A cell-permeable, orally active benzothiazepine that effectively blocks leaky intracellular calcium release by preventing the dissociation/depletion of calstabin from the ryanodine receptor (RyR) complex due to receptor modifications, such as oxidation, S-nitrosylation, hyperphosphorylation, or mutation (complete blockage of 1 mM tetracaine-induced leakage in murine RyR2 S2808D+/+ myocytes at 1uM). Shown to prevent stress-induced cognitive dysfunction by stabilizing RyR2-calstabin-2 (FKBP12.6) interaction in brain (75mg/kg/day, p.o.) and maintain exercise capacity by stabilizing RyR1-calstabin-1 (FKBP12) interaction in skeletal muscle (2.5ug/0.25uL/h/animal, s.c) in mice, as well as restore normal cardiac function (20mg/kg/day, s.c) in mice with R2474S or S2808D RyR2 mutation in vivo. Primary Target: RyR2 Synonyms: 7-methoxy-4-methyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine, Ryanodine Receptor Stabilizer, Rycal S107 Molecular Formula: C11H15NOS Molecular Weight: 209.3 Purity (HPLC): 98% Appearance: Supplied as an off-white solid. Solubility: A stock solution may be made by dissolving the S107 in an organic solvent purged with an inert gas. S107 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). The solubility of S107 in ethanol is approximately 0.5mg/ml and approximately 20mg/ml in DMSO and DMF. S107 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, S107 should first be dissolved in ethanol and then diluted with the aqueous buffer of choice. S107 has a solubility of approximately 0.5mg/ml in a 1:1 solution of ethanol:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day. Storage and Stability: Powder and reconstituted products are stable for 6 months after receipt at -20C. Reconstitute with DMSO. Aliquot to avoid repeated freezing and thawing. Store at -20C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap.
Molekulargewicht:
209.3
CAS Nummer:
[927871-76-9]
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
