Doramapimod
Synonym(s):Doramapimod, BIRB796, 1-(5- tert-Butyl-2- p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, JNK Inhibitor XVII;Doramapimod, BIRB796, 1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, JNK Inhibitor XVII;p38 MAP Kinase Inhibitor X, BIRB 796 - CAS 285983-48-4 - Calbiochem
- CAS NO.:285983-48-4
- Empirical Formula: C31H37N5O3
- Molecular Weight: 527.66
- MDL number: MFCD09752957
- EINECS: 1308068-626-2
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is Doramapimod?
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
The Uses of Doramapimod
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 bo rtezomib-triggered upregulation of p38 MAPK and Hsp27 phosphorylation leading to enhanced cytotoxicity and caspase activation.
The Uses of Doramapimod
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.
What are the applications of Application
Doramapimod is a potent p38α MAPK and JNK2 inhibitor
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
Properties of Doramapimod
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. |
Safety information for Doramapimod
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Doramapimod
New Products
(S)-3-Aminobutanenitrile hydrochloride 4-Methylphenylacetic acid N-Boc-D-alaninol N-BOC-D/L-ALANINOL Tert-butyl bis(2-chloroethyl)carbamate 3-Morpholino-1-(4-nitrophenyl)-5,6-dihydropyridin- 2(1H)-one Furan-2,5-Dicarboxylic Acid Tropic acid 1-Bromo-3,5-Di-Tert-Butylbenzene S-2-CHLORO PROPIONIC ACID ETHYL ISOCYANOACETATE 2-Bromo-1,3-Bis(Dimethylamino)Trimethinium Hexafluorophosphate 4-IODO BENZOIC ACID 3-NITRO-2-METHYL ANILINE 1-(2,4-DICHLOROPHENYL) ETHANAMINE (2-Hydroxyphenyl)acetonitrile 4-Bromopyrazole 2-(Cyanocyclohexyl)acetic acid 4-methoxy-3,5-dinitropyridine 1-(4-(aminomethyl)benzyl)urea hydrochloride 2-aminopropyl benzoate hydrochloride diethyl 2-(2-((tertbutoxycarbonyl)amino) ethyl)malonate tert-butyl 4- (ureidomethyl)benzylcarbamate Ethyl-2-chloro((4-methoxyphenyl)hydrazono)acetateRelated products of tetrahydrofuran
You may like
-
Doramapimod 98% CAS 285983-48-4View Details
285983-48-4 -
Doramapimod 98% (HPLC) CAS 285983-48-4View Details
285983-48-4 -
p38 MAP Kinase Inhibitor X, BIRB 796 CAS 285983-48-4View Details
285983-48-4 -
1975-50-4 98%View Details
1975-50-4 -
2-HYDROXY BENZYL ALCOHOL 98%View Details
90-01-7 -
2-Chloro-1,3-Bis(Dimethylamino)Trimethinium Hexafluorophosphate 221615-75-4 98%View Details
221615-75-4 -
14714-50-2 (2-Hydroxyphenyl)acetonitrile 98+View Details
14714-50-2 -
118753-70-1 98+View Details
118753-70-1