1268882-43-4
Chemical Structure
MK-1903
- CAS 番号: 1268882-43-4
- Formula:C8H8N2O2
- Molecular Weight:164.16
IUPAC Name: (4aR,5aR)-4,4a,5,5a-tetrahydro-1H-cyclopropa[4,5]cyclopenta[1,2-c]pyrazole-3-carboxylic acid
InChIKey: CUTZNERBKDMLAP-QWWZWVQMSA-N
SMILES: OC(C1=NNC2=C1C[C@]3([H])[C@@]2([H])C3)=O
Biological Activity: MK-1903 is an orally active full agonist of GPR109a/HCAR2, with an EC50 of 12.9 nM. MK-1903 activates antilipolytic and vasodilatory pathways, reduces plasma free fatty acid levels, and induces skin flushing. MK-1903 stimulates the expression of HCAR2 protein and regulates the inflammatory response of microglia. MK-1903 prevents the enhanced firing activity of spinal nociceptive neurons. MK-1903 triggers the release of MMP-9 and the formation of NET. MK-1903 can be used in the research of dyslipidemia and neuroinflammation-based central nervous system diseases[1][2][3].
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MK-1903 | 99.68% | MK-1903 is an orally active full agonist of GPR109a/HCAR2, with an EC50 of 12.9 nM. MK-1903 activates antilipolytic and vasodilatory pathways, reduces plasma free fatty acid levels, and induces skin flushing. MK-1903 stimulates the expression of HCAR2 protein and regulates the inflammatory response of microglia. MK-1903 prevents the enhanced firing activity of spinal nociceptive neurons. MK-1903 triggers the release of MMP-9 and the formation of NET. MK-1903 can be used in the research of dyslipidemia and neuroinflammation-based central nervous system diseases. | ||||||||||||||||||||
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MK-1903 (Standard) | ≥98% | MK-1903 (Standard) is the analytical standard of MK-1903 (HY-107581). This product is intended for research and analytical applications. MK-1903 is an orally active full agonist of GPR109a/HCAR2, with an EC50 of 12.9 nM. MK-1903 activates antilipolytic and vasodilatory pathways, reduces plasma free fatty acid levels, and induces skin flushing. MK-1903 stimulates the expression of HCAR2 protein and regulates the inflammatory response of microglia. MK-1903 prevents the enhanced firing activity of spinal nociceptive neurons. MK-1903 triggers the release of MMP-9 and the formation of NET. MK-1903 can be used in the research of dyslipidemia and neuroinflammation-based central nervous system diseases. | ||||||||||||||||||||
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[1]. Boatman PD, et al. (1a R, 5a R) 1a, 3, 5, 5a-Tetrahydro-1 H-2, 3-diaza-cyclopropa [a] pentalene-4-carboxylic Acid (MK-1903): A Potent GPR109a Agonist that Lowers Free Fatty Acids in Humans. Journal of medicinal chemistry. 2012 Apr 26;55(8):3644-66.
- [2]. Perrone M, et al. Potential role of the hydroxyl carboxylic acid receptor type 2 (HCAR2) in microglia pathophysiology: A possible cross-talk with C-X-C chemokine receptor 1 (CXCR1). Neuropharmacology. 2023;228:109456. [Content Brief]
- [3]. Carretta MD, et al. Hydroxycarboxylic acid receptor 2 (HCA2) agonists induce NET formation and MMP-9 release from bovine polymorphonuclear leukocytes. Dev Comp Immunol. 2023;139:104562. [Content Brief]
Keywords
