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MRS 2395

Cat. No. M7932
MRS 2395 Structure
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Biological Activity

Antagonist for P2Y12 purinoceptor; inhibits ADP-induced aggregation in rat platelets and antagonizes ADP-induced inhibition of cAMP in rat and human platelets in the presence of PGE1 without affecting P2Y1 receptor-induced PLC activity in transfected astrocytoma cells.

Chemical Information
Molecular Weight 439.94
Formula C20H30ClN5O4
CAS Number 491611-55-3
Solubility (25°C) DMSO: ≥10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Feng Jing, et al. P2Y12 receptor mediates microglial activation via RhoA/ROCK pathway in the trigeminal nucleus caudalis in a mouse model of chronic migraine

[2] Annachiara Mitrugno, et al. Potentiation of TRAP-6-induced platelet dense granule release by blockade of P2Y 12 signaling with MRS2395

[3] Hideaki Shirasaki, et al. Leukotriene E4 induces MUC5AC release from human airway epithelial NCI-H292 cells

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

[5] M G Zizzo, et al. Evidence that ATP or a related purine is an excitatory neurotransmitter in the longitudinal muscle of mouse distal colon

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