1228271-30-4
Chemical Structure
MRS2957
- CAS No.: 1228271-30-4
- Formula:C19H28N5O20P3
- Molecular Weight:739.37
InChIKey: SIKKMGJHOOQSAP-RTGFKBDUSA-N
SMILES: O[C@@H]1[C@H](O)[C@@H](COP(OP(OP(OC[C@H]([C@@H](O)[C@H]2O)O[C@H]2N(C(N3)=O)C=CC3=O)(O)=O)(O)=O)(O)=O)O[C@H]1N(C(N/4)=O)C=CC4=N\OC
Biological Activity: MRS2957 is a selective P2Y6 receptor agonist. MRS2957 activates Gq-coupled purinergic receptors, increasing phospholipase C, inositol trisphosphate, and intracellular calcium, and indirectly activates AMPK via CaMKKβ, thereby promoting P2Y6-dependent glucose uptake and GLUT4 translocation in skeletal muscle cells and adipocytes. MRS2957 can be used for research on type 2 diabetes[1][2][3][4][5][6][7].
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MRS2957 | MRS2957 is a selective P2Y6 receptor agonist. MRS2957 activates Gq-coupled purinergic receptors, increasing phospholipase C, inositol trisphosphate, and intracellular calcium, and indirectly activates AMPK via CaMKKβ, thereby promoting P2Y6-dependent glucose uptake and GLUT4 translocation in skeletal muscle cells and adipocytes. MRS2957 can be used for research on type 2 diabetes. | |||||||||||||||||||||
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References
- [1]. Figurek A, et al. Pyrimidinergic calcium signaling links tubular metabolism to fibrosis in kidney disease. Nature communications. 2026 Feb 19;17(1):3004.
- [2]. Balasubramanian R, et al. AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin secretion in mouse pancreatic β-cells. Biochemical pharmacology. 2013 Apr 01;85(7):991-8.
- [3]. Jacobson KA, et al. John Daly Lecture: Structure-guided drug design for adenosine and P2Y receptors.
- [4]. Balasubramanian R, et al. Enhancement of glucose uptake in mouse skeletal muscle cells and adipocytes by P2Y6 receptor agonists. PloS one. 2014;9(12):e116203.
- [5]. Jain S, et al. Adipocyte purinergic receptors activated by uracil nucleotides as obesity and type 2 diabetes targets. Current opinion in pharmacology. 2022 Apr;63:102190.
- [6]. Maruoka H, et al. Pyrimidine ribonucleotides with enhanced selectivity as P2Y(6) receptor agonists: novel 4-alkyloxyimino, (S)-methanocarba, and 5'-triphosphate gamma-ester modifications. Journal of medicinal chemistry. 2010 Jun 10;53(11):4488-501. [Content Brief]
- [7]. Jayasekara PS, et al. 4-Alkyloxyimino derivatives of uridine-5'-triphosphate: distal modification of potent agonists as a strategy for molecular probes of P2Y2, P2Y4, and P2Y6 receptors. Journal of medicinal chemistry. 2014 May 08;57(9):3874-83.
