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Chemical Structure| 1642288-47-8 Chemical Structure| 1642288-47-8

Structure of Mavacamten
CAS No.: 1642288-47-8

Chemical Structure| 1642288-47-8

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MYK-461 is a myosin inhibitor potentially for the treatment of hypertrophic cardiomyopathy, and can reduce contractility by decreasing the adenosine triphosphatase activity of the cardiac myosin heavy chain.

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Product Details of Mavacamten

CAS No. :1642288-47-8
Formula : C15H19N3O2
M.W : 273.33
SMILES Code : O=C1N(C(C)C)C(C=C(N[C@H](C2=CC=CC=C2)C)N1)=O
MDL No. :MFCD31746877

Safety of Mavacamten

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302-H319-H332-H372-H400
Precautionary Statements:P260-P264-P270-P273-P280-P301+P312+P330-P304+P312-P305+P351+P338-P314-P337+P313-P391-P501
Class:9
UN#:3077
Packing Group:

Related Pathways of Mavacamten

cytoskeleton

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Adult rat ventricular cardiomyocytes 0.18 µM (IC50) MYK-461 reduced fractional shortening in a dose-dependent manner without altering calcium transients PMC4784435
Mouse cardiac myofibrils 0.3 µM (IC50) MYK-461 reduced ATPase activity in a dose-dependent manner, with maximal doses (>10 µM) reducing the ATPase rate by ~90% PMC4784435
Rabbit psoas myofibrils 0.1-50 µM Mavacamten decreased the kinetics of force development in fast skeletal myofibrils, while it had no effect in human ventricular myofibrils. PMC8077167
Human ventricular myofibrils 0.1-50 µM Mavacamten had a fast, fully reversible, and dose-dependent negative effect on maximal Ca2+-activated isometric force at 15°C, which can be explained by a sudden decrease in the number of heads functionally available for interaction with actin. PMC8077167

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice HCM Mice models expressing α-cardiac myosin heavy chain missense mutations (R403Q, R719W, or R453C) Oral administration in drinking water 2.5 mg/kg Daily administration for 20 to 26 weeks (preventive treatment) or 4 weeks (reversal treatment) MYK-461 reduced cardiac contractility in a dose-dependent manner, prevented or ameliorated left ventricular hypertrophy (LVH), reduced myocardial fibrosis and cardiomyocyte disarray, and improved gene expression profiles PMC4784435

