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MK-0354

Chemical Structure : MK-0354

CAS No.: 851776-28-8

MK-0354 (MK0354)

Catalog No.: PC-43317Not For Human Use, Lab Use Only.

MK-0354 is a potent, selective niacin receptor GPR109A partial agonist with EC50 of 1.65 and 1.08 uM for hGPR109A and mGPR109A in the whole cell cAMP assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

MK-0354 is a potent, selective niacin receptor GPR109A partial agonist with EC50 of 1.65 and 1.08 uM for hGPR109A and mGPR109A in the whole cell cAMP assays.
MK-0354 shows no interaction with any other target in a panel of over 120 other proteins.
MK-0354 is a competitive inhibitor of 3H-nicotinic acid binding to hGPR109a with Ki of 505 nM, fully inhibits isoproterenol stimulated lipolysis in human adipocytes with IC50 of 3.1 uM.
MK-0354 also is a competitive antagonist of nicotinic acid-induced MAPK signaling in cells overexpressing either mGPR109a or hGPR109a.
MK-0354 possesses plasma FFA lowering effects in mice comparable to those of nicotinic acid, does not induce vasodilation.

Physicochemical Properties

M.Wt 176.1786
Formula C7H8N6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 36 mg/mL

Chemical Name/SMILES

Cyclopentapyrazole, 1,4,5,6-tetrahydro-3-(2H-tetrazol-5-yl)-

References

1. Semple G, et al. J Med Chem. 2008 Aug 28;51(16):5101-8.

2. Lai E, et al. J Clin Lipidol. 2008 Oct;2(5):375-83.

3. Walters RW, et al. J Clin Invest. 2009 May;119(5):1312-21.

4. Gaidarov I, et al. Cell Signal. 2013 Oct;25(10):2003-16.

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