Chemical Structure : AM-001
CAS No.:
340817-81-4
AM-001
(AM001)
Catalog No.: PC-23228Not For Human Use, Lab Use Only.
AM-001 is a potent, selective and allosteric inhibitor of exchange proteins directly activated by cAMP 1 (EPAC1), inhibits Sp-8-CPT-induced Epac1 (EC50=47.8 uM) but not Epac2 activity.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
AM-001 is a potent, selective and allosteric inhibitor of exchange proteins directly activated by cAMP 1 (EPAC1), inhibits Sp-8-CPT-induced Epac1 (EC50=47.8 uM) but not Epac2 activity.
AM-001 shows .no antagonist effect on Epac2 or protein kinase A activity.
AM-001 prevents the activation of the Epac1 downstream effector Rap1 in cultured cells, in response to the Epac1 preferential agonist, 8-CPT-AM.
AM-001 reduces infarct size after mouse myocardial ischaemia/reperfusion injury. attenuates cardiac hypertrophy, inflammation and fibrosis, and improves cardiac function during chronic β-adrenergic receptor activation with isoprenaline (ISO) in mice.
Physicochemical Properties
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M.Wt
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445.53
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Formula
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C24H16FN3OS2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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3-amino-N-(4-fluorophenyl)-4-phenyl-6-(thiophen-2-yl)thieno[2,3-b]pyridine-2-carboxamide
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References
1. Bufano M, et al. J Comput Aided Mol Des. 2020 Nov;34(11):1171-1179.
2. Laudette M, et al. Cardiovasc Res. 2019 Oct 1;115(12):1766-1777.
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