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500469 RyR-Calstabin Interaction Stabilizer, S107 - CAS 927871-76-9 - Calbiochem

RyR-Calstabin Interaction Stabilizer, S107 - CAS 927871-76-9 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 7-methoxy-4-methyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine, Ryanodine Receptor Stabilizer, Rycal S107

Primary Target: RyR2
500469
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Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

CAS #Empirical Formula
927871-76-9C₁₁H₁₅NOS

Products

KatalógusszámCsomagolás Menny./csomag
5.00469.0001 Üvegpalack 10 mg
Description
OverviewA 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 1 µM). Shown to prevent stress-induced cognitive dysfunction by stabilizing RyR2-calstabin-2 (FKBP12.6) interaction in brain (75 mg/kg/day; p.o.) and maintain exercise capacity by stabilizing RyR1-calstabin-1 (FKBP12) interaction in skeletal muscle (2.5 µg/0.25µL/h/animal; s.c) in mice, as well as restore normal cardiac function (20 mg/kg/day; s.c) in mice with R2474S or S2808D RyR2 mutation in vivo.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number500469
Brand Family Calbiochem®
Synonyms7-methoxy-4-methyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine, Ryanodine Receptor Stabilizer, Rycal S107
References
ReferencesLiu, X., et al. 2012. Cell. 150, 1055.
Shan, J., et al. 2010. J. Clin. Invest. 120, 4375.
Bellinger, A. M., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 2198.
Lehnart, S.E., et al. 2008. J. Clin. Invest. 118, 2230.
Product Information
CAS number927871-76-9
FormOff-white solid
Hill FormulaC₁₁H₁₅NOS
Chemical formulaC₁₁H₁₅NOS
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetRyR2
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalógusszám GTIN
5.00469.0001 04055977245547

Documentation

RyR-Calstabin Interaction Stabilizer, S107 - CAS 927871-76-9 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Hivatkozások áttekintése
Liu, X., et al. 2012. Cell. 150, 1055.
Shan, J., et al. 2010. J. Clin. Invest. 120, 4375.
Bellinger, A. M., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 2198.
Lehnart, S.E., et al. 2008. J. Clin. Invest. 118, 2230.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision14-June-2013 JSW
Synonyms7-methoxy-4-methyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine, Ryanodine Receptor Stabilizer, Rycal S107
DescriptionA cell-permeable, orally active benzothiazepine derivative 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, PKA-mediated hyperphosphorylation, or mutation (complete blockage of 1 mM tetracaine-induced leakage in murine RyR2 S2808D+/+ myocytes at 1 µM). Oral administration in mice (75 mg/kg/day via drinking water) is shown to prevent stress-induced cognitive dysfunction by stabilizing RyR2-calstabin-2 (FKBP12.6) interaction in brain of stressed animals. Likewise, s.c. administration (2.5 µg/0.25 µL/h/animal; by s.c. via neck dorsal surface osmotic pump implant) is reported to maintain mice exercise capacity by stabilizing RyR1-calstabin-1 (FKBP12) interaction in skeletal muscle following intensive exercise regimes. Also demonstrated to exhibit in vivo efficacy in restoring normal cardiac function in mice with R2474S (5 mg/kg/h; by s.c. via osmotic pump) or S2808D (20 mg/kg/day; by s.c. via osmotic pump) RyR2 mutation.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number927871-76-9
Chemical formulaC₁₁H₁₅NOS
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesLiu, X., et al. 2012. Cell. 150, 1055.
Shan, J., et al. 2010. J. Clin. Invest. 120, 4375.
Bellinger, A. M., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 2198.
Lehnart, S.E., et al. 2008. J. Clin. Invest. 118, 2230.