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2-Methylthioadenosine diphosphate trisodium

Cat. No. M30139
2-Methylthioadenosine diphosphate trisodium Structure
Synonym:

2-Methylthio-ADP trisodium

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Biological Activity

2-Methylthioadenosine diphosphate trisodium is a potent purinergic P2Y receptors agonist, with EC50s of 19, 6.2, and 5 nM for human P2Y13, mouse P2Y13 and human P2Y12, respectively. 2-Methylthioadenosine diphosphate trisodium has pEC50s of 8.29 and 5.75 for human P2Y1 and rat P2Y6, respectively. 2-Methylthioadenosine diphosphate trisodium induces platelet aggregation and shape change, and inhibits cyclic AMP accumulation in platelets exposed to prostaglandin E1.

Chemical Information
Molecular Weight 539.24
Formula C11H14N5Na3O10P2S
CAS Number 475193-31-8
Form Liquid
Storage -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Shulan Pi, et al. Autophagy. The P2RY12 receptor promotes VSMC-derived foam cell formation by inhibiting autophagy in advanced atherosclerosis

[2] Andrew Fedoriw, et al. Cancer Cell. Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss

[3] Katya Marjon, et al. Cell Rep. MTAP Deletions in Cancer Create Vulnerability to Targeting of the MAT2A/PRMT5/RIOK1 Axis

[4] C Quintas, et al. Neuroscience. Opposite modulation of astroglial proliferation by adenosine 5'-O-(2-thio)-diphosphate and 2-methylthioadenosine-5'-diphosphate: mechanisms involved

[5] D E Macfarlane, et al. J Clin Invest. 2-Methylthioadenosine[beta-32P]diphosphate. An agonist and radioligand for the receptor that inhibits the accumulation of cyclic AMP in intact blood platelets

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Keywords: 2-Methylthioadenosine diphosphate trisodium, 2-Methylthio-ADP trisodium supplier, P2 Receptor, inhibitors, activators


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