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 Summenformel: C₂₂H₂₆N₆O₂ Molekulargewicht: 406.48 EG-Nummer: 677-739-6

QUALITÄT & REINHEIT 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

Übersicht

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%

Spezifikationen

Synonyme

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

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

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.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Mechanismus der Wirkung

MAP kinase p38 alpha inhibitor

Produkteigenschaften

ALogP

3.269

hba_count

4

HBD-Zahl

3

Rotationsfähige Bindung

7

Namen und Kennungen

Isomere SMILES

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

Molekulargewicht

406.48

Reaxy-Rn

11821218

Reaxys-RN_link_address

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

Zugehörige Ziele (menschlich)

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)

Chemische und physikalische Eigenschaften

• DMSO (mg/ml) Maximale Löslichkeit: 81
• DMSO (mM) Maximale Löslichkeit: 199.2717969
• Wasser (mg/ml) Maximale Löslichkeit: ＜1