p38α-IN-12
p38α-IN-12 is an orally bioavailable p38α MAPK inhibitor, with an IC50 of 0.11 nM and a Ki of 0.2 nM against human targets. p38α-IN-12 inhibits the production of TNFα in cellular systems and exerts in vivo efficacy in acute mouse models.
For research use only. We do not sell to patients.
- CAS No.: 630106-85-3
- Formula: C22H17N7O2
- Molecular Weight:411.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | IC50 |
6 nM
Compound: 2x
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Inhibition of LPS-induced TNFalpha production in human PBMC
Inhibition of LPS-induced TNFalpha production in human PBMC
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[PMID: 18359226] |
In Vitro
p38α-IN-12 (compound 2x) inhibits LPS-induced TNFα production in human peripheral blood mononuclear cells with an IC50 of 6 nM[1].
p38α-IN-12 does not significantly inhibit human CYP 450 isoforms 1A2, 2C9, 2C19, 2D6, or 3A4, with IC50 values >40 μM for each[1].
p38α-IN-12 shows excellent metabolic stability in human and rat liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | Bioavailability | Clearance (CL) | Vd | T1/2 |
|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 60 % | 0.3 | 1.3 L/kg | 4.1 h |
Chemical Information
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CAS No. 630106-85-3
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Molecular Weight 411.43
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Formula C22H17N7O2
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SMILES
O=C(NC1=NOC=C1)C2=CC=C(C(=C2)NC3=NC=NC4=C3C=NN4C=5C=CC=CC5)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
p38α-IN-12 Related Classifications
HY-183042 Related Classifications
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