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT06112743 Cardiomyopathy, Hypertrophic PHASE4 RECRUITING 2026-07-31 Local Institution - 0087, West... More >> Hollywood, California, 90048-1804, United States|Piedmont Hospital, Atlanta, Georgia, 30309, United States|Local Institution - 0091, Honolulu, Hawaii, 96813-2414, United States|Local Institution - 0093, Boston, Massachusetts, 02114, United States|University Hospitals Cleveland Medical Center - 11100 Euclid Ave, Cleveland, Ohio, 44106, United States|Allegheny General Hospital, Pittsburgh, Pennsylvania, 15212-4756, United States|Houston Methodist Hospital, Houston, Texas, 77030, United States|Local Institution - 0035, Murray, Utah, 84107-5701, United States|Local Institution - 0075, Caba, Buenos Aires, 0, Argentina|Local Institution - 0076, Ciudad Autónoma de Buenos Aires, Buenos Aires, C1093AAS, Argentina|Local Institution - 0079, Pilar, Buenos Aires, B1629ODT, Argentina|Local Institution - 0077, Ciudad De Cordoba, Cordoba, X5000JHGQ, Argentina|Local Institution - 0074, Rosario, Santa FE, S2000GAP, Argentina|Local Institution - 0080, Buenos Aires, C1181ACH, Argentina|Royal Prince Alfred Hospital, Camperdown, New South Wales, 2050, Australia|Local Institution - 0082, Darlinghurst, New South Wales, 2010, Australia|Prince Charles Hospital, Chermside, Queensland, 4032, Australia|Local Institution - 0022, Herston, Queensland, 4029, Australia|The Alfred Hospital, Melbourne, Victoria, 3004, Australia|Local Institution - 0057, Klagenfurt am W?rthersee, K?rnten, 9020, Austria|Local Institution - 0032, Braunau am Inn, Upper Austria, 5280, Austria|Local Institution - 0028, Graz, 8036, Austria|Local Institution - 0088, Wien, 1090, Austria|Local Institution - 0007, Wien, 1100, Austria|Local Institution - 0084, Anderlecht, Brussels, 1070, Belgium|Local Institution - 0070, Bruxelles, Brussels, 1200, Belgium|Local Institution - 0069, Jette, Brussels, 1090, Belgium|Local Institution - 0092, Genk, Limburg, 3600, Belgium|Local Institution - 0083, Leuven, Vlaams Brabant, 3000, Belgium|Local Institution - 0071, Roeselare, West-Vlaanderen, 8800, Belgium|Local Institution - 0004, Calgary, Alberta, T2N 1N4, Canada|Local Institution - 0001, Montreal, Quebec, H1T 1C8, Canada|Local Institution - 0068, Quebec, G1V 4G5, Canada|Local Institution - 0016, Broumov, Královéhradecky Kraj, 550 01, Czechia|Local Institution - 0053, Trinec, Moravskoslezsky Kraj, 739 61, Czechia|Local Institution - 0050, Prague, Praha, Hlavní Mesto, 140 21, Czechia|Local Institution - 0011, Praha 2, Praha, Hlavní Mesto, 128 21, Czechia|Local Institution - 0052, Brno, 656 91, Czechia|Local Institution - 0073, Helsinki, Etel?-Suomen L??ni, 00290, Finland|Local Institution - 0072, Turku, L?nsi-Suomen L??ni, 20540, Finland|Local Institution - 0031, Grenoble, 38043, France|Local Institution - 0014, Paris, 75015, France|Local Institution - 0026, Pessac, 33604, France|Local Institution - 0002, Rennes, 35000, France|Local Institution - 0047, Giessen, Hessen, 35392, Germany|Local Institution - 0034, G?ttingen, Niedersachsen, 37075, Germany|Local Institution - 0040, Bad Oeynhausen, Nordrhein-Westfalen, 32545, Germany|Local Institution - 0023, Berlin, 12203, Germany|Local Institution - 0009, Athina, Attiki, 115 27, Greece|Local Institution - 0008, Athina, Attiki, 176 74, Greece|Local Institution - 0059, Chaidari, Athens, Attiki, 124 62, Greece|Local Institution - 0037, Heraklion, 71110, Greece|Local Institution - 0006, Thessaloniki, 546 36, Greece|Local Institution - 0021, Thessaloniki, 546 42, Greece|Local Institution - 0042, Pécs, Baranya, 7621, Hungary|Local Institution - 0054, Szeged, Csongrád, 6720, Hungary|Local Institution - 0020, Balatonfüred, Veszprém, 8230, Hungary|Local Institution - 0019, Budapest, 1083, Hungary|Local Institution - 0013, Budapest, 1096, Hungary|Local Institution - 0041, Budapest, 1097, Hungary|Local Institution - 0063, Budapest, 1134, Hungary|Local Institution - 0038, Milano, Lombardia, 20149, Italy|Local Institution - 0060, Milano, Lombardia, 20162, Italy|Local Institution - 0056, Pavia, Lombardia, 27100, Italy|Local Institution - 0048, Firenze, Toscana, 50139, Italy|Local Institution - 0062, Pisa, Toscana, 56124, Italy|Local Institution - 0051, Arezzo, 52100, Italy|Local Institution - 0018, Warszawa, Mazowieckie, 02-507, Poland|Local Institution - 0094, Warszawa, Mazowieckie, 04-628, Poland|Local