ML221

SKU: orb1302896

Description

ML221 is a potent functional antagonist of the apelin/APJ system, inhibiting apelin-13-induced signaling with IC50 values of 0.70 μM (cAMP) and 1.75 μM (β-arrestin). This compound is a valuable research tool for investigating the APJ receptor's role in cardiovascular function and metabolic diseases in both cellular and animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 877636-42-5
• MW: 385.35
• Purity: 97.74% (May vary between batches)
• Formula: C₁₇H₁₁N₃O₆S
• SMILES: [O-][N+](=O)c1ccc(cc1)C(=O)Oc1coc(CSc2ncccn2)cc1=O
• Target: Apelin receptor,Arrestin
• Solubility: DMSO:6.25 mg/mL (16.22 mM)

Bioactivity

• Target IC50:
  APJ:1.75 μM
• In Vitro:
  ML221 is a potent apelin/APJ functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays. ML221 is >37-fold selective over the closely related angiotensin II type 1 (AT1) receptor (IC50, >79 μM) in cells. ML221 displays limited cross reactivity against a range of GPCRs except the κ-opioid and benzodiazepinone receptors (<50/<70%I at 10 μM)
• Cell Research:
  ML221 is dissolved in DMSO. Cells (angiotensin II receptor-like 1 (AGTRL-1) cell line) are seeded at 1000 cell/well (1536 plate) in 4 μL and grown overnight (16-18 h) at 37°C, 5% CO2, 100% humidity, then 60 nL of either DMSO control or 2 mM stock test compounds (ML221, etc.) in DMSO are transferred to each well, followed by 2 μL of 30 nM Apelin-13 to negative control and test compound wells, and 2 μL of assay media (F12 nutrient mix HAMs supplemented with 10% hi-FBS, 1× penicillin/streptomycin) to positive control wells. This yields a final concentration of test compound (ML221, etc.) of 20 μM and 1% final DMSO. Assay is incubated for 90 min at room temperature, and then developed with 3 μL of detection reagent for 60 min and luminescence read on a ViewLux. They are for reference only.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ML221, ML-221, ML 221, inhibit, Inhibitor, APJ, Apelin receptor, Apelinreceptor

Compound Identifiers

PubChem CID

7217941