Aficamten
Based on 3 publication(s) in Google Scholar
Aficamten (CK-274) is a potent cardiac myosin inhibitor with an IC50 of 1.4 μM. Aficamten can be used for the research of hypertrophic cardiomyopathy (HCM).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.86%
- CAS. Nr.: 2364554-48-1
- Formel: C18H19N5O2
- Molecular Weight:337.38
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) Aficamten
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Biologische Aktivität
Aficamten exhibits moderate oral bioavailability (mouse 98%, rat 55%, rat 58%,rat 79%, dog 45%, monkey 41%) following oral administration (mouse 1 mg/kg, rat 2 mg/kg, rat 3 mg/kg, rat 8 mg/kg, dog 1 mg/kg and monkey 1 mg/kg)[1].
Aficamten exhibits terminal elimination half-lives (mouse 4.5 h, rat 3.0 h, dog 33.8 h and, monkey 8.1 h) following intravenous administration (mouse 0.5 mg/kg, rat 1 mg/kg, dog 1 mg/kg and monkey 1.0 mg/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2364554-48-1
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Appearance Solid
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Molecular Weight 337.38
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Formel C18H19N5O2
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Color White to light brown
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SMILES
O=C(C1=CN(C)N=C1)N[C@H]2C3=CC=C(C4=NOC(CC)=N4)C=C3CC2
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Synonyms
CK-274; CK-3773274
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Cardiovasc Drugs Ther
Novel Selective Cardiac Myosin-Targeted Inhibitors Alleviate Myocardial Ischaemia-Reperfusion Injury. [Abstract]2025 Jan 4. PMID: 39754660
Aficamten purchased from MedChemExpress. Usage Cited in: Cardiovasc Drugs Ther. 2025 Jan 4. [Abstract]
Aficamten (CK-274) dose-response to the percentage of cells that contracted at different time points after CCCP treatment.
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bioRxiv
Myosin modulator Aficamten inhibits force in cardiac muscle by altering myosin's biochemical activity without changing thick filament structure. [Abstract]2025 May 18:2025.05.14.654110. PMID: 40463178
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (370.50 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (6.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 2.9640 mL | 14.8201 mL | 29.6402 mL | 74.1004 mL |
| 5 mM | 0.5928 mL | 2.9640 mL | 5.9280 mL | 14.8201 mL | |
| 10 mM | 0.2964 mL | 1.4820 mL | 2.9640 mL | 7.4100 mL | |
| 15 mM | 0.1976 mL | 0.9880 mL | 1.9760 mL | 4.9400 mL | |
| 20 mM | 0.1482 mL | 0.7410 mL | 1.4820 mL | 3.7050 mL | |
| 25 mM | 0.1186 mL | 0.5928 mL | 1.1856 mL | 2.9640 mL | |
| 30 mM | 0.0988 mL | 0.4940 mL | 0.9880 mL | 2.4700 mL | |
| 40 mM | 0.0741 mL | 0.3705 mL | 0.7410 mL | 1.8525 mL | |
| 50 mM | 0.0593 mL | 0.2964 mL | 0.5928 mL | 1.4820 mL | |
| 60 mM | 0.0494 mL | 0.2470 mL | 0.4940 mL | 1.2350 mL | |
| 80 mM | 0.0371 mL | 0.1853 mL | 0.3705 mL | 0.9263 mL | |
| 100 mM | 0.0296 mL | 0.1482 mL | 0.2964 mL | 0.7410 mL |
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