Institution - 0044, Katowice, Slaskie, 40-555, Poland|Local Institution - 0049, Zabrze, Slaskie, 41-800, Poland|Local Institution - 0064, Bialystok, 15-276, Poland|Local Institution - 0012, Lódz, 93-338, Poland|Local Institution - 0043, Palma de Mallorca, Baleares, 07198, Spain|Local Institution - 0046, Malaga, Málaga, 29010, Spain|Local Institution - 0030, Barcelona, 08035, Spain|Local Institution - 0089, Madrid, 28034, Spain|Local Institution - 0081, Madrid, 28035, Spain|Local Institution - 0045, Salamanca, 37007, Spain|Local Institution - 0039, Sevilla, 41013, Spain|Luzerner Kantonsspital (LUKS), Luzern, Luzern (de), 6000, Switzerland|Istituto Cardiocentro Ticino, Lugano, Ticino (it), 6900, Switzerland|Local Institution - 0055, Lugano, Ticino (it), 6900, Switzerland|Local Institution - 0036, Bern, 3010, Switzerland|H?pitaux Universitaires de Genève, Geneva, 1205, Switzerland|Universit?tsspital Zürich, Zürich (de), 8091, Switzerland|Local Institution - 0027, Belfast, Antrim, BT16 1RH, United Kingdom|Leeds General Infirmary, Leeds, Yorkshire, LS1 3EX, United Kingdom|Local Institution - 0010, London, SW17 0QT, United Kingdom Less <<
NCT05135871 Hypertrophic Cardiomyopathy PHASE1 COMPLETED 2022-02-28 Huashan Hospital Fudan Univers... More >>ity, Shanghai, Shanghai, 200040, China Less <<
NCT05362045 Healthy Participants PHASE1 COMPLETED 2022-08-19 Clinical pharmacology of Miami... More >>, Miami, Florida, 33014, United States|Advanced Pharma CR, LLC, Miami, Florida, 33147, United States|QPS Springfield, Springfield, Missouri, 65802, United States|Ppd Phase I Clinic, Austin, Texas, 78744, United States Less <<
NCT06549608 Hypertrophic Cardiomyopathy ACTIVE_NOT_RECRUITING 2025-04-18 St. Paul's Hospital, Vancouver... More >>, British Columbia, Canada Less <<
NCT05414175 Cardiomyopathy, Hypertrophic O... More >>bstructive Less << PHASE3 ACTIVE_NOT_RECRUITING 2026-03-06 Local Institution - 0020, Uwaj... More >>ima, Ehime, 798-8510, Japan|Local Institution - 0026, Himeji-Shi, Hyogo, 672-8044, Japan|Local Institution - 0016, Kobe-shi, Hyogo, 650-0047, Japan|Local Institution - 0017, Tsukuba-Shi, Ibaraki, 305-0005, Japan|Local Institution - 0023, Kanazawa-shi, Ishikawa, 920-8641, Japan|Local Institution - 0019, Yokohama, Kanagawa, 227-8501, Japan|Local Institution - 0015, Nankoku-shi, Kochi, 783-8505, Japan|Local Institution - 0028, Tsu-Shi, MIE, 514-0001, Japan|Local Institution - 0027, Sendai, Miyagi, 980-8574, Japan|Local Institution - 0011, Suita-Shi, Osaka, 565-0871, Japan|Local Institution - 0014, Suita, Osaka, 564-8565, Japan|Local Institution - 0012, Hamamatsu-city, Shizuoka, 431-3192, Japan|Local Institution - 0010, Bunkyo-Ku, Tokyo, 113-0033, Japan|Local Institution - 0009, Chuo-Ku, Tokyo, 104-0044, Japan|Local Institution - 0003, Fuchu-Shi, Tokyo, 1830003, Japan|Local Institution - 0001, Itabashi-Ku, Tokyo, 173-0003, Japan|Local Institution - 0007, Koto-Ku, Tokyo, 135-0061, Japan|Local Institution - 0005, Shinjuku-Ku, Tokyo, 160-8582, Japan|Local Institution - 0013, Shinjuku-ku, Tokyo, 162-8666, Japan|Local Institution - 0018, Osaka, 558-8558, Japan Less <<
NCT06338202 Obstructive Hypertrophic Cardi... More >>omyopathy (oHCM) Less << RECRUITING 2024-11-01 London Health Science Centre (... More >>LHSC), London, Ontario, N6A 5A5, Canada Less <<
NCT06551129 Obstructive Hypertrophic Cardi... More >>omyopathy Less << RECRUITING 2027-06-30 Analysis Group Inc., Boston, M... More >>assachusetts, 02199, United States Less <<
NCT05719805 Healthy Participants PHASE1 COMPLETED 2023-07-25 Local Institution - 0001, Miam... More >>i, Florida, 33136, United States|Local Institution - 0002, Saint Paul, Minnesota, 55114, United States Less <<
NCT05939700 Breastfeeding|Hypertrophic Car... More >>diomyopathy|Pregnancy Related Less << RECRUITING 2025-04-27 The Mavacamten Pregnancy Surve... More >>illance Program, PPD Inc, Wilmington, North Carolina, 28401-3331, United States Less <<
NCT06146660 Obstructive Hypertrophic Cardi... More >>omyopathy Less << RECRUITING 2026-11-30 Local Institution - 0001, Seou... More >>l, 06234, Korea, Republic of|Novotech Laboratory Korea Co., Ltd., Seoul, 06234, Korea, Republic of Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.66mL

0.73mL

0.37mL

18.29mL

3.66mL

1.83mL

36.59mL

7.32mL

3.66mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

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