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.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 218.21. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||4.58 mL||22.91 mL||45.83 mL|
|5 mM||0.92 mL||4.58 mL||9.17 mL|
|10 mM||0.46 mL||2.29 mL||4.58 mL|
|50 mM||0.09 mL||0.46 mL||0.92 mL|
References are publications that support the products' biological activity.
Cayen et al (1982) Evaluation of the lipid-lowering activity of AY-25,712 in rats. Atherosclerosis 45 267 PMID: 6818976
Jirkovsky and Cayen (1982) Hypolipidemic 4,5-dihydro-4-oxo-5,5-disubstituted-2-furancarboxylic acids. J.Med.Chem. 25 1154 PMID: 7143351
Jung et al (2007) Analogues of acrifan: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b. J.Med.Chem. 50 1445 PMID: 17358052
Wise et al (2003) Molecular identification of high and low affinity receptors for nicotinic acid. J.Biol.Chem. 278 9869 PMID: 12522134
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Keywords: Acifran, supplier, Hypolipidemic, agent, agonists, GPR109A, HM74A, GPR109B, receptors, HM74, nicotinic, acid, AY25712, AY, 25712, Hydroxycarboxylic, Acid, Receptors, Hydroxycarboxylic, Acid, Receptors, Tocris Bioscience
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