Synonym
Cgp 37157; Cgp-37157; Cgp37157.
IUPAC/Chemical Name
4,1-Benzothiazepin-2(3H)-one, 7-chloro-5-(2-chlorophenyl)-1,5-dihydro-
InChi Key
KQEPIRKXSUIUTH-HNNXBMFYSA-N
InChi Code
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)/t15-/m0/s1
SMILES Code
c12[C@@H](SCC(=O)Nc1ccc(c2)Cl)c1c(Cl)cccc1
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
324.22
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Neumann JT, Diaz-Sylvester PL, Fleischer S, Copello JA. CGP-37157 inhibits the sarcoplasmic reticulum Ca²+ ATPase and activates ryanodine receptor channels in striated muscle. Mol Pharmacol. 2011 Jan;79(1):141-7. doi: 10.1124/mol.110.067165. Epub 2010 Oct 5. PubMed PMID: 20923851; PubMed Central PMCID: PMC3014283.
2: Luciani DS, Ao P, Hu X, Warnock GL, Johnson JD. Voltage-gated Ca(2+) influx and insulin secretion in human and mouse beta-cells are impaired by the mitochondrial Na(+)/Ca(2+) exchange inhibitor CGP-37157. Eur J Pharmacol. 2007 Dec 8;576(1-3):18-25. Epub 2007 Aug 3. PubMed PMID: 17719029.
3: Thu le T, Ahn JR, Woo SH. Inhibition of L-type Ca2+ channel by mitochondrial Na+-Ca2+ exchange inhibitor CGP-37157 in rat atrial myocytes. Eur J Pharmacol. 2006 Dec 15;552(1-3):15-9. Epub 2006 Sep 23. PubMed PMID: 17054940.
4: Czyz A, Kiedrowski L. Inhibition of plasmalemmal Na(+)/Ca(2+) exchange by mitochondrial Na(+)/Ca(2+) exchange inhibitor 7-chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one (CGP-37157) in cerebellar granule cells. Biochem Pharmacol. 2003 Dec 15;66(12):2409-11. PubMed PMID: 14637198.
5: Omelchenko A, Bouchard R, Le HD, Choptiany P, Visen N, Hnatowich M, Hryshko LV. Inhibition of canine (NCX1.1) and Drosophila (CALX1.1) Na(+)-Ca(2+) exchangers by 7-chloro-3,5-dihydro-5-phenyl-1H-4,1-benzothiazepine-2-one (CGP-37157). J Pharmacol Exp Ther. 2003 Sep;306(3):1050-7. Epub 2003 Jun 13. PubMed PMID: 12808003.
6: Scanlon JM, Brocard JB, Stout AK, Reynolds IJ. Pharmacological investigation of mitochondrial ca(2+) transport in central neurons: studies with CGP-37157, an inhibitor of the mitochondrial Na(+)-Ca(2+) exchanger. Cell Calcium. 2000 Nov-Dec;28(5-6):317-27. PubMed PMID: 11115371.
7: Cox DA, Conforti L, Sperelakis N, Matlib MA. Selectivity of inhibition of Na(+)-Ca2+ exchange of heart mitochondria by benzothiazepine CGP-37157. J Cardiovasc Pharmacol. 1993 Apr;21(4):595-9. PubMed PMID: 7681905.
