Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Targets |
p38α (pKi = 8.1); p38β (pKi = 7.6)
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ln Vitro |
Losmapimod (GW856553X, GW856553, GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor.
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ln Vivo |
Losmapimod attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1beta (IL-1beta) after significantly enhancing survival, endothelial-dependent and -independent vascular relaxation, and indicators of renal function in spontaneously hypertensive stroke-prone rats (SHR-SP). [1]
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Enzyme Assay |
A ligand-displacement fluorescence polarization assay is used to determine the inhibition of p38β and p38.
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Cell Assay |
For two hours, cells were exposed to the drug at the indicated concentration.
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Animal Protocol |
Male SHR-SPs (n=70) were divided into five groups (n=14 per group) based on body weight and randomly assigned to one of five diets: normal diet controls (ND), high salt-fat diet controls (SFD), SFD + GSK-AHAB (1.2 mg/kg/day), and SFD + GSK-AHAB (12 mg/kg/day) and SFD + MK 966 (18 mg/kg/day). All medications are taken orally by mixing with SFD. The conscious measurement of mean arterial blood pressure and heart rate is performed on a subgroup of animals from each group (n=6 per group) who have undergone anesthesia and have been surgically outfitted with radiotelemetry devices. Before the study begins, these animals are given at least 7 days to recover.
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References |
Molecular Formula |
C22H26FN3O2
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Molecular Weight |
383.46
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Exact Mass |
383.20
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Elemental Analysis |
C, 68.91; H, 6.83; F, 4.95; N, 10.96; O, 8.34
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CAS # |
585543-15-3
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Related CAS # |
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Appearance |
white solid powder
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SMILES |
CC1=C(C=C(C=C1F)C(=O)NC2CC2)C3=NC=C(C=C3)C(=O)NCC(C)(C)C
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InChi Key |
KKYABQBFGDZVNQ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H26FN3O2/c1-13-17(9-15(10-18(13)23)21(28)26-16-6-7-16)19-8-5-14(11-24-19)20(27)25-12-22(2,3)4/h5,8-11,16H,6-7,12H2,1-4H3,(H,25,27)(H,26,28)
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Chemical Name |
6-[5-(cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)pyridine-3-carboxamide
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Synonyms |
GW856553; Losmapimod; GSKAHAB; GW856553X; GW-856553; GW 856553, GSK-AHAB; GSK AHAB; GW-856553X; GW 856553X; SB856553; SB-856553; SB 856553
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.75 mg/mL (7.17 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.75 mg/mL (7.17 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (7.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2.5 mg/mL (6.52 mM) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix well. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 6: 4% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6078 mL | 13.0392 mL | 26.0783 mL | |
5 mM | 0.5216 mL | 2.6078 mL | 5.2157 mL | |
10 mM | 0.2608 mL | 1.3039 mL | 2.6078 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04264442 | Active Recruiting |
Drug: Losmapimod | Facioscapulohumeral Muscular Dystrophy (FSHD) |
Fulcrum Therapeutics | February 13, 2020 | Phase 2 |
NCT04004000 | Active Recruiting |
Drug: Losmapimod | Facioscapulohumeral Muscular Dystrophy 1 |
Fulcrum Therapeutics | August 23, 2019 | Phase 2 |
NCT05397470 | Active Recruiting |
Drug: Losmapimod Drug: Placebo oral tablet |
Facioscapulohumeral Muscular Dystrophy (FSHD) |
Fulcrum Therapeutics | June 16, 2022 | Phase 3 |
NCT01756495 | Active Recruiting |
Drug: Losmapimod Drug: Moxifloxacin |
Acute Coronary Syndrome | GlaxoSmithKline | January 10, 2013 | Phase 1 |
NCT01039961 | Completed | Drug: losmapimod Drug: losmapimod 1 mg |
Cardiovascular Disease | GlaxoSmithKline | February 2, 2010 | Phase 1 |
Structure (A) and activity profile (B) of GSK-AHAB, anarylheteroarylbis-carboxyamide series p38 MAPK inhibitor.J Pharmacol Exp Ther.2009 Sep;330(3):964-70. td> |
A, plasma concentration of GSK-AHAB and rofecoxib after 4 weeks of dietary dosing. B, COX1 and COX2 activity was determined in rofecoxib samples obtained at 8:00 AM.J Pharmacol Exp Ther.2009 Sep;330(3):964-70. td> |
Effects of treatment on survival (A) and mean arterial blood pressure (B) in stroke-prone, SHR-SPs placed on a SFD.J Pharmacol Exp Ther.2009 Sep;330(3):964-70. td> |
Urinary albumin excretion and creatinine clearance was determined at baseline before introduction of the SFD and at 2, 4, and 6 weeks of the study in all groups.J Pharmacol Exp Ther.2009 Sep;330(3):964-70. td> |
Vascular relaxation studies were performed in isolated thoracic aorta ring segments obtained from stroke-prone hypertensive rats maintained on a SFD for 8 weeks.J Pharmacol Exp Ther.2009 Sep;330(3):964-70. td> |
PRA and plasma concentrations of aldosterone and IL-1β were measured from blood samples obtained at 4 and 8 weeks of the study and in all groups.J Pharmacol Exp Ther.2009 Sep;330(3):964-70. td> |