Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-(2,4-dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]aMino]-

Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-(2,4-dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]aMino]- Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

FRAX486 is an inhibitor of group I p21-activated kinases (PAKs; IC₅₀s = 8.25, 39.5, and 55.3 nM for PAK1, PAK2, and PAK3, respectively). It is selective for group I PAKs over PAK4, a group II PAK (IC₅₀ = 779 nM). FRAX486 (20 mg/kg) reverses decreases in the mean density of apical dendritic spines in the temporal cortex in the Fmr1^-/- mouse model of fragile X syndrome. It completely abolishes audiogenic seizures, hyperactivity, and stereotypical movements in Fmr1^-/- mice when administered at a dose of 30 mg/kg. FRAX486 prevents adolescent cortical dendritic spine loss and rescues prepulse inhibition deficits in a Disc1 knockdown mouse model of schizophrenia.

Verwenden

FRAX 486 is a small-molecule PAK inhibitor. This compound has neuroprotective properties.

Biochem/physiol Actions

FRAX486 is a potent, group I-selective p21-activated kinase (PAK) inhibitor (PAK1/2/3 IC50 = 8.25/39.5/55.3 nM; group II PAK4 IC50 = 779 nM). FRAX486 effectively inhibits PAK-mediated PKD1 Ser203 phosphorylation and PAK1/2 Ser144/141 autophosphorylation upon angiotensin II (ANGII) stimulation of rat IEC-18 cells (IC50 ～0.5 μM) and exhibits in vivo efficacy in rescuing the autism-like phenotypes among Fmr1 knockout fragile syndrome (FXS) mice (20 mg/kg s.c.) as well as in ameliorating schizophrenia-associated dendritic spine deterioration among Disc1 knockdown mice (10 μg/g or 10 mg/kg i.p.) with good pharmacokinetic properties and blood–brain barrier (BBB) permeability.

Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-(2,4-dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]aMino]- Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-(2,4-dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]aMino]- Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10523	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58
Hangzhou MolCore BioPharmatech Co.,Ltd.	+86-057181025280; +8617767106207	sales@molcore.com	China	49739	58
Nantong HI-FUTURE Biology Co., Ltd.	+undefined18051384581	sales@chemhifuture.com	China	3136	58
TargetMol Chemicals Inc.	+1-781-999-5354	support@targetmol.com	United States	19973	58
Shanghai Acmec Biochemical Technology Co., Ltd.	+undefined18621343501	product@acmec-e.com	China	33349	58
Aladdin Scientific	+1-833-552-7181	sales@aladdinsci.com	United States	57511	58
Amadis Chemical Company Limited	571-89925085	sales@amadischem.com	China	131981	58
Dalian Meilun Biotech Co., Ltd.	0411-62910999 13889544652	sales@meilune.com	China	4647	58

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• FRAX486
• Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-(2,4-dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]aMino]-
• 6-(2,4-dichlorophenyl)-8-ethyl-2-{[3-fluoro-4-(1-piperazinyl)phen Yl]amino}pyrido[2,3-d]pyrimidin-7(8h)-one FRAX597
• 6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
• CS-1943
• 6-(2,4-dichlorophenyl)-8-ethyl-2-((3-fluoro-4-(piperazin-1-yl)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one
• FRAX 486; FRAX-486
• 1232030-35-1
• C25H23Cl2FN6O