APJ receptor agonist 1

Name: APJ receptor agonist 1
Brand: TargetMol
SKU: T39813
Rating: 4.5 (1 reviews)

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Catalog No. T39813Cas No. 2287153-38-0

APJ receptor agonist 1, a potent biphenyl acid derivative, acts as an agonist (EC50 of 0.093 nM and 0.12 nM for human and rat APJ receptors, respectively) for the APJ receptor (APJ-R). It exhibits significant in vitro potency towards apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 holds promise for heart failure research.

APJ receptor agonist 1

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Catalog No. T39813Cas No. 2287153-38-0

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
5 mg	$970	Inquiry	Inquiry

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Product Introduction

Bioactivity

Description	APJ receptor agonist 1, a potent biphenyl acid derivative, acts as an agonist (EC50 of 0.093 nM and 0.12 nM for human and rat APJ receptors, respectively) for the APJ receptor (APJ-R). It exhibits significant in vitro potency towards apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 holds promise for heart failure research.
In vitro	The S-atropisomer of APJ receptor agonist 1 (compound 15a) exhibits 200 times greater potency than its R-atropisomer counterpart.[1].
In vivo	APJ receptor agonist 1, administered via intravenous infusion at dosages of 10-100 μg/min/kg, resulted in a 10% enhancement of cardiac output (CO) with negligible effects on blood pressure, specifically less than a 5% transient reduction. This outcome was observed in isoflurane-anesthetized male Sprague Dawley rats. The administration involved infusing the compound into the jugular vein for 15 minutes, demonstrating a dose-dependent increase in cardiac output without significant alterations in mean arterial blood pressure or heart rate[1].

Chemical Properties

Molecular Weight	524.02
Formula	C₃₁H₂₆ClN₃O₃
Cas No.	2287153-38-0
Smiles	CCCC(NC(=O)c1ccc(c(c1)C(O)=O)-c1c(Cl)cccc1-c1nc2ccccc2[nH]1)c1ccccc1

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.

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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

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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