Welcome to Shanghai Probechem Biochemicals Co Ltd !Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : MK-0354
CAS No.: 851776-28-8
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $128 | In stock | |
| 50 mg | $398 | In stock | |
| 100 mg | $678 | In stock | |
| 500 mg | Get quote | ||
| 1 g | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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.
| M.Wt | 176.1786 | |
| Formula | C7H8N6 | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
DMSO: ≥ 36 mg/mL |
|
| Chemical Name/SMILES |
Cyclopentapyrazole, 1,4,5,6-tetrahydro-3-(2H-tetrazol-5-yl)- |
|
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.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
