Doramapimod

Bezeichnung:Doramapimod

CAS-Nr285983-48-4

Englisch Name:Doramapimod

CBNumberCB2855127

SummenformelC31H37N5O3

Molgewicht527.66

MOL-Datei285983-48-4.mol

Doramapimod physikalisch-chemischer Eigenschaften

Schmelzpunkt	142-143 °C
Siedepunkt	631.6±55.0 °C(Predicted)
Dichte	1.20±0.1 g/cm3(Predicted)
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 30 mg/ml).
Aggregatzustand	solid
pka	13.47±0.70(Predicted)
Farbe	White or off-white
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.

Sicherheit

HS Code

2934999090

Gefahreninformationscode (GHS)

Doramapimod Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Doramapimod (285983-48-4) potently and selectively inhibits p38 MAPK by simultaneously binding to the ATP-binding domain and an allosteric site.1?(IC50=18 nM). Displays anti-inflammatory activity2?but differential effects on inflammatory genes3. Cell permeable.
Chemische Eigenschaften
Pale Beige Solid
Verwenden
Doramapimod is a highly potent inhibitor of p38 mitogen-activated protein kinase (MAPK). Doramapimod is a potential agent for the treatment of inflammatory diseases. Doramapimod blocks baseline and bortezomib-triggered upregulation of p38 MAPK and Hsp27 phosphorylation leading to enhanced cytotoxicity and caspase activation.
Definition
ChEBI: A member of the class of pyrazoles that is an immunomodulator used for treatment of rheumatoid arthritis, Crohn's disease and psoriasis.
in vitro
birb 796 is a picomolar inhibitor of human p38 map kinase with a 12,000-fold increase in binding affinity. moreover, birb 796 behavors as one of the most potent and slowest dissociating human p38 map kinase inhibitors now known [1].
in vivo
in a lps-stimulated tnf-α synthesis mouse model, a 65% inhibition of tnf-α synthesis was observed when birb 796 was dosed orally at 10 mg/kg. in a model of established collagen-induced arthritis using b10.riii mice, birb 796 showed a 63% inhibition of arthritis severity when dosed orally at 30 mg/kg qd [2].
Lager
Store at -20°C
Einzelnachweise
1) Pargellis?et al. (2002),?Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site; Nat. Struct. Biol.,?9?268 2) Branger?et al.?(2002),?Anti-inflammatory effects of a p38 mitogen-activated protein kinase inhibitor during human endotoxemia; J. Immunol.,?168?4070 3) Joos?et al. (2010),?Differential effects of p38MAP kinase inhibitors on the expression of inflammation-associated genes in primary, interleukin-1 beta-stimulated human chondrocytes; Br. J. Pharmacol.,?160?1252

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