MRS2690
MRS2690 is a selective P2Y14 receptor agonist. MRS2690 inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 induces intracellular calcium mobilization, activates P38 and stimulates [35S]GTPγS binding to RBL-2H3 cell membranes. MRS2690 enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release. MRS2690can be used for ischemic heart disease.
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- CAS. Nr.: 7077-89-6
- Formel: C15H24N2O16P2S
- Molecular Weight:582.37
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | EC50 |
0.049 μM
Compound: 15, MRS-2690
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Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
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[PMID: 17407275] |
| COS-7 | EC50 |
0.049 μM
Compound: 2
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Agonist activity at human P2Y14 receptor expressed in human COS7 cells
Agonist activity at human P2Y14 receptor expressed in human COS7 cells
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[PMID: 19502066] |
| COS-7 | EC50 |
11 μM
Compound: 4
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Agonist activity at recombinant human P2Y14 receptor expressed in African green monkey COS7 cells co-transfected with Galphaqi assessed as stimulation of phospholipase Cbeta
Agonist activity at recombinant human P2Y14 receptor expressed in African green monkey COS7 cells co-transfected with Galphaqi assessed as stimulation of phospholipase Cbeta
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[PMID: 25868749] |
MRS2690 (0.001-10 μM) elicits concentration-dependent contractions of porcine isolated coronary arteries at basal tone (log EC50 = 6.30 M)[1].
MRS2690 (0.001-10 μM) shows enhanced concentration-dependent contractile responses in porcine coronary arteries pre-treated with Forskolin (HY-15371) plus U46619 (HY-108566) (Rmax = 1.77 g),which can be blocked by the P2Y14 antagonist PPTN (HY-110322A), but not affected by the P2Y6 antagonist MRS2578 (HY-13104)[1].
MRS2690 (10 μM) significantly reduces forskolin-induced VASP phosphorylation (an indicator of cAMP levels) in porcine coronary arteries[1].
MRS2690 (0.0001-1000 nM) induces intracellular calcium mobilization in RBL-2H3 cells in a concentration-dependent manner with an EC50 of 538 nM[2].
MRS2690 (0.0001-100 nM) stimulates [35S]GTPγS binding to RBL-2H3 cell membranes in a concentration-dependent manner with an EC50 of 8.1 nM[2].
MRS2690 (1 μM) activates P38 mitogen-activated protein kinase (MAPK) in RBL-2H3 cells[2].
MRS2690 alone cannot induce β-hexosaminidase (HEX) release, but it concentration-dependently enhances antigen (DNP-BSA)-induced HEX release in RBL-2H3 cells primed with anti-DNP-BSA antibody, with an EC50 of 103 nM[2].
MRS2690 (1 μM, 50 min) significantly enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release in LAD2 cells[3].
MRS2690 (10-1000 nM) significantly induces platelet-dependent neutrophil chemotaxis towards Macrophage derived chemokine (MDC, CCL22) in a concentration-dependent manner[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 7077-89-6
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Molecular Weight 582.37
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Formel C15H24N2O16P2S
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SMILES
OC[C@H]1O[C@@H]([C@@H]([C@H]([C@@H]1O)O)O)OP(O)(OP(O)(OC[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C(NC(C=C3)=O)=S)O2)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Abbas ZSB, et al. UDP-sugars activate P2Y14 receptors to mediate vasoconstriction of the porcine coronary artery. Vascul Pharmacol. 2018 Apr;103-105:36-46. [Content Brief]
[2]. Gao ZG, et al. UDP-glucose acting at P2Y14 receptors is a mediator of mast cell degranulation. Biochem Pharmacol. 2010 Mar 15;79(6):873-9. [Content Brief]
[3]. Gao ZG, et al. The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells. Purinergic Signal. 2013 Mar;9(1):31-40. [Content Brief]
[4]. Amison RT, et al. Lipopolysaccharide (LPS) induced pulmonary neutrophil recruitment and platelet activation is mediated via the P2Y1 and P2Y14 receptors in mice. Pulm Pharmacol Ther. 2017 Aug;45:62-68. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MRS2690 Related Classifications
HY-116295 Related Classifications
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