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Losmapimod

Cat. No. M3751
Losmapimod Structure
Synonym:

GW-856553

Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 360 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Losmapimod is a promising new agent against cardiovascular diseases. This compound works by inhibiting p38 MAP kinases, which play an important role in the development of atherosclerosis and heart failure caused by ischemic conditions. Losmapimod did not cause an improvement in exercise tolerance or lung function, despite being well-tolerated in this COPD population.The p38 MAPK inhibitor losmapimod (GW856553) attenuates the pro-inflammatory response in humans by reducing PIC production.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Spontaneously hypertensive stroke-prone rats
Formulation
Dosages ~12 mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 383.46
Formula C22H26FN3O2
CAS Number 585543-15-3
Purity >98%
Solubility DMSO
Storage at -20°C
References

A low-frequency variant in MAPK14 provides mechanistic evidence of a link with myeloperoxidase: a prognostic cardiovascular risk marker.
Waterworth DM, et al. J Am Heart Assoc. 2014 Aug 27;3(4). PMID: 25164947.

Losmapimod, a novel p38 mitogen-activated protein kinase inhibitor, in non-ST-segment elevation myocardial infarction: a randomised phase 2 trial.
Newby LK, et al. Lancet. 2014 Sep 27;384(9949):1187-95. PMID: 24930728.

Evaluation of antidepressant properties of the p38 MAP kinase inhibitor losmapimod (GW856553) in Major Depressive Disorder: Results from two randomised, placebo-controlled, double-blind, multicentre studies using a Bayesian approach.
Inamdar A, et al. J Psychopharmacol. 2014 Apr 2;28(6):570-581. PMID: 24699061.

Efficacy and safety of the p38 MAPK inhibitor losmapimod for patients with chronic obstructive pulmonary disease: a randomised, double-blind, placebo-controlled trial.
Watz H, et al. Lancet Respir Med. 2014 Jan;2(1):63-72. PMID: 24461903.

Losmapimod: a novel drug against cardiovascular diseases?
Dewenter M, et al. Dtsch Med Wochenschr. 2013 Jan;138(1-2):39-42. PMID: 23250695.

Safety, tolerability, pharmacokinetics and pharmacodynamics of losmapimod following a single intravenous or oral dose in healthy volunteers.
Barbour AM, et al. Br J Clin Pharmacol. 2013 Jul;76(1):99-106. PMID: 23215699.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Losmapimod, GW-856553 supplier, p38 MAPK, inhibitors

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