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MAY0132

Cat. No. M8614
MAY0132 Structure
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Biological Activity

MAY0132 is a selective inhibitor of the cAMP-binding Protein EPAC2 (Exchange Protein directly Activated by Cyclic AMP) subtype 2. MAY0132 has a submicromolar IC50 value at EPAC2, and no activity at EPAC1. MAY0132 is believed to act at an allosteric site, perhaps at the interface of both cAMP binding domains in the EPAC2 protein.

Chemical Information
Molecular Weight 313.75
Formula C16H15ClF3N
CAS Number 1895861-88-7
Solubility (25°C) DMSO: 20 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] Eun-Jin Choi, et al. Broad Impact of Exchange Protein Directly Activated by cAMP 2 (EPAC2) on Respiratory Viral Infections

[2] Urooj Qureshi, et al. Identification of novel Epac2 antagonists through in silico and in vitro analyses

[3] Abdul Hameed, et al. Coixol amplifies glucose-stimulated insulin secretion via cAMP mediated signaling pathway

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Keywords: MAY0132 supplier, inhibitors, activators


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