BMS-582949 - Moligand™, 10mM in DMSO , MAP kinase p38 alpha inhibitor, CAS No.623152-17-0, MAP kinase p38 alpha inhibitor

CAS: 623152-17-0 Cat. No.: B408984 Fórmula: C₂₂H₂₆N₆O₂ Peso molecular: 406.48 Número CE: 677-739-6

GRAU & PUREZA Moligand™, 10mM in DMSO

Synonyms

PS540446 | Pyrrolo[2,​1-​f]​[1,​2,​4]​triazine-​6-​carboxamide, 4-​[[5-​[(cyclopropylamino)​carbonyl]​-​2-​methylphenyl]​amino]​-​5-​methyl-​N-​propyl-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

BMS-582949 BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.
In vitro

BMS-582949 is found to inhibit p38 activation in cells, as measured by phosphorylation of p38. BMS-582949 treatment of cells in which p38 has been activated by LPS rapidly reversed p38 activation as shown by loss of phosphorylation of p38. BMS-582949 is therefore a dual action p38 kinase inhibitor, inhibiting both p38 kinase activity and p38 activation in cells. BMS-582949 binding to p38a results in a conformational change of the activation loop which is phosphorylated by upstream kinases, therefore it inhibits phosphorylation of p38 by upstream MKK by inducing a less accessible conformation of the activation loop.

In vivo

The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And at an oral dose of 10 mg/kg, the mouse AUC0-8 h for BMS-582949 is 75.5 μM•h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively.
Cell Data

cell lines：Human colon carcinoma cell line HT-29

Concentrations：

Incubation Time：

Powder Purity:≥99%

Especificações

Sinónimos

PS540446 | Pyrrolo[2,​1-​f]​[1,​2,​4]​triazine-​6-​carboxamide, 4-​[[5-​[(cyclopropylamino)​carbonyl]​-​2-​methylphenyl]​amino]​-​5-​methyl-​N-​propyl-

Especificações e pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos e fisiológicos

BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Grau

Moligand™

Tipo de ação

INHIBITOR

Mecanismo de ação

MAP kinase p38 alpha inhibitor

Propriedades do produto

ALogP

3.269

hba_count

4

Contagem HBD

3

Ligação rotativa

7

Nomes e identificadores

SMILES isoméricas

CCCNC(=O)C1=CN2C(=C1C)C(=NC=N2)NC3=C(C=CC(=C3)C(=O)NC4CC4)C

Peso molecular

406.48

Reaxy-Rn

11821218

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11821218&ln=

Alvos associados (humanos)

MAPK14 Tchem Mitogen-activated protein kinase 14 (3 Activities)

Discover Target: MAPK14

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propriedades químicas e físicas

• DMSO (mg/mL) Solubilidade máxima: 81
• DMSO (mM) Solubilidade máxima: 199.2717969
• Água (mg/mL) Solubilidade máxima: ＜1