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).
Synonym(s):
CGP-37157, 7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one
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About This Item
Empirical Formula (Hill Notation):
C15H11Cl2NOS
CAS Number:
Molecular Weight:
324.22
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
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
storage temp.
2-8°C
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
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)
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Storage Class
11 - Combustible Solids
wgk
WGK 3
Certificates of Analysis (COA)
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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