Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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
Synonyms | AS-19375 | HMS3747G11 | GTPL5668 | SMR004458704 | BIRB-0796 | 1-[3-(1,1-Dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-3-[4-[2-(morpholin-4-yl)ethoxy]naphthalen-1-yl]urea | CCG-264915 | HY-10320 | 1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3-[4- |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Doramapimod 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 Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | MAP kinase p38 alpha inhibitor |
Note | Wherever 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. |
ALogP | 5.7 |
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Pubchem Sid | 488188270 |
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Pubchem Sid Url | https://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 |
CAS Registry No. | 285983-48-4 |
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DiscoveRx TREEspot | BIRB-796| |
PubChem CID | 156422 |
ChEMBL Ligand | CHEMBL103667 |
RCSB PDB Ligand | B96 |
PubChem SID | 488188270 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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D23131149 | Certificate of Analysis | Mar 01, 2023 | D125100 |
D23131200 | Certificate of Analysis | Mar 01, 2023 | D125100 |
D23131204 | Certificate of Analysis | Mar 01, 2023 | D125100 |
D23131211 | Certificate of Analysis | Mar 01, 2023 | D125100 |
D23131217 | Certificate of Analysis | Mar 01, 2023 | D125100 |
B1525024 | Certificate of Analysis | Nov 16, 2022 | D125100 |
Solubility | Soluble in DMSO (~25 mg/ml), water (poorly soluble), ethanol (~3 mg/ml), and DMF (~25 mg/ml). |
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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, 9 (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] |