285983-48-4 Doramapimod AKSci X7401
 
 
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  X7401    AKSci Reference Standard
Doramapimod
, 98% (HPLC)
 
BIRB 796




IDENTITY
CAS Number:285983-48-4
MDL Number:MFCD09752957
MF:C31H37N5O3
MW:527.66
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:98% (HPLC)
Physical Form (at 20°C):Solid
Melting Point:143-147°C
Density:1.2
Refractive Index:1.62
Long-Term Storage:Store long-term at -20°C
DOT/IATA TRANSPORT INFORMATION
Not hazardous material

BIOLOGICAL INFO
Solubility:DMSO 106 mg/mL
Application(s):P38a MAPK inhibitor
Form:Free base

REVIEW

 Doramapimod is a highly potent cell-permeable N-pyrazole-N''-naphthly urea inhibitor of p38 MAPK that blocks TNFalpha release in LPS-stimulated THP-1 cells. The stress-activated p38 mitogen-activated protein kinase (MAPK) plays a critical role in regulating the production of proinflammatory cytokines such as tumor necrosis factor and interleukin-1.

REFERENCES
[1]Regan, John; Breitfelder, Steffen; Cirillo, Pier; Gilmore, Thomas; Graham, Anne G.; Hickey, Eugene; Klaus, Bernhard; Madwed, Jeffrey; Moriak, Monica; Moss, Neil; et al. Pyrazole Urea-Based Inhibitors of p38 MAP Kinase: From Lead Compound to Clinical Candidate. Journal of Medicinal Chemistry. (2002) 45(14): 2994-3008.
[2] 'Schreiber S, Feagan B, D''Haens G, Colombel JF, Geboes K, Yurcov M, Isakov V, Golovenko O, Bernstein CN, Ludwig D, Winter T, Meier U, Yong C, Steffgen J; BIRB 796 Study Group. Oral p38 mitogen-activated protein kinase inhibition with BIRB 796 for active Crohn''s disease: a randomized, double-blind, placebo-controlled trial. Clin Gastroenterol Hepatol. (2006) Mar;4(3): 325-34.'
[3] Ryoo S, Choi J, Kim J, Bae S, Hong J, Jo S, Kim S, Lee Y. BIRB 796 has Distinctive Anti-inflammatory Effects on Different Cell Types. Immune Netw. (2013) Dec;13(6): 283-8.
[4] Cirillo, Pier F.; Gilmore, Thomas A.; Hickey, Eugene R.; Regan, John R.; Zhang, Lin-Hua Preparation of aromatic heterocyclic ureas as antiinflammatory agents PCT Int. Appl. (2000), WO 2000043384 A1 20000727.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


Current as of April 15, 2024

AKSci Reference Standards are high-purity, low-impurity compounds suitable for use as standards.


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