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CMF019

Name: CMF019
Brand: TargetMol
SKU: T10843
Price: 105 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T10843 Copy Product Info

Purity: 99.5%

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CMF019 (CMF-019) is a potent, G-protein-biased small-molecule agonist of the Apelin receptor (APJ/APLNR). CMF019 exhibits pKi values of 8.58, 8.49, and 8.71 for binding to APJ in humans, rats, and mice, respectively. CMF-019 exhibits cardioprotective effects in rodents. CMF019 can be utilized in mechanism and drug development for heart failure and pulmonary arterial hypertension.

Cas No. 1586787-08-7

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Pack Size	Price	USA Stock	Global Stock
1 mg	$105	In Stock	In Stock
5 mg	$246	In Stock	In Stock
10 mg	$416	In Stock	In Stock
25 mg	$677	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$245	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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Custom-made molecule. TargetMol’s expert synthesis team delivers cost-effective solutions. Contact us for inquiries. Committed to serving you.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.5%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

CMF019 AI Summary

CMF019 exhibits agonist activity at the recombinant human Giaq-coupled APJ receptor, resulting in an increase in intracellular calcium flux, with an EC50 value of 47.0 nM..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	CMF019 (CMF-019) is a potent, G-protein-biased small-molecule agonist of the Apelin receptor (APJ/APLNR). CMF019 exhibits pKi values of 8.58, 8.49, and 8.71 for binding to APJ in humans, rats, and mice, respectively. CMF-019 exhibits cardioprotective effects in rodents. CMF019 can be utilized in mechanism and drug development for heart failure and pulmonary arterial hypertension.
Targets & IC50	Apelin receptor (human):8.58 (pKi), Apelin receptor (mouse):8.71 (pKi), Apelin receptor (rat):8.49 (pKi)
In vitro	Methods: Human pulmonary artery endothelial cells were treated with TNFα (1.5 ng/mL) + actinomycin D (20 μg/mL) for 5 hours to induce apoptosis. Prior to apoptosis induction, cells were pretreated with CMF019 (1 μM and 10 μM) or positive control rhVEGF (10 ng/mL) for 18 hours. Apoptosis was detected by Annexin V/PI staining followed by flow cytometry. Results: CMF019 (1 μM) significantly reduced apoptosis to 5.66 ± 0.97%, approximately half the effect of rhVEGF (11.59 ± 1.85%). [1] Methods: Human, rat, and mouse cardiac tissue homogenates, as well as CHO-K1 cells expressing human apelin receptors, were used. [¹²⁵I]-apelin-13 (0.1 nM) served as the tracer for competitive binding with CMF019 at various concentrations (2 pM–10 μM). Results: CMF019 exhibited high affinity for apelin receptors in human, rat, and mouse tissues (pKi values: 8.58 ± 0.04, 8.49 ± 0.04, 8.71 ± 0.06, respectively).[2]
In vivo	Methods: Male SD rats (271 ± 3 g) underwent left ventricular and femoral artery catheterization. Increasing doses of CMF019 (50, 500, 5000 nmol), [Pyr¹]apelin-13 (10, 50, 150 nmol), or solvent control were administered via intravenous bolus injection. Each dose was administered at least 10 minutes apart, with hemodynamics allowed to return to baseline before the next dose. Results: At the 500 nmol dose, CMF019 significantly increased myocardial contractility (+251 ± 89 mmHg/s); at both 50 and 500 nmol doses, it significantly increased stroke volume and cardiac output. [1]

Chemical Properties

Molecular Weight	455.61
Formula	C₂₅H₃₃N₃O₃S
Cas No.	1586787-08-7
Smiles	CCC(CC)n1c(Cc2cccs2)nc2cc(ccc12)C(=O)N[C@@H](CC(C)C)CC(O)=O
Relative Density.	1.22 g/cm3 (Predicted)

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: 255 mg/mL (559.69 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.97 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	2.1949 mL	10.9743 mL	21.9486 mL	109.7430 mL
5 mM	0.4390 mL	2.1949 mL	4.3897 mL	21.9486 mL
10 mM	0.2195 mL	1.0974 mL	2.1949 mL	10.9743 mL
20 mM	0.1097 mL	0.5487 mL	1.0974 mL	5.4871 mL
50 mM	0.0439 mL	0.2195 mL	0.4390 mL	2.1949 mL
100 mM	0.0219 mL	0.1097 mL	0.2195 mL	1.0974 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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