| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C25H33N3O3S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
CMF019 is an orally active, potent, small-molecule agonist of the apelin receptor (APJ) with G-protein bias, binding APJ with pKi values of 8.58, 8.49, and 8.71 for human, rat, and mouse receptors, respectively. It mimics the beneficial cardiovascular actions of apelin in rodents[1]. APJ is a G-protein-coupled receptor (GPCR) activated by the endogenous peptide apelin, and CMF019 has been studied in relation to chronic diseases such as pulmonary arterial hypertension[1][2][3][4]. It is supplied as a white to light yellow solid (C25H33N3O3S, MW 455.61) at 99.89% purity.
Physical & Chemical Properties
| CAS Number | 1586787-08-7 |
|---|---|
| Molecular Formula | C25H33N3O3S |
| Molecular Weight | 455.61 g/mol |
| Purity | 99.89% |
| Appearance | Solid |
| Color | White to light yellow |
| SMILES | CC(C)C[C@H](NC(C1=CC=C2C(N=C(CC3=CC=CS3)N2C(CC)CC)=C1)=O)CC(O)=O |
| Signaling Pathway | GPCR/G Protein |
| Solubility | In Vitro: DMSO: 50 mg/mL (109.74 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
pKi: 8.58 (human Apelin receptor); 8.49 (rat Apelin receptor); 8.71 (mouse Apelin receptor)[1].
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[3]. Ma K F O, et al. CMF-019 elevates neuronal insulin sensitivity: an implication of therapeutic potential of Alzheimer’s disease[C]//26th Medical Research Conference. Hong Kong Academy of Medicine Press. The Journal's web site is located at http://www. hkmj. org/, 2021.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 50 mg/mL (109.74 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (5.49 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 2.5 mg/mL (5.49 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (5.49 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
CMF019 (1-10 μM, 18 h) protects human pulmonary arterial endothelial cells (PAEC) from apoptosis induced by TNFα and CHX[4].
Apoptosis Analysis[4]
| Cell Line | PAEC cells |
|---|---|
| Concentration | 1-10 μM |
| Incubation Time | 18 h |
| Result | Significantly increased the percentage of annexin+ /PI-cells. |
In Vivo
In rats, three successive i.v. doses of CMF019 (50-5000 nmol, 0.5 mL) reduce peripheral artery pressure[4].
| Animal Model | male Sprague-Dawley rats[2] |
|---|---|
| Dosage | 50-5000 nmol, 0.5 mL |
| Administration | i.v., three successive doses |
| Result | Revealed reproducible peripheral reduction in femoral artery pressure. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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