Delocamten
Based on 1 Customer Validation
Delocamten is an orally active, selective Cardiac Myosin inhibitor with an IC50 of approximately 1.11 μM. Delocamten directly modulates myosin complexes, inhibits excessive myocardial contraction, and improves diastolic function. Delocamten can be used in studies of hypertrophic cardiomyopathy (HCM), left ventricular hypertrophy, and diastolic dysfunction.
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- Pureté : 99.93%
- CAS No.: 2417411-02-8
- Formule: C19H21F2N3O3
- Masse moléculaire:377.39
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
Delocamten (Compound 3) (0.3 μM; 5 min) inhibits the fractional shortening rate of myocardial contraction in adult rat ventricular myocytes[1].
Delocamten (up to 50 μM; 15 min) inhibits the activity of myosin ATPase in bovine cardiac myofibrils/rabbit skeletal muscle myofibrils[1].
Delocamten (30 μM; 60 min) exhibits a safety profile with extremely low formation of reactive metabolites in human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Delocamten (2-10 mg/kg; p.o.; single administration; recorded 2 h post-dose) exerts dose-dependent activity in modulating cardiac systolic parameters in conscious SD rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Isoflurane (HY-A0134)-anesthetized SD rats[1]
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Dosage:2.0 mg/kg/hr
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Administration:i.v.; continuous administration; lasting 30-60 min
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Result:Dose-dependently attenuated cardiac contractile function.
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Animal Model:Conscious SD rats[1]
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Dosage:2 mg/kg , 5 mg/kg , 10 mg/kg
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Administration:p.o.; single administration; recorded 2 h post-dose
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Result:Dose-dependently attenuated cardiac contractile function.
Chemical Information
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CAS No. 2417411-02-8
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Appearance Solid
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Masse moléculaire 377.39
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Formule C19H21F2N3O3
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Color White to off-white
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SMILES
O=C1C2=C(NC(N1C3CCOCC3)=O)N[C@@H](C4=C(C=CC(C)=C4)F)[C@H](C2)F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (264.98 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)
In Vivo:
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: ≥ 5 mg/mL (13.25 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 2.6498 mL | 13.2489 mL | 26.4978 mL | 66.2445 mL |
| 5 mM | 0.5300 mL | 2.6498 mL | 5.2996 mL | 13.2489 mL | |
| 10 mM | 0.2650 mL | 1.3249 mL | 2.6498 mL | 6.6244 mL | |
| 15 mM | 0.1767 mL | 0.8833 mL | 1.7665 mL | 4.4163 mL | |
| 20 mM | 0.1325 mL | 0.6624 mL | 1.3249 mL | 3.3122 mL | |
| 25 mM | 0.1060 mL | 0.5300 mL | 1.0599 mL | 2.6498 mL | |
| 30 mM | 0.0883 mL | 0.4416 mL | 0.8833 mL | 2.2081 mL | |
| 40 mM | 0.0662 mL | 0.3312 mL | 0.6624 mL | 1.6561 mL | |
| 50 mM | 0.0530 mL | 0.2650 mL | 0.5300 mL | 1.3249 mL | |
| 60 mM | 0.0442 mL | 0.2208 mL | 0.4416 mL | 1.1041 mL | |
| 80 mM | 0.0331 mL | 0.1656 mL | 0.3312 mL | 0.8281 mL | |
| 100 mM | 0.0265 mL | 0.1325 mL | 0.2650 mL | 0.6624 mL |
Delocamten Related Classifications
HY-172424 Related Classifications
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Keywords
- Delocamten
- 2417411-02-8
- Myosin
- Heart failure with midrange ejection fraction
- Left ventricular hypertrophy
- Valvular aortic stenosis
- cardiac myosin
- Hypertrophic cardiomyopathy
- Heart failure with preserved ejection fraction
- Tetralogy of fallot
- Chagas disease
- Angina pectoris
- Restrictive cardiomyopathy
- Inhibitor
- inhibitor
- inhibit