2. Cytoskeleton
  3. Myosin
  4. Ulacamten

Ulacamten  (Synonyms: CK-4021586; CK-586)

Art. -Nr.: HY-159821 Reinheit: 99.22%
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Ulacamten (CK-4021586; CK-586) is an orally active cardiac myosin inhibitor and an inhibitor of the double-headed cardiac heavy meromyosin (HMM)ATPase (excluding single-headed myosin subfragment-1), with an EC50 of 2.9 μM. Ulacamten regulates cardiac myosin, reduces excessive myocardial contractility, and alleviates left ventricular outflow tract obstruction. Ulacamten increases the left ventricular short-axis systolic internal diameter, inhibits dobutamine-induced exacerbation of obstruction, and exerts only a mild reducing effect on left ventricular systolic function. Ulacamten also inhibits the fractional shortening of the short axis without altering calcium transients. Ulacamten shows good safety and tolerability in purpose-bred cats with naturally occurring obstructive hypertrophic cardiomyopathy.

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Ulacamten

Ulacamten Chemische Struktur

CAS. Nr. : 2830607-59-3

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Beschreibung

Ulacamten (CK-4021586; CK-586) is an orally active cardiac myosin inhibitor and an inhibitor of the double-headed cardiac heavy meromyosin (HMM)ATPase (excluding single-headed myosin subfragment-1), with an EC50 of 2.9 μM. Ulacamten regulates cardiac myosin, reduces excessive myocardial contractility, and alleviates left ventricular outflow tract obstruction. Ulacamten increases the left ventricular short-axis systolic internal diameter, inhibits dobutamine-induced exacerbation of obstruction, and exerts only a mild reducing effect on left ventricular systolic function. Ulacamten also inhibits the fractional shortening of the short axis without altering calcium transients. Ulacamten shows good safety and tolerability in purpose-bred cats with naturally occurring obstructive hypertrophic cardiomyopathy[1][2].

IC50 & Target

MLCK

 

In Vitro

Ulacamten (5 μM) inhibits fractional shortening by >80% in electrically-paced adult rat ventricular cardiomyocytes without altering the calcium transient[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ulacamten Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax
Cat[1] 3 mg/kg p.o. 0.28 μM 6.6 h
Cat[1] 10 mg/kg p.o. 1.21 μM 6.6 h
In Vivo

Ulacamten (2-15 mg/kg; p.o.; single dose) safely and dose-dependently ameliorates left ventricular outflow tract obstruction, reduces LV systolic function, and increases systolic LV chamber size in purpose-bred cats with naturally occurring obstructive hypertrophic cardiomyopathy, with the greatest effects observed at 6 hours post-dose[1].
Ulacamten reduces cardiac fractional shortening in normal Sprague-Dawley rats in a dose- and concentration-dependent manner[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Purpose-bred cats (1-10 years old; naturally occurring obstructive hypertrophic cardiomyopathy with subclinical LV hypertrophy without left atrial enlargement and left ventricular outflow tract obstruction)[1]
Dosage: 2 mg/kg; 5 mg/kg; 10 mg/kg; 15 mg/kg
Administration: p.o.; single dose
Result: Showed no significant differences in heart rate from vehicle at any timepoint across all doses.
Increased systolic LV internal diameter (LVIDs Sx) significantly from baseline at 6 hours post-dose at 15 mg/kg; produced significantly greater LVIDs Sx than vehicle in 2 mg/kg and 15 mg/kg groups at 6-hour dobutamine challenge.
Resolved dobutamine-induced increases in LV fractional shortening (LV FS%) seen in vehicle-treated cats at all tested doses; reduced LV FS% significantly from baseline at 6 hours post-dose at 15 mg/kg; produced significantly lower LV FS% than vehicle in 15 mg/kg group at 6 hours post-dose and 6-hour challenge, and in 10 mg/kg group at 24 hours post-dose.
Resolved dobutamine-induced increases in LV ejection fraction (LV EF%) seen in vehicle-treated cats at all tested doses; reduced LV EF% significantly from baseline at 6 hours post-dose at 15 mg/kg; produced significantly lower LV EF% than vehicle in 15 mg/kg group at 6 hours post-dose and 6-hour challenge, and in 10 mg/kg group at 24 hours post-dose.
Blunted dobutamine-induced increases in LVOT maximum pressure gradient (LVOTmaxPG) at 10 mg/kg and 15 mg/kg; reduced LVOTmaxPG significantly from baseline at 6 hours post-dose at 15 mg/kg; maintained median LVOTmaxPG values below the 14.5 mmHg obstruction threshold up to 48 hours post-dose in 5, 10, and 15 mg/kg groups.
Caused a dose-dependent decrease in the incidence of LVOTO (LVOTmaxPG ≥14.5 mmHg) at each timepoint; provided protection against dobutamine-induced obstruction in 10 and 15 mg/kg groups.
Molekulargewicht

405.44

Formel

C21H25F2N3O3
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N([C@@H]1CC[C@H](CC1)C)CC2=O)C3(CN(C3)C=O)N2CC4=CC(F)=C(C=C4)F
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 125 mg/mL (308.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4665 mL 12.3323 mL 24.6646 mL
5 mM 0.4933 mL 2.4665 mL 4.9329 mL
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.
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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation

Purity: 99.22%

SDS (251 KB)

COA (255 KB) HNMR (256 KB) LCMS (101 KB)

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 2.4665 mL 12.3323 mL 24.6646 mL 61.6614 mL
5 mM 0.4933 mL 2.4665 mL 4.9329 mL 12.3323 mL
10 mM 0.2466 mL 1.2332 mL 2.4665 mL 6.1661 mL
15 mM 0.1644 mL 0.8222 mL 1.6443 mL 4.1108 mL
20 mM 0.1233 mL 0.6166 mL 1.2332 mL 3.0831 mL
25 mM 0.0987 mL 0.4933 mL 0.9866 mL 2.4665 mL
30 mM 0.0822 mL 0.4111 mL 0.8222 mL 2.0554 mL
40 mM 0.0617 mL 0.3083 mL 0.6166 mL 1.5415 mL
50 mM 0.0493 mL 0.2466 mL 0.4933 mL 1.2332 mL
60 mM 0.0411 mL 0.2055 mL 0.4111 mL 1.0277 mL
80 mM 0.0308 mL 0.1542 mL 0.3083 mL 0.7708 mL
100 mM 0.0247 mL 0.1233 mL 0.2466 mL 0.6166 mL
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Ulacamten Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ulacamten2830607-59-3CK-4021586 CK-586CK4021586CK 4021586CK586CK 586CK-586Myosinmyocardial hypercontractilityobstructive hypertrophic cardiomyopathyleft ventricular outflow tract obstructionadult rat ventricular cardiomyocytescardiac heavy meromyosin (HMM) ATPasecardiac myosinhypertrophic cardiomyopathymyosin subfragment-1regulatory light chaincardiac myofibrillar ATPaseInhibitorinhibitorinhibit

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