M201-A | RyR2 inhibitor | Probechem Biochemicals

Chemical Structure : M201-A

M201-A (RyR2 inhibitor)

Catalog No.: PC-22420Not For Human Use, Lab Use Only.

M201-A is a potent, selective ryanodine receptor 2 (RyR2) inhibitor, inhibits G-protein-gated atrial K+ channel (IKACh) with IC50 of 0.35 uM.

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Biological Activity

M201-A is a potent, selective ryanodine receptor 2 (RyR2) inhibitor, inhibits G-protein-gated atrial K+ channel (IKACh) with IC50 of 0.35 uM.

M201-A significantly reduces the diastolic Ca2+ in isolated rat ventricular cardiomyocytes, exhibits positive lusi-inotropic effects on rat heart.

M201-A inhibits G-protein-gated atrial K+ channel (IKACh) at an IC50 value of 0.35 μM, which is associated with a 38% increase in the atrial effective refractory period (ERP) and high atrial selectivity with an atrial ERP/ventricular ERP of 5.7.

M201-A inhibits rapid component of the delayed rectifier potassium current (IC50 value of 0.43 μM) but induced only a limited prolongation in the action potential duration in rabbit ventricular cells and human induced pluripotent stem cell-derived cardiomyocytes.

M201-A is an R-enantiomer of the active metabolite M201-R of K201.

M201-A is 5-fold more biologically active than K201 in humans due to protein binding rates.

Physicochemical Properties

M.Wt	440.60
Formula	C25H32N2O3S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-4-[3-(4-benzylpiperidin-1-yl)propanoyl]-7-methoxy-2,3,4,5-tetrahydro-1,4-benzothiazepine-1-oxide

References

1. Noboru Kaneko, et al. Br J Pharmacol. 2024 May 21. doi: 10.1111/bph.16379.