ChemicalBook > CAS DataBase List > tiraseMtiv (CK-2017357)

tiraseMtiv (CK-2017357)

Product Name: tiraseMtiv (CK-2017357)
CAS No.: 1005491-05-3
Chemical Name: tiraseMtiv (CK-2017357)
Synonyms: CS-1484;TiraseMtiv;CK 2017357;Tirasemitiv;Tirasemtiv, >=98%;tiraseMtiv (CK-2017357);Tirasemtiv, 10 mM in DMSO;Tirasemtiv(CK-2017357), >98%;Troponin Activator, CK-2017357;CK-2017357; CK2017357; CK 2017357
CBNumber: CB92631164
Molecular Formula: C12H14N4O
Formula Weight: 230.27
MOL File: 1005491-05-3.mol

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tiraseMtiv (CK-2017357) Property

Melting point:: >130°C (dec.)
storage temp.: -20°C Freezer
solubility: DMSO (Slightly), Methanol (Slightly)
form: Solid
color: Beige to Brown

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H320Causes eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 26075
Product name: Tirasemtiv
Purity: ≥98%
Packaging: 5mg
Price: $47
Updated: 2024/03/01

Cayman Chemical

Product number: 26075
Product name: Tirasemtiv
Purity: ≥98%
Packaging: 10mg
Price: $84
Updated: 2024/03/01

Cayman Chemical

Product number: 26075
Product name: Tirasemtiv
Purity: ≥98%
Packaging: 25mg
Price: $182
Updated: 2024/03/01

Cayman Chemical

Product number: 26075
Product name: Tirasemtiv
Purity: ≥98%
Packaging: 50mg
Price: $272
Updated: 2024/03/01

TRC

Product number: T446700
Product name: Tirasemtiv
Packaging: 25mg
Price: $150
Updated: 2021/12/16

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tiraseMtiv (CK-2017357) Chemical Properties,Usage,Production

Description

Tirasemtiv is an activator of the fast skeletal troponin complex. It selectively binds to purified fast skeletal troponin complex (K_d = 40 nM) over slow skeletal (K_d = 3,800 nM) and cardiac troponin complexes. Tirasemtiv (20 μM) slows the rate of calcium release from the fast skeletal troponin complex. It increases the ATPase activity of isolated rabbit fast skeletal myofibrils at a fixed calcium concentration (EC₅₀ = 390 nM) and sensitizes skinned fast skeletal muscle fibers isolated from human and rabbit to calcium in a concentration-dependent manner. Tirasemtiv increases in situ extensor digitorum longus (EDL) muscle force and forelimb grip strength in a rat model of myasthenia gravis. It also increases forelimb grip strength, grid hang test performance, and rotarod performance in a mouse model of amyotrophic lateral sclerosis (ALS) when administered at a dose of 10 mg/kg.

Uses

Tirasemtiv is a fast skeletal muscle troponin activator and is used for treating patients with amyotrophic lateral sclerosis (ALS).

in vivo

A single dose of Tirasemtiv significantly increases submaximal isometric force, forelimb grip strength, grid hang time, and rotarod performance in a female transgenic mouse model (B6SJL-SOD1^G93A) of ALS with functional deficits. Additionally, diaphragm force and tidal volume are significantly higher in Tirasemtiv-treated female B6SJL-SOD1^G93A mice. At the 25% deficit milestone, vehicle-treated B6SJL-SOD1^G93A mice demonstrated forelimb grip strength of 49.6±4.6 g. Tirasemtiv increases grip strength by 38% to 68.6±8.1g (p<0.05, single tailed t-test). Tirasemtiv doses of 2, 2, 2, and 4 mg/kg given at approximately 20 min intervals to achieve a cumulative dose of 10 mg/kg. Regression analysis of the log dose vs. response relationship indicated that Tirasemtiv significantly increased muscle force in WT and mid-stage B6SJL-SOD1^G93A mice (WT p<0.0001; mid-stage p=0.0028). At later stages of disease, the mice exhibited a trend for increased muscle function in response to Tirasemtivcompared to baseline (p=0.064)^[1].

References

[1] ALAN J RUSSELL. Activation of fast skeletal muscle troponin as a potential therapeutic approach for treating neuromuscular diseases[J]. Nature Medicine, 2012, 18 3: 452-455. DOI: 10.1038/nm.2618
[2] DARREN T HWEE. Fast skeletal muscle troponin activator tirasemtiv increases muscle function and performance in the B6SJL-SOD1G93A ALS mouse model.[J]. PLoS ONE, 2014: e96921. DOI: 10.1371/journal.pone.0096921

tiraseMtiv (CK-2017357) Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from tiraseMtiv (CK-2017357) manufacturers

Wuhan Nutra Biotechnology Co.,Ltd

Product: Tirasemtiv;CK-2017357 1005491-05-3
Price: US $500.00-0.00/g
Min. Order: 1g
Purity: 98%+
Supply Ability: 100kgs
Release date: 2021-05-24

Career Henan Chemical Co

Product: tiraseMtiv (CK-2017357) 1005491-05-3
Price: US $1.00/KG
Min. Order: 1KG
Purity: 95%
Supply Ability: 200KG
Release date: 2018-08-19

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