1. Cytoskeleton
  2. Myosin
  3. Aficamten

Aficamten (Synonyms: CK-274; CK-3773274)

Cat. No.: HY-139465
Handling Instructions

Aficamten (CK-274) is a potent cardiac myosin inhibitor with an IC50 of 1.4 μM. Aficamten can be used for the research of hypertrophic cardiomyopathy (HCM).

For research use only. We do not sell to patients.

Aficamten Chemical Structure

Aficamten Chemical Structure

CAS No. : 2364554-48-1

Size Price Stock Quantity
5 mg USD 380 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Aficamten (CK-274) is a potent cardiac myosin inhibitor with an IC50 of 1.4 μM. Aficamten can be used for the research of hypertrophic cardiomyopathy (HCM)[1].

In Vivo

Aficamten is a next-generation cardiac myosin inhibitor that provides a projected human half-life appropriate for once a day dosing, reaching steady state within two weeks, and demonstrates a wide therapeutic window in vivo with a clear PK/PD relationship[1]
Aficamten exhibits moderate oral bioavailability (mouse 98%, rat 55%, rat 58%,rat 79%, dog 45%, monkey 41%) following oral administration (mouse 1 mg/kg, rat 2 mg/kg, rat 3 mg/kg, rat 8 mg/kg, dog 1 mg/kg and monkey 1 mg/kg)[1].
Aficamten exhibits terminal elimination half-lives (mouse 4.5 h, rat 3.0 h, dog 33.8 h and, monkey 8.1 h) following intravenous administration (mouse 0.5 mg/kg, rat 1 mg/kg, dog 1 mg/kg and monkey 1.0 mg/kg)[1].

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

Molecular Weight

337.38

Formula

C₁₈H₁₉N₅O₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (370.50 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9640 mL 14.8201 mL 29.6402 mL
5 mM 0.5928 mL 2.9640 mL 5.9280 mL
10 mM 0.2964 mL 1.4820 mL 2.9640 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.17 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.17 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.17 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Aficamten
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