| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
CMF-019 targets the Apelin receptor (APJ), a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. It acts as a potent agonist with G protein bias. The compound binds to APJ with high affinity, as indicated by pKi values of 8.58 (human), 8.49 (rat), and 8.71 (mouse). By activating APJ, CMF-019 modulates cardiovascular functions including cardiac contractility, angiogenesis, and fluid homeostasis.
|
|---|---|
| ln Vitro |
In vitro, CMF-019 acts as a potent APJ agonist with G protein bias. It binds to APJ with pKi values of 8.58 for human, 8.49 for rat, and 8.71 for mouse. The compound's activity is typically assessed in cell-based assays measuring APJ-mediated signaling, such as cAMP inhibition or β-arrestin recruitment. Its G protein bias makes it a valuable tool for studying biased agonism at the APJ receptor.
|
| ln Vivo |
In vivo, CMF-019 increases cardiac contractility and demonstrates beneficial cardiovascular effects in rodents. As a potent APJ agonist, it mimics the cardiovascular actions of the endogenous peptide apelin. The compound has shown significant potential in modulating cardiovascular functions and is being studied for its therapeutic applications in cardiovascular disease.
|
| Enzyme Assay |
In cell-free receptor binding assays, CMF-019's activity is evaluated by measuring its affinity for the APJ receptor. Membrane preparations from cells expressing human, rat, or mouse APJ are incubated with a radiolabeled ligand and varying concentrations of CMF-019. The displacement of the radioligand is measured, and the pKi values (8.58, 8.49, 8.71) are calculated from the competition curves.
|
| Cell Assay |
In vitro cell-based experiments with CMF-019 typically involve cell lines expressing the APJ receptor, such as CHO or HEK293 cells. Cells are treated with the compound, and receptor activation is assessed by measuring downstream signaling events such as inhibition of forskolin-stimulated cAMP accumulation (Gαi pathway) or β-arrestin recruitment. The EC50 for receptor activation and the bias factor are determined from concentration-response curves.
|
| Animal Protocol |
In vivo animal experiments with CMF-019 have been conducted in rodents to evaluate its cardiovascular effects. In typical protocols, rodents are administered the compound, and cardiac contractility is measured using echocardiography or hemodynamic monitoring. The compound's effects on blood pressure, heart rate, and other cardiovascular parameters are assessed to characterize its in vivo pharmacological profile.
|
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for CMF-019. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) properties have not been extensively characterized. The compound is a small molecule that is typically administered in vivo to study its cardiovascular effects. Its bioavailability and half-life have not been well established in the available literature.
|
| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available for CMF-019. In preclinical studies, the compound has shown beneficial cardiovascular effects without reported significant toxicity. The compound is for research use only and is not intended for human therapeutic applications. Further toxicological studies would be needed to fully characterize its safety profile.
|
| References |
|
| Additional Infomation |
Apeline agonist; structure described in the first article.
CMF-019 has a CAS number of 1586787-08-7. It is a potent small molecule agonist at the Apelin receptor (APJ) with G protein bias. The compound is also known as CMF019. It binds to APJ with pKi values of 8.58, 8.49, and 8.71 for human, rat, and mouse, respectively. CMF-019 mimics the beneficial cardiovascular actions of apelin in rodents and is used for research purposes only. |
| Molecular Formula |
C25H33N3O3S
|
|---|---|
| Molecular Weight |
455.613
|
| Exact Mass |
455.224
|
| CAS # |
1586787-08-7
|
| Related CAS # |
1586787-08-7 (free);1993426-69-9 (potassium);
|
| PubChem CID |
73442763
|
| Appearance |
White to light yellow solid powder
|
| LogP |
5.4
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
32
|
| Complexity |
628
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C(C(N1C2=CC=C(C(NC(CC(C)C)CC(O)=O)=O)C=C2N=C1CC1SC=CC=1)CC)C
|
| InChi Key |
VCQKKZXFASLXAH-SFHVURJKSA-N
|
| InChi Code |
InChI=1S/C25H33N3O3S/c1-5-19(6-2)28-22-10-9-17(25(31)26-18(12-16(3)4)14-24(29)30)13-21(22)27-23(28)15-20-8-7-11-32-20/h7-11,13,16,18-19H,5-6,12,14-15H2,1-4H3,(H,26,31)(H,29,30)/t18-/m0/s1
|
| Chemical Name |
(3S)-5-methyl-3-[[1-pentan-3-yl-2-(thiophen-2-ylmethyl)benzimidazole-5-carbonyl]amino]hexanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~109.74 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.49 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1949 mL | 10.9743 mL | 21.9486 mL | |
| 5 mM | 0.4390 mL | 2.1949 mL | 4.3897 mL | |
| 10 mM | 0.2195 mL | 1.0974 mL | 2.1949 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
