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ML221 

Cat. No.: HY-103254 Purity: 99.25%
Handling Instructions

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.

For research use only. We do not sell to patients.

ML221 Chemical Structure

ML221 Chemical Structure

CAS No. : 877636-42-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
25 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 390 In-stock
Estimated Time of Arrival: December 31
100 mg USD 690 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

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.

IC50 & Target

IC50: 1.75 μM (APJ, cell-based)[1]

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)[1].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (80.45 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5950 mL 12.9752 mL 25.9504 mL
5 mM 0.5190 mL 2.5950 mL 5.1901 mL
10 mM 0.2595 mL 1.2975 mL 2.5950 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (5.19 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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[1].

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

References
Molecular Weight

385.35

Formula

C₁₇H₁₁N₃O₆S

CAS No.

877636-42-5

SMILES

O=C1C=C(CSC2=NC=CC=N2)OC=C1OC(C3=CC=C([N+]([O-])=O)C=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.25%

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Product Name:
ML221
Cat. No.:
HY-103254
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ML221

Cat. No.: HY-103254