220005
CGP-37157
A cell-permeable benzothiazepine derivative of clonazepam that acts as a specific and potent inhibitor of the mitochondrial Na+/Ca2+ exchanger (IC50 = 360 nM).
别名:
CGP-37157, 7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one
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关于此项目
经验公式（希尔记法）:
C15H11Cl2NOS
化学文摘社编号:
分子量:
324.22
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
S1C(c3c(ccc(c3)Cl)NC(=O)C1)c2c(cccc2)Cl
InChI
1S/C15H11Cl2NOS/c16-9-5-6-13-11(7-9)15(20-8-14(19)18-13)10-3-1-2-4-12(10)17/h1-7,15H,8H2,(H,18,19)
InChI key
KQEPIRKXSUIUTH-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 5 mg/mL
shipped in
ambient
Quality Level
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General description
A cell-permeable benzothiazepine derivative of clonazepam that acts as a specific and potent inhibitor of the mitochondrial Na+/Ca2+ exchanger (IC50 = 360 nM). Enhances the export of Ca2+ from isolated mitochondria. Also reported to directly inhibit voltage-gated Ca2+ channels.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Mitochondrial Na+/Ca2+ exchanger
Mitochondrial Na+/Ca2+ exchanger
Product does not compete with ATP.
Reversible: no
Target IC50: 360 nM against mitochondrial Na+/Ca2+ exchanger
Packaging
Packaged under inert gas
Preparation Note
Dilute in Ca2+-free buffer just prior to use.
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Jornot, L., et al. 1999. J. Cell Sci.112, 1013.
Babcock, D.F., et al. 1997. J. Cell Biol.136, 833.
Baron. K.T., and Thayer, S.A. 1997. Eur. J. Pharmacol.340, 295.
Griffiths, E.J., et al. 1997. Cell Calcium21, 321.
White, R.J., and Reynolds, I.J. 1996, J. Neurosci.16, 5688.
Cox, D.A., et al. 1993. J. Cardivasc. Pharmacol.21, 595.
Cox, D.A., and Matlib, M.A. 1993. J. Biol. Chem.268, 938.
Babcock, D.F., et al. 1997. J. Cell Biol.136, 833.
Baron. K.T., and Thayer, S.A. 1997. Eur. J. Pharmacol.340, 295.
Griffiths, E.J., et al. 1997. Cell Calcium21, 321.
White, R.J., and Reynolds, I.J. 1996, J. Neurosci.16, 5688.
Cox, D.A., et al. 1993. J. Cardivasc. Pharmacol.21, 595.
Cox, D.A., and Matlib, M.A. 1993. J. Biol. Chem.268, 938.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
Beatriz F Côrte-Real et al.
Cell metabolism, 35(2), 299-315 (2023-02-09)
FOXP3+ regulatory T cells (Tregs) are central for peripheral tolerance, and their deregulation is associated with autoimmunity. Dysfunctional autoimmune Tregs display pro-inflammatory features and altered mitochondrial metabolism, but contributing factors remain elusive. High salt (HS) has been identified to alter immune
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