Danicamtiv (MYK-491)

Synonyms: SAR 440181

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

Danicamtiv (MYK-491) Chemical Structure

Danicamtiv (MYK-491) Chemical Structure

CAS: 1970972-74-7

Selleck's Danicamtiv (MYK-491) has been cited by 1 publication

Purity & Quality Control

Batch: S994801 DMSO] 87 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.13%
99.13

Danicamtiv (MYK-491) Related Products

Choose Selective Cardiac Myosin Inhibitors

Biological Activity

Description

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

Targets
cardiac myosin [1]
In vitro
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.<sup><a class="sref" href="#s_ref">[2]</a></sup>

Cell Research 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.

In Vivo
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.<sup><a class="sref" href="#s_ref">[1]</a></sup>

Animal Research Animal Models male beagle dogs
Dosages 2–3 mg/kg
Administration p.o. , i. pl.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03447990 Completed
Heart Failure With Reduced Ejection Fraction|Dilated Cardiomyopathy
Bristol-Myers Squibb
February 6 2018 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 435.42 Formula

C16H20F3N5O4S

CAS No. 1970972-74-7 SDF --
Smiles C[N]1C=C(C(=N1)C(F)F)[S](=O)(=O)C(C)(F)C2CCN(CC2)C(=O)NC3=NOC=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 87 mg/mL ( (199.8 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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