Molecular structure of Acifran, CAS Number: 72420-38-3
Acifran (CAS 72420-38-3)
Alternate Names:
AY 25712
Application:
Acifran is an agonist at the human orphan GPCR HM74A/GPR109A and GPR109B
CAS Number:
72420-38-3
Purity:
≥95%
Molecular Weight:
218.21
Molecular Formula:
C12H10O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Acifran is a hypolipidaemic agent; more potent than nicotinic acid and clofibrate. Full and potent agonist at the human orphan GPCR HM74A/GPR109A and HM74B (GPR109B) (EC50 values are 1.3 and 4.2 μM respectively). Can reduce serum triglycerides and circulating LDL-cholesterol in vivo, without having an effect on liver weight or liver enzymes.
Acifran (CAS 72420-38-3) References
- Molecular identification of high and low affinity receptors for nicotinic acid. | Wise, A., et al. 2003. J Biol Chem. 278: 9869-74. PMID: 12522134
- (D)-beta-Hydroxybutyrate inhibits adipocyte lipolysis via the nicotinic acid receptor PUMA-G. | Taggart, AK., et al. 2005. J Biol Chem. 280: 26649-52. PMID: 15929991
- Characterization of determinants of ligand binding to the nicotinic acid receptor GPR109A (HM74A/PUMA-G). | Tunaru, S., et al. 2005. Mol Pharmacol. 68: 1271-80. PMID: 16099840
- Niacin induces PPARgamma expression and transcriptional activation in macrophages via HM74 and HM74a-mediated induction of prostaglandin synthesis pathways. | Knowles, HJ., et al. 2006. Biochem Pharmacol. 71: 646-56. PMID: 16386710
- Langerhans cells release prostaglandin D2 in response to nicotinic acid. | Maciejewski-Lenoir, D., et al. 2006. J Invest Dermatol. 126: 2637-46. PMID: 17008871
- Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b. | Jung, JK., et al. 2007. J Med Chem. 50: 1445-8. PMID: 17358052
- Role of GPR81 in lactate-mediated reduction of adipose lipolysis. | Cai, TQ., et al. 2008. Biochem Biophys Res Commun. 377: 987-91. PMID: 18952058
- GPR109A is a G-protein-coupled receptor for the bacterial fermentation product butyrate and functions as a tumor suppressor in colon. | Thangaraju, M., et al. 2009. Cancer Res. 69: 2826-32. PMID: 19276343
- Differential tissue and ligand-dependent signaling of GPR109A receptor: implications for anti-atherosclerotic therapeutic potential. | Gaidarov, I., et al. 2013. Cell Signal. 25: 2003-16. PMID: 23770183
- Niacin receptor activation improves human microvascular endothelial cell angiogenic function during lipotoxicity. | Hughes-Large, JM., et al. 2014. Atherosclerosis. 237: 696-704. PMID: 25463108
- The role of the C-terminus of the human hydroxycarboxylic acid receptors 2 and 3 in G protein activation using Gα-engineered yeast cells. | Liu, R., et al. 2016. Eur J Pharmacol. 770: 70-7. PMID: 26656756
- 3-(3-Hydroxyphenyl)-Propionic Acid (PPA) Suppresses Osteoblastic Cell Senescence to Promote Bone Accretion in Mice. | Chen, JR., et al. 2019. JBMR Plus. 3: e10201. PMID: 31667457
- Computational insights on molecular interactions of acifran with GPR109A and GPR109B. | Adepu, KK., et al. 2022. J Mol Model. 28: 237. PMID: 35900600
- The metabolic disposition of acifran, a new antihyperlipidemic agent, in rats and dogs. | Cayen, MN., et al. 1986. Xenobiotica. 16: 251-63. PMID: 3705621
- Evaluation of the lipid-lowering activity of AY-25,712 in rats. | Cayen, MN., et al. 1982. Atherosclerosis. 45: 267-79. PMID: 6818976
- Hypolipidemic 4,5-dihydro-4-oxo-5,5-disubstituted-2-furancarboxylic acids. | Jirkovsky, I. and Cayen, MN. 1982. J Med Chem. 25: 1154-6. PMID: 7143351
Activator of:
HM74A, and HM74B.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Acifran, 10 mg | sc-203496 | 10 mg | $141.00 | |||
| US: Only available in the US | ||||||
Acifran, 50 mg | sc-203496A | 50 mg | $585.00 | |||
| US: Only available in the US | ||||||