Biological Activity
High affinity and selective P2Y14 antagonist (KB = 434 pM). Exhibits >10,000-fold selectivity for P2Y14 over other P2Y receptors. Inhibits UDP-glucose and MRS 2690-induced porcine pancreatic artery contraction ex vivo. Also blocks UDP-glucose-induced chemotaxis of HL-60 leukemia cells in vitro.
Technical Data
M. Wt | 511.96 |
Formula | C29H24F3NO2.HCl |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
PubChem ID | 121513852 |
InChI Key | FKMVYPCBLWYNAV-UHFFFAOYSA-N |
Smiles | FC(F)(F)C(C=C4)=CC=C4C1=CC=C(C(C3=CC=C(C5CCNCC5)C=C3)=CC(C(O)=O)=C2)C2=C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 51.2 | 100 | |
ethanol | 10.24 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 511.96. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.95 mL | 9.77 mL | 19.53 mL |
5 mM | 0.39 mL | 1.95 mL | 3.91 mL |
10 mM | 0.2 mL | 0.98 mL | 1.95 mL |
50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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References
References are publications that support the products' biological activity.
Gao et al (2013) The role of P2Y14 and other P2Y receptors in degranulation of human LAD2 mast cells. Purinergic Signal. 9 31 PMID: 22825617
Alsaqati et al (2014) Novel vasocontractile role of the P2Y14 receptor: characterization of its signalling in porcine isolated pancreatic arteries. Br.J.Pharmacol. 171 701 PMID: 24138077
Barrett et al (2013) A selective high-affinity antagonist of the P2Y14 receptor inhibits UDP-glucose-stimulated chemotaxis of human neutrophils. Mol.Pharmacol. 84 41 PMID: 23592514
Keywords: PPTN hydrochloride, supplier, 1160271-30-6, high, affinity, selective, P2Y14, purinergics, antagonists, Purinergic, P2Y, Receptors, Purinergic, P2Y, Receptors, Tocris Bioscience