Cariporide

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Cat.No. 5358 - Cariporide | C12H17N3O3S | CAS No. 159138-80-4
Description: Selective NHE1 inhibitor; cardioprotective and antitumor
Alternative Names: HOE 642
Chemical Name: N-(Aminoiminomethyl)-4-(1-methylethyl)-3-(methylsulfonyl)benzamide
Purity: ≥99% (HPLC)
Datasheet
Citations
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Literature

Biological Activity

Selective Na+/H+ exchanger isoform 1 (NHE1) inhibitor (IC50 values are 0.05, 3 and 1000 μM for NHE1, NHE3 and NHE2 respectively). Attenuates ischemia-induced cardiomyocyte apoptosis in vitro. Reduces cardiac arrhythmia in vivo. Also promotes apoptosis in cancer cells overexpressing NHE1. Orally active.

Technical Data

M. Wt 283.35
Formula C12H17N3O3S
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 159138-80-4
PubChem ID 151172
InChI Key IWXNYAIICFKCTM-UHFFFAOYSA-N
Smiles CC(C)C1=C(S(C)(=O)=O)C=C(C(NC(N)=N)=O)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 28.34 100

Preparing Stock Solutions

The following data is based on the product molecular weight 283.35. Batch specific molecular weights may vary from batch to batch due to solvent 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 3.53 mL 17.65 mL 35.29 mL
5 mM 0.71 mL 3.53 mL 7.06 mL
10 mM 0.35 mL 1.76 mL 3.53 mL
50 mM 0.07 mL 0.35 mL 0.71 mL

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References

References are publications that support the biological activity of the product.

Scholz et al (1995) Protective effects of HOE642, a selective sodium-hydrogen exchange subtype 1 inhibitor, on cardiac ischaemia and reperfusion. Cardiovasc.Res. 29 260 PMID: 7736504

Chakrabarti et al (1997) A rapid ischemia-induced apoptosis in isolated rat hearts and its attenuation by the sodium-hydrogen exchange inhibitor HOE 642 (cariporide). J.Mol.Cell.Cardiol. 29 3169 PMID: 9405190

Teshima et al (2003) Cariporide (HOE642), a selective Na+-H+ exchange inhibitor, inhibits the mitochondrial death pathway. Circulation 108 2275 PMID: 14568900

Harguindey et al (2013) Cariporide and other new and powerful NHE1 inhibitors as potentially selective anticancer drugs--an integral molecular/biochemical/metabolic/clinical approach after one hundred years of cancer research. J.Transl.Med. 11 282 PMID: 24195657


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Literature in this Area

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Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure