ML221
Based on 10 publication(s) in Google Scholar
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.
- Purity: 98.45%
- CAS No.: 877636-42-5
- Formula: C17H11N3O6S
- Molecular Weight:385.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ML221
More- Cell Commun Signal. 2025 Oct 30;23(1):469. [Abstract]
- Eur J Pharmacol. 2021 Aug 5:904:174149. [Abstract]
- Int Immunopharmacol. 2026 Feb 1:170:116068. [Abstract]
- Exp Neurol. 2024 Aug:378:114802. [Abstract]
- Neuropharmacology. 2022 Nov 15:219:109235. [Abstract]
- Stem Cells Int. 2022 Mar 21;2022:3742678. [Abstract]
- Peptides. 2026 Mar:196:171472. [Abstract]
- SSRN. 2026 Jun 17.
- Oxid Med Cell Longev. 2021 Jan 25:2021:8836058. [Abstract]
- Research Square Preprint. 2020 Jul.
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Biological Activity
IC50: 1.75 μM (APJ, cell-based)[1]
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | IC50 |
1.75 μM
Compound: 6 , ML221
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Antagonist activity at APJ receptor expressed in CHOK1 cells assessed as inhibition of apelin13-induced beta-arrestin recruitment after 90 mins by luminescence assay
Antagonist activity at APJ receptor expressed in CHOK1 cells assessed as inhibition of apelin13-induced beta-arrestin recruitment after 90 mins by luminescence assay
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[PMID: 23010269] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 877636-42-5
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Appearance Solid
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Molecular Weight 385.35
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Formula C17H11N3O6S
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Color Off-white to yellow
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SMILES
O=C1C=C(CSC2=NC=CC=N2)OC=C1OC(C3=CC=C([N+]([O-])=O)C=C3)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Cell Commun Signal
Mechanistic insights into targeting APLN/APJ for ameliorating testosterone deficiency and reproductive disorders in diabetic mice. [Abstract]2025 Oct 30;23(1):469. PMID: 41168800
ML221 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Oct 30;23(1):469. [Abstract]
Mitochondrial ROS levels labeled with MitoSOX in Leydig cells treated with ML221 (40 μM).
ML221 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Oct 30;23(1):469. [Abstract]
Representative histograms of MitoSOX Red flow cytometry from Leydig cells treated with ML221 (40 μM) for 24 h.
ML221 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Oct 30;23(1):469. [Abstract]
Western blot analysis of StAR, TSPO, and NR2F2 protein expression in Leydig cells after ML221 (40 μM) treatment.
ML221 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Oct 30;23(1):469. [Abstract]
Expression levels of Hsd3b1, Hsd17b1, Star, and Tspo mRNAs in Leydig cells treated with ML221 (40 μM) and SLG.
ML221 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Oct 30;23(1):469. [Abstract]
ATP levels in Leydig cells treated with ML221 (40 μM) across four independent experiments.
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Eur J Pharmacol
2021 Aug 5:904:174149. PMID: 33961873 -
Int Immunopharmacol
Elabela APJ Axis attenuates type II diabetes osteoporosis by enhancing the coupling of H-type angiogenesis and osteogenesis. [Abstract]2026 Feb 1:170:116068. PMID: 41455365 -
Exp Neurol
Elabela ameliorates neuronal pyroptosis and mitochondrial fission via APJ/ZBP1 signaling in ischemic stroke. [Abstract]2024 Aug:378:114802. PMID: 38679280 -
Neuropharmacology
Neuropeptide apelin presented in the dopaminergic neurons modulates the neuronal excitability in the substantia nigra pars compacta. [Abstract]2022 Nov 15:219:109235. PMID: 36041497 -
Stem Cells Int
Apelin-13 Pretreatment Promotes the Cardioprotective Effect of Mesenchymal Stem Cells against Myocardial Infarction by Improving Their Survival. [Abstract]2022 Mar 21;2022:3742678. PMID: 35355588 -
Peptides
Apelin-36 attenuates diabetic glomerular endothelial hyperpermeability via the KLF2/Occludin pathway. [Abstract]2026 Mar:196:171472. PMID: 41690598 -
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Oxid Med Cell Longev
Apelin/APJ-Manipulated CaMKK/AMPK/GSK3 β Signaling Works as an Endogenous Counterinjury Mechanism in Promoting the Vitality of Random-Pattern Skin Flaps. [Abstract]2021 Jan 25:2021:8836058. PMID: 33574981 -
Solvent & Solubility
DMSO : ≥ 31 mg/mL (80.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5950 mL | 12.9752 mL | 25.9504 mL | 64.8761 mL |
| 5 mM | 0.5190 mL | 2.5950 mL | 5.1901 mL | 12.9752 mL | |
| 10 mM | 0.2595 mL | 1.2975 mL | 2.5950 mL | 6.4876 mL | |
| 15 mM | 0.1730 mL | 0.8650 mL | 1.7300 mL | 4.3251 mL | |
| 20 mM | 0.1298 mL | 0.6488 mL | 1.2975 mL | 3.2438 mL | |
| 25 mM | 0.1038 mL | 0.5190 mL | 1.0380 mL | 2.5950 mL | |
| 30 mM | 0.0865 mL | 0.4325 mL | 0.8650 mL | 2.1625 mL | |
| 40 mM | 0.0649 mL | 0.3244 mL | 0.6488 mL | 1.6219 mL | |
| 50 mM | 0.0519 mL | 0.2595 mL | 0.5190 mL | 1.2975 mL | |
| 60 mM | 0.0433 mL | 0.2163 mL | 0.4325 mL | 1.0813 mL | |
| 80 mM | 0.0324 mL | 0.1622 mL | 0.3244 mL | 0.8110 mL |
ML221 Related Classifications
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