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Losmapimod

Cat. No. M3751
Losmapimod Structure
Synonym:

GW-856553X; GSK-AHAB; SB856553

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 55  USD55 In stock
10mg USD 77  USD77 In stock
25mg USD 155  USD155 In stock
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Quality Control & Documentation
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. The p38 MAPK inhibitor losmapimod (GW856553) attenuates the pro-inflammatory response in humans by reducing PIC production.

Protocol (for reference only)
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.
Chemical Information
Molecular Weight 383.46
Formula C22H26FN3O2
CAS Number 585543-15-3
Solubility (25°C) DMSO 25 mg/mL
Ethanol 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Waterworth DM, et al. J Am Heart Assoc. A low-frequency variant in MAPK14 provides mechanistic evidence of a link with myeloperoxidase: a prognostic cardiovascular risk marker.

[2] Newby LK, et al. Lancet. Losmapimod, a novel p38 mitogen-activated protein kinase inhibitor, in non-ST-segment elevation myocardial infarction: a randomised phase 2 trial.

[3] Inamdar A, et al. J Psychopharmacol. 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.

[4] Watz H, et al. Lancet Respir Med. Efficacy and safety of the p38 MAPK inhibitor losmapimod for patients with chronic obstructive pulmonary disease: a randomised, double-blind, placebo-controlled trial.

[5] Dewenter M, et al. Dtsch Med Wochenschr. Losmapimod: a novel drug against cardiovascular diseases?

[6] Barbour AM, et al. Br J Clin Pharmacol. Safety, tolerability, pharmacokinetics and pharmacodynamics of losmapimod following a single intravenous or oral dose in healthy volunteers.

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Keywords: Losmapimod, GW-856553X; GSK-AHAB; SB856553 supplier, p38 MAPK, inhibitors, activators

 
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