CMF019
Based on 1 Customer Validation
CMF019 is an orally active, potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents. Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. CMF019 is promising for research of chronic diseases, such as, pulmonary arterial hypertension.
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- Purity: 99.89%
- CAS No.: 1586787-08-7
- 화학식: C25H33N3O3S
- 분자량:455.61
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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GPCR/G Protein Compound Library
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Biological Activity
pKi: 8.58 (human Apelin receptor) ; 8.49 (rat Apelin receptor); 8.71 (mouse Apelin receptor)[1].
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
47 nM
Compound: 7; CMF-019
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Agonist activity at recombinant human Giaq-coupled APJ receptor stably expressed in HEK293 cells assessed as increase in intracellular calcium flux incubated for 10 mins and measured at 2 secs interval for 60 times by fluo-4 dye based fluorescence assay
Agonist activity at recombinant human Giaq-coupled APJ receptor stably expressed in HEK293 cells assessed as increase in intracellular calcium flux incubated for 10 mins and measured at 2 secs interval for 60 times by fluo-4 dye based fluorescence assay
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[PMID: 31948845] |
CMF019 (1-10 μM, 18 h) rescues human pulmonary arterial endothelial cells (PAEC) apoptosis induced by TNFα and CHX [4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PAEC cells
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Concentration:1-10 μM
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Incubation Time:18 h
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Result:Significantly increased the percentage of annexin+ /PI-cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:male Sprague-Dawley rats[2]
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Dosage:50-5000 nmol, 0.5 mL
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Administration:i.v., three successive doses
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Result:Revealed reproducible peripheral reduction in femoral artery pressure.
Chemical Information
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CAS No. 1586787-08-7
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Appearance Solid
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분자량 455.61
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화학식 C25H33N3O3S
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Color White to light yellow
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SMILES
CC(C)C[C@H](NC(C1=CC=C2C(N=C(CC3=CC=CS3)N2C(CC)CC)=C1)=O)CC(O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (109.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.49 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Trifonov L, et al. An Expedient Synthesis of CMF-019: (S)-5-Methyl-3-{1-(pentan-3-yl)-2- (thiophen-2-ylmethyl)-1H-benzo[d]imidazole-5-carboxamido}hexanoic Acid, a Potent Apelin Receptor (APJ) Agonist. Med Chem. 2018;14(7):688-694. [Content Brief]
[2]. Read C, et al. Cardiac action of the first G protein biased small molecule apelin agonist. Biochem Pharmacol. 2016 Sep 15;116:63-72. [Content Brief]
[4]. Read C, et al. The G Protein Biased Small Molecule Apelin Agonist CMF-019 is Disease Modifying in Endothelial Cell Apoptosis In Vitro and Induces Vasodilatation Without Desensitisation In Vivo. Front Pharmacol. 2021 Jan 21;11:588669. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1949 mL | 10.9743 mL | 21.9486 mL | 54.8715 mL |
| 5 mM | 0.4390 mL | 2.1949 mL | 4.3897 mL | 10.9743 mL | |
| 10 mM | 0.2195 mL | 1.0974 mL | 2.1949 mL | 5.4871 mL | |
| 15 mM | 0.1463 mL | 0.7316 mL | 1.4632 mL | 3.6581 mL | |
| 20 mM | 0.1097 mL | 0.5487 mL | 1.0974 mL | 2.7436 mL | |
| 25 mM | 0.0878 mL | 0.4390 mL | 0.8779 mL | 2.1949 mL | |
| 30 mM | 0.0732 mL | 0.3658 mL | 0.7316 mL | 1.8290 mL | |
| 40 mM | 0.0549 mL | 0.2744 mL | 0.5487 mL | 1.3718 mL | |
| 50 mM | 0.0439 mL | 0.2195 mL | 0.4390 mL | 1.0974 mL | |
| 60 mM | 0.0366 mL | 0.1829 mL | 0.3658 mL | 0.9145 mL | |
| 80 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.6859 mL | |
| 100 mM | 0.0219 mL | 0.1097 mL | 0.2195 mL | 0.5487 mL |
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