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Cariporide

Name: Cariporide
Brand: TargetMol
SKU: T2238
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2238Cas No. 159138-80-4

Alias HOE-642

Cariporide (HOE-642) (HOE-642), an effective NHE1 inhibitor, has inhibitory effects on the degranulation of human platelets, the formation of platelet-leukocyte-aggregates, and the activation of the GPIIb/IIIa receptor (PAC-1).

Cariporide

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Purity: 99.88%

Catalog No. T2238Alias HOE-642Cas No. 159138-80-4

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$39	In Stock	In Stock
10 mg	$55	In Stock	In Stock
25 mg	$113	In Stock	In Stock
50 mg	$222	In Stock	In Stock
100 mg	$346	In Stock	In Stock
500 mg	$819	-	In Stock
1 mL x 10 mM (in DMSO)	$43	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.88%

Color:White

Resource Download

COA LCMS HPLC HNMR

Product Introduction

Cariporide AI Summary

Cariporide exhibits diverse bioactivities, primarily targeting the sodium/hydrogen exchanger (NHE) family, with potent inhibition of NHE1 (IC50 of 30.0 nM) and moderate inhibition of NHE2 (IC50 of 4300.0 nM). It shows weak activity against NHE3 and NHE5 (IC50 ≥ 1000.0 nM and >30000.0 nM, respectively). It effectively inhibits NHE1-mediated intracellular pH recovery in various cell types, including rat and human platelets, and acidified rabbit erythrocytes. The compound also demonstrates significant cardioprotective effects, reducing myocardial infarct size and improving heart function in ischemia-reperfusion injury models in rats and guinea pigs. Additionally, it shows efficacy in mitigating serum creatine kinase levels and left ventricular end diastolic pressure during ischemic conditions. Pharmacokinetically, Cariporide has an oral bioavailability of 37.0% in rats, a volume of distribution at steady state of 1.3 L/kg, and a mean residence time of 0.4 hours post-intravenous administration. It exhibits a high clearance rate (82% relative to hepatic blood flow). Further, Cariporide shows modest inhibitory activity against SARS-CoV-2, including its 3CL-Pro protease, with inhibition percentages around 13-14% at 20 µM concentration. Lastly, it demonstrates potential inhibitory effects on human HDAC6, shown by inhibition percentages in enzymatic assays with peptide substrates. Overall, Cariporide holds promise for cardiovascular and antiviral therapeutic applications..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Cariporide (HOE-642) (HOE-642), an effective NHE1 inhibitor, has inhibitory effects on the degranulation of human platelets, the formation of platelet-leukocyte-aggregates, and the activation of the GPIIb/IIIa receptor (PAC-1).
Targets&IC50	NHE1:30 nM
Synonyms	HOE-642

Chemical Properties

Molecular Weight	283.35
Formula	C₁₂H₁₇N₃O₃S
Cas No.	159138-80-4
Smiles	CC(C)c1ccc(cc1S(C)(=O)=O)C(=O)N=C(N)N
Relative Density.	1.34g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (882.3 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.06 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.5292 mL	17.6460 mL	35.2920 mL	176.4602 mL
5 mM	0.7058 mL	3.5292 mL	7.0584 mL	35.2920 mL
10 mM	0.3529 mL	1.7646 mL	3.5292 mL	17.6460 mL
20 mM	0.1765 mL	0.8823 mL	1.7646 mL	8.8230 mL
50 mM	0.0706 mL	0.3529 mL	0.7058 mL	3.5292 mL
100 mM	0.0353 mL	0.1765 mL	0.3529 mL	1.7646 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc