2. GPCR/G Protein
  3. Apelin Receptor (APJ)
  4. APJ antagonist-1

APJ antagonist-1 is an apelin receptor (APJ) antagonist. APJ antagonist-1 shows strong β-arrestin inhibition with an IC50 of 3.1 μM. APJ antagonist-1 selectively inhibits APJ-overexpressing cancer cells and suppresses apelin-induced endothelial cell migration. APJ antagonist-1exhibits high metabolic stability. APJ antagonist-1 can used for the studies of ovarian cancer and tumor angiogenesis.

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APJ antagonist-1

APJ antagonist-1 Chemical Structure

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APJ antagonist-1 Related Antibodies

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Description

APJ antagonist-1 is an apelin receptor (APJ) antagonist. APJ antagonist-1 shows strong β-arrestin inhibition with an IC50 of 3.1 μM. APJ antagonist-1 selectively inhibits APJ-overexpressing cancer cells and suppresses apelin-induced endothelial cell migration. APJ antagonist-1exhibits high metabolic stability. APJ antagonist-1 can used for the studies of ovarian cancer and tumor angiogenesis[1].

In Vitro

APJ antagonist-1 (Compound 21) (1 h) exhibits significantly enhanced metabolic stability than ML221 (HY-103254) (100 % remaining in plasma after 1 h; liver microsomal t1/2 = 5 min)[1].
APJ antagonist-1 (12.5-100 μM, 3 days) shows a greater reduction in the viability of OVCAR8 cells and HT-29 cells[1].
APJ antagonist-1 (30 μM, 8 h) significantly inhibits apelin-induced migration in OVCAR3 cells and HUVECs[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

APJ antagonist-1 Related Antibodies

Cell Migration Assay [1]

Cell 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.
Molecular Weight

433.46

Formula

C18H15N3O6S2
SMILES

O=S(C1=CC=C([N+]([O-])=O)C=C1)(OC2=CC(CSC3=NC=CC=N3)=CC=C2OC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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APJ antagonist-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

APJ antagonist-1APJ antagonist1APJ antagonist 1Apelin Receptor (APJ)APJ antagonistApelin receptor (APJ)ML221 analogsPlasma and liver microsomal stabilityStructure-activity relationship (SAR)Sulfonate linkageβ-arrestin inhibitionInhibitorinhibitorinhibit

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