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Doramapimod - ≥99%, high purity , MAP kinase p38 alpha inhibitor, CAS No.285983-48-4, MAP kinase p38 alpha inhibitor

  • Moligand™
  • ≥99%
Item Number
D125100
Grouped product items
SKUSizeAvailabilityPrice Qty
D125100-10mg
10mg
Available within 1-2 weeks(?)
Item is derived from our semi-finished stock and is processed in 1-2 weeks.
$64.90
D125100-50mg
50mg
Available within 1-2 weeks(?)
Item is derived from our semi-finished stock and is processed in 1-2 weeks.
$146.90
D125100-250mg
250mg
In stock
$661.90

Potent, selective, cell permeable p38 MAPK inhibitor

Basic Description

SynonymsDoramapimod|285983-48-4|BIRB-796|BIRB 796|BIRB 796 (Doramapimod)|BIRB796|BIRB-796 BS|BIRB 796 BS|3-[3-tert-butyl-1-(4-methylphenyl)-1H-pyrazol-5-yl]-1-{4-[2-(morpholin-4-yl)ethoxy]naphthalen-1-yl}urea|1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(
Specifications & PurityMoligand™, ≥99%
Biochemical and Physiological MechanismsDoramapimod is a highly selective p38α MAPK inhibitor to TNF-α with EC50 of 18 nM. At 10 μM, doramapimod inhibits JNK2 in vitro, but at the low concentration necessary to inhibit p38α, it does not affect the phosphorylation of JNK substrates in cells.Pote
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionMAP kinase p38 alpha inhibitor
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

BIRB 796 (Doramapimod) is a highly selective p38α MAPK inhibitor with Kd of 0.1 nM, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2, ZAP-70, EGFR, HER2, PKA, PKC, PKCα/β/γ.
A p38α MAPK and JNK2;p38 MAPK抑制剂

Product Properties

ALogP5.7

Names and Identifiers

Pubchem Sid488188270
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488188270
IUPAC Name 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea
INCHI InChI=1S/C31H37N5O3/c1-22-9-11-23(12-10-22)36-29(21-28(34-36)31(2,3)4)33-30(37)32-26-13-14-27(25-8-6-5-7-24(25)26)39-20-17-35-15-18-38-19-16-35/h5-14,21H,15-20H2,1-4H3,(H2,32,33,37)
InChi Key MVCOAUNKQVWQHZ-UHFFFAOYSA-N
Canonical SMILES CC1=CC=C(C=C1)N2C(=CC(=N2)C(C)(C)C)NC(=O)NC3=CC=C(C4=CC=CC=C43)OCCN5CCOCC5
Isomeric SMILES CC1=CC=C(C=C1)N2C(=CC(=N2)C(C)(C)C)NC(=O)NC3=CC=C(C4=CC=CC=C43)OCCN5CCOCC5
PubChem CID 156422
Molecular Weight 527.67

Certificates

Certificate of Analysis(COA)

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6 results found

Lot NumberCertificate TypeDateItem
D23131149Certificate of AnalysisMar 01, 2023 D125100
D23131200Certificate of AnalysisMar 01, 2023 D125100
D23131204Certificate of AnalysisMar 01, 2023 D125100
D23131211Certificate of AnalysisMar 01, 2023 D125100
D23131217Certificate of AnalysisMar 01, 2023 D125100
B1525024Certificate of AnalysisNov 16, 2022 D125100

Chemical and Physical Properties

SolubilitySoluble in DMSO (~25 mg/ml), water (poorly soluble), ethanol (~3 mg/ml), and DMF (~25 mg/ml).

Related Documents

References

1. Pargellis C, Tong L, Churchill L, Cirillo PF, Gilmore T, Graham AG, Grob PM, Hickey ER, Moss N, Pav S et al..  (2002)  Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site..  Nat Struct Biol,  (4): (268-72).  [PMID:11896401]
2. Moffett K, Konteatis Z, Nguyen D, Shetty R, Ludington J, Fujimoto T, Lee KJ, Chai X, Namboodiri H, Karpusas M et al..  (2011)  Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD)..  Bioorg Med Chem Lett,  21  (23): (7155-65).  [PMID:22014550]
3. Ivshina MP et al..  (2022)  CPEB1 regulates the inflammatory immune response, phagocytosis, and alternative polyadenylation in microglia..  Glia,  70  (10): (1850-1863).  [PMID:35635122]
4. Lanfranco MF et al..  (2021)  Expression and secretion of apoE isoforms in astrocytes and microglia during inflammation..  Glia,  69  (6): (1478-1493).  [PMID:33556209]

Solution Calculators