Mavacamten [1642288-47-8]
Référence HY-109037-5mg
Conditionnement : 5mg
Marque : MedChemExpress
Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
Mavacamten Chemical Structure
CAS No. : 1642288-47-8
This product is a controlled substance and not for sale in your territory.
Based on 8 publication(s) in Google Scholar
Other Forms of Mavacamten:
- Mavacamten-d6 Obtenir un devis
- Mavacamten-d1 Obtenir un devis
- Mavacamten-d5 Obtenir un devis
Description |
Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively. |
IC50 & Target |
IC50: 490 nM (bovine cardiac), 711 nM (human cardiac)[1]. |
||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
In Vitro |
Mavacamten is found to have an IC50 value of 490 nM in the bovine system, 711 nM in the human system, and 2140 nM in the rabbit system, indicating selectivity of >4-fold for cardiac myosin[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||
In Vivo |
Treatment with Mavacamten reduces FS from 52±3% to 38±7%. Treatment with Mavacamten reduces FS from 81±7% to 60±13%, corresponding to a relative reduction of 25%. Across all measurements there is a linear correlation between FS and Mavacamten plasma concentrations with each 100 ng/mL increase in Mavacamten concentration lowering FS by 4.9%[2]. Mavacamten reduces contractility by decreasing the adenosine triphosphatase activity of the cardiac myosin heavy chain. Chronic administration of Mavacamten suppresses the development of ventricular hypertrophy, cardiomyocyte disarray, and myocardial fibrosis and attenuates hypertrophic and profibrotic gene expression in mice harboring heterozygous human mutations in the myosin heavy chain[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||
Essai clinique |
|
||||||||||||
Masse moléculaire |
273.33 |
||||||||||||
Formule |
C15H19N3O2 |
||||||||||||
CAS No. |
1642288-47-8 |
||||||||||||
Appearance |
Solid |
||||||||||||
Color |
White to off-white |
||||||||||||
SMILES |
CC(N(C1=O)C(C=C(N[C@H](C2=CC=CC=C2)C)N1)=O)C |
||||||||||||
Livraison | Room temperature in continental US; may vary elsewhere. |
||||||||||||
Stockage |
|
||||||||||||
Solvant et solubilité |
In Vitro:
DMSO : 83.33 mg/mL (304.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
View the 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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
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).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
|
||||||||||||
Pureté et documentation |
Purity: 99.94% |
||||||||||||
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
---|
DMSO | 1 mM | 3.6586 mL | 18.2929 mL | 36.5858 mL | 91.4645 mL |
5 mM | 0.7317 mL | 3.6586 mL | 7.3172 mL | 18.2929 mL | |
10 mM | 0.3659 mL | 1.8293 mL | 3.6586 mL | 9.1465 mL | |
15 mM | 0.2439 mL | 1.2195 mL | 2.4391 mL | 6.0976 mL | |
20 mM | 0.1829 mL | 0.9146 mL | 1.8293 mL | 4.5732 mL | |
25 mM | 0.1463 mL | 0.7317 mL | 1.4634 mL | 3.6586 mL | |
30 mM | 0.1220 mL | 0.6098 mL | 1.2195 mL | 3.0488 mL | |
40 mM | 0.0915 mL | 0.4573 mL | 0.9146 mL | 2.2866 mL | |
50 mM | 0.0732 mL | 0.3659 mL | 0.7317 mL | 1.8293 mL | |
60 mM | 0.0610 mL | 0.3049 mL | 0.6098 mL | 1.5244 mL | |
80 mM | 0.0457 mL | 0.2287 mL | 0.4573 mL | 1.1433 mL | |
100 mM | 0.0366 mL | 0.1829 mL | 0.3659 mL | 0.9146 mL |
Mavacamten Related Classifications
- Cytoskeleton
- Myosin