Doramapimod
Doramapimod Basic information
- Product Name:
- Doramapimod
- Synonyms:
-
- 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(2-morpholinoethoxy)-1-naphthyl]urea
- 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea
- BIRB 796; BIRB-796; BIRB796;
- CS-379
- BIRB 796 - BIRB 0796 | Doramapimod
- CS-1863
- BIBR-796
- 1-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(4-(2-morpholinoethoxy)naphthalen-1-yl)urea
- CAS:
- 285983-48-4
- MF:
- C31H37N5O3
- MW:
- 527.66
- EINECS:
- 1308068-626-2
- Product Categories:
-
- Anti-cancer&immunity
- Aromatics
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Protein Kinase Inhibitors and Activators
- Inhibitors
- MAPK
- Mol File:
- 285983-48-4.mol
Doramapimod Chemical Properties
- Melting point:
- 142-143 °C
- Boiling point:
- 631.6±55.0 °C(Predicted)
- Density
- 1.20±0.1 g/cm3(Predicted)
- storage temp.
- Sealed in dry,Store in freezer, under -20°C
- solubility
- Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 30 mg/ml).
- form
- solid
- pka
- 13.47±0.70(Predicted)
- color
- White or off-white
- Stability:
- 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.
Doramapimod Usage And Synthesis
Description
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.
Chemical Properties
Pale Beige Solid
Uses
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].
storage
Store at -20°C
References
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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Doramapimod(285983-48-4)Related Product Information
- Cyhalofop-butyl
- Diethylene glycol monobutyl ether
- Moroxydine hydrochloride
- Butylnaphtalenesulfonic Acid Sodium Salt
- tert-Butanol
- tert-Butylchlorodiphenylsilane
- Buprofezin
- 2-Butoxyethanol
- Tridemorph
- Moroxydine
- Butyl acetate
- Butyl acrylate
- Dimethomorph
- MORPHINE
- 5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-ylamine
- 4-(2-MORPHOLIN-4-YLETHOXY)ANILINE
- 4-(2-Morpholinoethoxy)naphthalen-1-amine
- BIRB 796 (Doramapimod)