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APJ antagonist-1
Catalog No. T213030 Copy Product Info
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APJ antagonist-1 is an apelin receptor (APJ) antagonist with potent β-arrestin inhibitory activity, exhibiting an IC50 of 3.1 μM. It selectively inhibits cancer cells overexpressing APJ and suppresses apelin-induced endothelial cell migration. The compound demonstrates high metabolic stability and is applicable in research on ovarian cancer and tumor angiogenesis.
APJ antagonist-1
Copy Product Info🥰Excellent
Catalog No. T213030
APJ antagonist-1 is an apelin receptor (APJ) antagonist with potent β-arrestin inhibitory activity, exhibiting an IC50 of 3.1 μM. It selectively inhibits cancer cells overexpressing APJ and suppresses apelin-induced endothelial cell migration. The compound demonstrates high metabolic stability and is applicable in research on ovarian cancer and tumor angiogenesis.
APJ antagonist-1
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | APJ antagonist-1 is an apelin receptor (APJ) antagonist with potent β-arrestin inhibitory activity, exhibiting an IC50 of 3.1 μM. It selectively inhibits cancer cells overexpressing APJ and suppresses apelin-induced endothelial cell migration. The compound demonstrates high metabolic stability and is applicable in research on ovarian cancer and tumor angiogenesis. |
| In vitro | APJ antagonist-1 (Compound 21) demonstrates significantly greater metabolic stability compared to ML221, with 100% remaining in plasma after 1 hour and a liver microsomal half-life of 5 minutes. At concentrations of 12.5-100 μM over three days, it notably reduces the viability of OVCAR8 and HT-29 cells. At 30 μM for 8 hours, APJ antagonist-1 significantly inhibits Apelin-induced migration in OVCAR3 cells and HUVECs, showing results that are comparable to or exceeding those of ML211.Cell Migration AssayCell Line: OVCAR3 cells and HUVECs Concentration: 30 μM Incubation Time: 8 h Result: Significantly inhibited apelin-induced migration and the effect was comparable to or even better than ML211. |
| 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, and a total of 10 animals are to be administered, using a formulation of 
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 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 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 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.
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