Biological Activity
Selective antagonist of P2Y6 nucleotide receptors; IC50 values are 37 and 98 nM at human and rat P2Y6 receptors respectively. Displays no activity at P2Y1, P2Y2, P2Y4 and P2Y11 receptors (IC50 > 10 μM). Inhibits agonist-induced cardiomyocyte contraction and UDP-induced phagocytosis.
Technical Data
M. Wt | 472.66 |
Formula | C20H20N6S4 |
Storage | Desiccate at -20°C |
Purity | ≥95% (HPLC) |
CAS Number | 711019-86-2 |
PubChem ID | 16078986 |
InChI Key | QOHNRGHTJPFMSL-UHFFFAOYSA-N |
Smiles | S=C(NCCCCNC(NC2=CC(N=C=S)=CC=C2)=S)NC1=CC(N=C=S)=CC=C1 |
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 | 23.63 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 472.66. 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 | 2.12 mL | 10.58 mL | 21.16 mL |
5 mM | 0.42 mL | 2.12 mL | 4.23 mL |
10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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References
References are publications that support the products' biological activity.
Mamedova et al (2004) Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors. Biochem.Pharmacol. 67 1763 PMID: 15081875
Koizumi et al (2007) UDP acting at P2Y6 receptors is a mediator of microglial phagocytosis. Nature 446 1091 PMID: 17410128
Kukulski et al (2007) Extracellular nucleotides mediate LPS-induced neutrophil migration in vitro and in vivo. J.Leukoc.Biol. 81 1269 PMID: 17322022
Keywords: MRS 2578, supplier, Selective, P2Y6, antagonists, Receptors, Purinergic, purinoceptors, MRS2578, Purinergic, P2Y, Receptors, Purinergic, P2Y, Receptors, Tocris Bioscience