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Acifran

Cat. No. M6401
Acifran Structure
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Quality Control & Documentation
Biological Activity

Acifran is a hypolipidemic agent. Exhibits higher potency than nicotinic acid and clofibrate. Full and potent agonist at the human orphan GPCR HM74A/GPR109A and GPR109B (EC50 values are 1.3 and 4.2 μM respectively). Reduces serum triglycerides and circulating LDL-cholesterol in vivo, without affecting liver weight or liver enzymes.

Chemical Information
Molecular Weight 218.21
Formula C12H10O4
CAS Number 72420-38-3
Solubility (25°C) DMSO 21.82 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Vellenga, et al. Br J Pharmacol. Interleukin-6 production by activated human monocytic cells is enhanced by MK-571, a specific inhibitor of the multi-drug resistance protein-1.

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