1047980-83-5
Chemical Structure
MRS2768
- CAS No.: 1047980-83-5
- Formula:C15H20N2O18P4
- Molecular Weight:640.22
InChIKey: XACAXTUDTIBBSW-FMKGYKFTSA-N
SMILES: O[C@@H]1[C@H](O)[C@@H](COP(OP(OP(OP(OC2=CC=CC=C2)(O)=O)(O)=O)(O)=O)(O)=O)O[C@H]1N3C(NC(C=C3)=O)=O
Biological Activity: MRS2768 is a potent, selective, and metabolically stable P2Y2 receptor agonist with an EC50 of 1.89 μM for the human P2Y2 receptor. MRS2768 activates Gq/PLC/PKC signaling, leading to downstream phosphorylation of Akt, eNOS, and ERK, with effects varying by cell type. MRS2768 inhibits ENaC via Gq/PKC/Src/Akt to promote natriuresis and lower blood pressure in the kidney. MRS2768 activates eNOS to increase NO secretion in endothelial cells. MRS2768 drives proliferation via PI3K/Akt in fibroblasts and cancer cells. MRS2768 exerts anti-apoptotic effects through PKC/Src/Akt in cardiomyocytes. MRS2768 can be applied to investigate P2Y2-dependent pathological processes, including acute kidney injury, chronic kidney disease and renal fibrosis, DOCA-salt induced hypertension, myocardial infarction, pulmonary arterial hypertension, pancreatic cancer, cardiac fibrosis, dry eye disease, as well as shear stress-mediated vascular remodeling and atherosclerosis[1][2][3][4][5][6][5][8][9][10][11][12][13].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
MRS2768 | MRS2768 is a potent, selective, and metabolically stable P2Y2 receptor agonist with an EC50 of 1.89 μM for the human P2Y2 receptor. MRS2768 activates Gq/PLC/PKC signaling, leading to downstream phosphorylation of Akt, eNOS, and ERK, with effects varying by cell type. MRS2768 inhibits ENaC via Gq/PKC/Src/Akt to promote natriuresis and lower blood pressure in the kidney. MRS2768 activates eNOS to increase NO secretion in endothelial cells. MRS2768 drives proliferation via PI3K/Akt in fibroblasts and cancer cells. MRS2768 exerts anti-apoptotic effects through PKC/Src/Akt in cardiomyocytes. MRS2768 can be applied to investigate P2Y2-dependent pathological processes, including acute kidney injury, chronic kidney disease and renal fibrosis, DOCA-salt induced hypertension, myocardial infarction, pulmonary arterial hypertension, pancreatic cancer, cardiac fibrosis, dry eye disease, as well as shear stress-mediated vascular remodeling and atherosclerosis. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Maruoka H, et al. Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphate δ-ester modifications as selective agonists of the P2Y(4) receptor. J Med Chem. 2011 Jun 23;54(12):4018-33. [Content Brief]
- [2]. Ko H, et al. Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists. Bioorg Med Chem. 2008 Jun 15;16(12):6319-32. [Content Brief]
- [3]. Jeong K, et al. Activation of Purinergic P2Y2 Receptor Protects the Kidney Against Renal Ischemia and Reperfusion Injury in Mice. Int J Mol Sci. 2024 Nov 22;25(23):12563. [Content Brief]
- [4]. Hochhauser E, et al. P2Y2 receptor agonist with enhanced stability protects the heart from ischemic damage in vitro and in vivo. Purinergic Signal. 2013 Dec;9(4):633-42. [Content Brief]
- [5]. Jeong K, et al. Deficiency of purinergic P2Y2 receptor impairs the recovery after renal ischemia-reperfusion injury and accelerates renal fibrosis and tubular senescence in mice. Sci Rep. 2024 Dec 30;14(1):31932. [Content Brief]
- [6]. Mironova E, et al. Renal Na+excretion consequent to pharmacogenetic activation of Gq-DREADD in principal cells. Am J Physiol Renal Physiol. 2019 Apr 1;316(4):F758-F767. [Content Brief]
- [8]. Fjærvoll KA, et al. Pyrimidinergic P2Y1-Like Nucleotide Receptors Are Functional in Rat Conjunctival Goblet Cells. Invest Ophthalmol Vis Sci. 2025 Jan 2;66(1):46. [Content Brief]
- [9]. Sathanoori R, et al. P2Y2 receptor modulates shear stress-induced cell alignment and actin stress fibers in human umbilical vein endothelial cells. Cell Mol Life Sci. 2017 Feb;74(4):731-746. [Content Brief]
- [10]. Alsaqati M, et al. Investigation of the functional expression of purine and pyrimidine receptors in porcine isolated pancreatic arteries. Purinergic Signal. 2014;10(2):241-9. [Content Brief]
- [11]. Certal M, et al. Calcium signaling and the novel anti-proliferative effect of the UTP-sensitive P2Y11 receptor in rat cardiac myofibroblasts. Cell Calcium. 2015 Nov;58(5):518-33. [Content Brief]
- [12]. Soares AG, et al. P2Y2 receptor decreases blood pressure by inhibiting ENaC. JCI Insight. 2023 Jul 24;8(14):e167704. [Content Brief]
- [13]. Stockburger J, et al. The physiological function of the purinergic receptor P2Y2 in pulmonary arterial endothelial cells and its role in pulmonary hypertension. Pneumologie. 2020;74(S 01):18.
