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Chemical Structure| 159138-80-4 Chemical Structure| 159138-80-4

Structure of Cariporide
CAS No.: 159138-80-4

Chemical Structure| 159138-80-4

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Cariporide is a selective inhibitor of Na+/H+ exchanger isoform 1 (NHE1) with IC50 value of 0.05 μM with cardioprotective and antiarrhythmic effects.

Synonyms: HOE-642 Free Base; HOE 642

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Product Details of Cariporide

CAS No. :159138-80-4
Formula : C12H17N3O3S
M.W : 283.35
SMILES Code : CS(C1=CC(C(N=C(N)N)=O)=CC=C1C(C)C)(=O)=O
Synonyms :
HOE-642 Free Base; HOE 642
MDL No. :MFCD00864683
InChI Key :IWXNYAIICFKCTM-UHFFFAOYSA-N
Pubchem ID :151172

Safety of Cariporide

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HCT116 cells 1 μM and 10 μM EMPA did not inhibit the activity of the human NHE1 isoform. PMC8683707
Rat ventricular cardiomyocytes 10 μM Cariporide nearly completely inhibited NHE1 activity, while EMPA (1, 3, 10, or 30 μM) showed no NHE1 inhibition. PMC8683707
Human atrial cardiomyocytes 10 µM 45 min Cariporide significantly reduced Na influx in atrial cardiomyocytes of HFpEF patients. PMC11288740
Rat ventricular cardiomyocytes 10 μM Cariporide nearly completely inhibited NHE1 activity PMC8683707
Cardiomyocytes 10 µM 5 min Measure NHE1 activity, Cariporide inhibited NHE1 activity PMC11461573

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats, mice, and guinea pigs Langendorff-perfused hearts Perfusion 10 μM 15 minutes Cariporide significantly inhibited pH i recovery, while EMPA did not affect [Na+]i or pH i recovery. PMC8683707
Rats Langendorff-perfused hearts Perfusion 10 μM 15 minutes Cariporide significantly inhibited pH recovery and [Na+]i rise PMC8683707
Mice TAC/DOCA-induced heart failure model Oral 600 mg/kg Once daily for 10-12 days Cariporide mimicked EMPA's protection, preventing the development of heart failure PMC11461573
Mice Type 2 diabetic dbb mice Perfusion 1 μM Administered 10 minutes before inducing ischemia and remained throughout the experiment To investigate the role of NHE in cytoplasmic Ca2+ overload and ischemic myocardial damage during ischemia-reperfusion in type 2 diabetic mouse hearts. Results showed that Cariporide significantly reduced Ca2+ overload during ischemia-reperfusion and improved the recovery of ventricular function in diabetic hearts. PMC3366908

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.53mL

0.71mL

0.35mL

17.65mL

3.53mL

1.76mL

35.29mL

7.06mL

3.53mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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