Danicamtiv (MYK-491)

Catalog No.S9948 Batch:S994801

Technical Data

Formula

C₁₆H₂₀F₃N₅O₄S

Molecular Weight

435.42

CAS No.

1970972-74-7

Solubility (25°C)*

In vitro

DMSO

87 mg/mL (199.8 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.35mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 87 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.725mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 14.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Danicamtiv (MYK-491, SAR 440181) is a novel cardiac myosin activator that enhances cardiomyocyte contraction.

Targets

cardiac myosin ^[1]

In vitro

Danicamtiv metabolism pathways in vitro included CYP-mediated amide-cleavage, N-demethylation, as well as isoxazole- and piperidine-ring-opening.Danicamtiv show high permeability and no efflux in a Caco-2 cell line.<a class="sref" href="#s_ref">[2]</a>

In vivo

Danicamtiv selectively enhances cardiac actomyosin activity, the molecular force‐generating unit of the sarcomere, prolonging contraction while preserving actin-myosin detachment, allowing relaxation, and without impacting Ca2+ homeostasis.<a class="sref" href="#s_ref">[1]</a>

Protocol (from reference)

Cell Assay:^{<sup><a class="sref" href="#s_ref">[2]</a></sup>}	Cell lines Caco-2/TC7 cell lines, male human hepatocytes Concentrations 1 µM, 10 µM Incubation Time 0, 2, 4, 6, 8, and 24 h Method Incubations of plated human hepatocytes (1.4 million viable cells/mL, 0.2 mL, n = 2) with danicamtiv (1 µM) are performed in a cell culture incubator (37 °C, 5% CO<sub>2</sub>, 95% humidity). Incubations are quenched with 200 µL of ACN containing 50 nM CBZ internal standard at incubation times 0, 2, 4, 6, 8, and 24 h. Supernatants are analysed by LC-MS/MS for the analysis of danicamtiv from preclinical pharmacokinetic studies. Caco-2 cells are seeded on 96-well cell culture plates with PCF membrane filters and maintained for 21/25 days post-seeding with culture medium exchanged every 4th day. The bidirectional permeability (efflux) experiments are conducted on a TECAN automated liquid handling platform. Danicamtiv is examined at 1 and 10 μM, permeability controls are tested at 10 μM, and efflux controls are tested either at 2 μM or 1 μM in duplicate wells.
Animal Study:^{<sup><a class="sref" href="#s_ref">[1]</a></sup>}	Animal Models male beagle dogs Dosages 2–3 mg/kg Administration p.o. , i. pl.

Cell Assay:^{<a class="sref" href="#s_ref">[2]</a>}

Cell lines
Caco-2/TC7 cell lines, male human hepatocytes
Concentrations
1 µM, 10 µM
Incubation Time
0, 2, 4, 6, 8, and 24 h
Method
Incubations of plated human hepatocytes (1.4 million viable cells/mL, 0.2 mL, n = 2) with danicamtiv (1 µM) are performed in a cell culture incubator (37 °C, 5% CO2, 95% humidity). Incubations are quenched with 200 µL of ACN containing 50 nM CBZ internal standard at incubation times 0, 2, 4, 6, 8, and 24 h. Supernatants are analysed by LC-MS/MS for the analysis of danicamtiv from preclinical pharmacokinetic studies. Caco-2 cells are seeded on 96-well cell culture plates with PCF membrane filters and maintained for 21/25 days post-seeding with culture medium exchanged every 4th day. The bidirectional permeability (efflux) experiments are conducted on a TECAN automated liquid handling platform. Danicamtiv is examined at 1 and 10 μM, permeability controls are tested at 10 μM, and efflux controls are tested either at 2 μM or 1 μM in duplicate wells.

Animal Study:^{<a class="sref" href="#s_ref">[1]</a>}

Animal Models
male beagle dogs
Dosages
2–3 mg/kg
Administration
p.o. , i. pl.

References

Selleck's Danicamtiv (MYK-491) has been cited by 2 publications

Danicamtiv reduces myosin's working stroke but enhances contraction by activating the thin filament [ bioRxiv, 2024, 2024.10.09.617269]	PubMed: 39416013
Effect of the Novel Myotrope Danicamtiv on Cross-Bridge Behavior in Human Myocardium [ J Am Heart Assoc, 2023, 12(20):e030682]	PubMed: 37804193

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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