterologous Production of a Benzoyl-Primed Tricarboxylic Acid Polyketide Intermediate from the Zaragozic Acid A Biosynthetic Pathway

[2] Chia-I Liu, et al. J Biol Chem. Binding modes of zaragozic acid A to human squalene synthase and staphylococcal dehydrosqualene synthase

[3] R G Bostedor, et al. J Biol Chem. Farnesol-derived dicarboxylic acids in the urine of animals treated with zaragozic acid A or with farnesol

[4] T S Chen, et al. J Antibiot (Tokyo). The preparation of zaragozic acid A analogues by directed biosynthesis

[5] S Lindsey, et al. J Biol Chem. Inhibition of mammalian squalene synthetase activity by zaragozic acid A is a result of competitive inhibition followed by mechanism-based irreversible inactivation

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Keywords: Zaragozic Acid A supplier, Squalene synthase, inhibitors, activators


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