S107 binds RyR1 and enhances the binding affinity of calstabin-1. S107 inhibits Ca leak from the sarcoplasmic reticulum (SR). S107 increases FKBP12 binding to RyR1 in SR vesicles in the presence of reduced glutathione and the NO-donor NOC12, with no effect in the presence of oxidized glutathione. S107 can reverse the harmful effects of redox active species on SR Ca2+ release in skeletal muscle by binding to RyR1 low affinity sites.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 30 mg/mL|
Stabilization of the skeletal muscle ryanodine receptor ion channel-FKBP12 complex by the 1,4-benzothiazepine derivative S107.
Mei Y, et al. PLoS One. 2013;8(1):e54208. PMID: 23349825.
Leaky Ca2+ release channel/ryanodine receptor 2 causes seizures and sudden cardiac death in mice.
Lehnart SE, et al. J Clin Invest. 2008 Jun;118(6):2230-45. PMID: 18483626.
Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM.
|Recombinant Human GM-CSF (CHO-expressed)
Recombinant Human Granulocyte-Macrophage Colony Stimulating Factor (CHO-expressed) is a hematopoietic growth factor and immune modulator.
Glutathione oxidized is produced by the oxidation of glutathione.
NG25 is a potent dual TAK1 and MAP4K2 inhibitor with IC50s of 149 nM and 21.7 nM, respectively.
|IRAK-1-4 Inhibitor I
IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.3 μM and 0.2 μM, respectively.
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