Losmapimod (GW856553X)

Name: Losmapimod (GW856553X)
Brand: Selleck Chemicals
SKU: S7215
Rating: 5 (5 reviews)

For research use only. Not for use in humans.

Catalog No.S7215 Synonyms: GW856553, GSK-AHAB

5 publications

Losmapimod (GW856553X) Chemical Structure

Molecular Weight(MW): 383.46

Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pK_i of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.

Selleck's Losmapimod (GW856553X) has been cited by 5 publications

Cell Signal, 2020, 68:109528

PubMed: 31917191 ( click the link to review the publication )

J Neurogenet, 2018, 32(2):106-117

PubMed: 29718742 ( click the link to review the publication )

Pharmacol Res, 2018, 128:244-251

PubMed: 29079427 ( click the link to review the publication )

Oncotarget, 2018, 9(51):29680-29697

PubMed: 30038713 ( click the link to review the publication )

Auton Autacoid Pharmacol, 2015, 35(3):32-40

PubMed: 26913580 ( click the link to review the publication )

1 Customer Review

Intracellular pathways of b-adrenoceptor-induced proliferation. Urothelial proliferation (% of basal responses) in T24 in the absence and presence of (d) losmapimod (1-30 μM).

Auton Autacoid Pharmacol, 2015, 35(3):32-40.. Losmapimod (GW856553X) purchased from Selleck.

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

Biological Activity

Description

Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pK_i of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.

Targets

p38α ^[1] (Cell-free assay)	p38β ^[1] (Cell-free assay)
8.1(pKi)	7.6(pKi)

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
PBMC	NUHGeolmTnWwY4Tpc44h[XO\|YYm=		Ml30NUBp		Mn\CTY5pcWKrdHnvckBw\iCyM{jhcJBp[S2mZYDlcoRmdnRiVF7GZYxxcGFicILv[JVkfGmxbjDpckBpfW2jbjDQRm1EKHC{ZXnuZ5Vj[XSnZDDmc5IhOSCqcjDi[YZwemViTGDTJINp[WyuZX7n[UBjgSCHTFnTRUwhUUN3ME2wMlEh\|ryP	MXKxPVc4OjJ6Nx?=

... Click to View More Cell Line Experimental Data

In vivo

In spontaneously hypertensive stroke-prone rats (SHR-SP), Losmapimod significantly improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and subsequently attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1beta (IL-1beta). ^[1]

Protocol

Animal Research: ^[1]	- Collapse Animal Models: Spontaneously hypertensive stroke-prone rats Formulation: -- Dosages: ~12 mg/kg Administration: p.o. (Only for Reference)

References

[1] Willette RN, et al. J Pharmacol Exp Ther. 2009, 330(3), 964-970.

Solubility (25°C)

In vitro	DMSO	76 mg/mL (198.19 mM)
	Ethanol	41 mg/mL warmed (106.92 mM)
	Water	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Losmapimod (GW856553X) SDF

Molecular Weight	383.46
Formula	C₂₂ H₂₆ F N₃ O₂
CAS No.	585543-15-3
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	GW856553, GSK-AHAB
Smiles	CC1=C(F)C=C(C=C1C2=CC=C(C=N2)C(=O)NCC(C)(C)C)C(=O)NC3CC3

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04004000	Recruiting	Drug: Losmapimod	Facioscapulohumeral Muscular Dystrophy 1	Fulcrum Therapeutics	August 23 2019	Phase 2
NCT04003974	Recruiting	Drug: Losmapimod\|Drug: Placebo oral tablet	Facioscapulohumeral Muscular Dystrophy (FSHD)	Fulcrum Therapeutics	August 9 2019	Phase 2
NCT02000440	Completed	Drug: Losmapimod	Glomerulosclerosis Focal Segmental	GlaxoSmithKline	July 1 2014	Phase 2
NCT00976560	Completed	Drug: GW856553\|Other: Placebo	Depressive Disorder Major	GlaxoSmithKline	September 25 2009	Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

p38 MAPK Signaling Pathway Map

Related p38 MAPK Products

Pexmetinib (ARRY-614) ^New

Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
SB239063 ^New

SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.
Ravoxertinib (GDC-0994) ^New

GDC-0994 is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
SB203580

SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM.

Features:First reported p38 inhibitor.
Doramapimod (BIRB 796)

Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with K_d of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.

Features:The first p38 MAPK inhibitor to be tested in a phase III clinical trial.
SB202190 (FHPI)

SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo.
Ralimetinib (LY2228820)

Ralimetinib (LY2228820) is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.
PH-797804

PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.
VX-702

VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.

Features:Highly selective, orally active inhibitor of p38 MAPK.
TAK-715

TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.

Choose Your Country or Region

By Signaling Pathways

By product type

Losmapimod (GW856553X)