JAK1/TYK2-IN-3
JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells.
For research use only. We do not sell to patients.
- CAS No.: 2734918-37-5
- Formula: C17H21F2N7O
- Molecular Weight:377.39
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Tyk2 6 nM (IC50) |
JAK1 37 nM (IC50) |
JAK2 140 nM (IC50) |
JAK3 362 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| H9c2 | IC50 |
13.4 μM
Compound: 48
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Cytotoxicity against rat H9C2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against rat H9C2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
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[PMID: 35113547] |
| HUVEC | IC50 |
76.7 μM
Compound: 48
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Cytotoxicity against HUVEC cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
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[PMID: 35113547] |
| L02 | IC50 |
146.9 μM
Compound: 48
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Cytotoxicity against human LO2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against human LO2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
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[PMID: 35113547] |
JAK1/TYK2-IN-3 (compound 48) (10, 20, 30 mg/kg) shows anti-inflammatory effect by regulating the formation of Th1, Th2, Th17 cells[1].
JAK1/TYK2-IN-3 (10, 20, 30 mg/kg) inhibits the NF-κB signaling pathway by inhibits the JAK-STAT pathway, thereby reducing the inflammatory response in ulcerative colitis (UC) mice[1].
JAK1/TYK2-IN-3 (10, 20, 30 mg/kg) dose-dependently inhibits the mRNA expression of TNF-α, IL-1β, IL-12, IL-17A, IL-22, IFN-α, and IFN-β[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
JAK1/TYK2-IN-3 (5 mg/kg, p.o.) shows 23.7% oral bioavailability in rats[1].
Pharmacokinetic Parameters of JAK1/TYK2-IN-3 in male Sprague-Dawley rats[1].
| compd | dose(mg/kg) | Administration | Cmax(ng/mL) | Cl (Lh-1kg-1) | T1/2(h) | AUC0-t(ng·h/mL) | F (%) |
| 48 | 5 mg/kg | p.o. | 400.4±55.3 | 11.3±5.2 | 2.4±2.1 | 440.9±157.0 | 23.7 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8 weeks, 270-325g male Sprague-Dawley rats[1]
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Dosage:5 mg/kg
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Administration:p.o.
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Result:Showed 23.7% oral bioavailability in rats.
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Animal Model:Six-eight week old male C57BL/6 mice, 20-22 g (2.5% dextran sulfate sodium (DSS)-induced acute UC mouse model)[1]
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Dosage:10, 20, 30 mg/kg
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Administration:p.o., twice a day, 12 days
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Result:Improved the infiltration of inflammatory factors and reduced the damage caused by DSS.
Chemical Information
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CAS No. 2734918-37-5
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Molecular Weight 377.39
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Formula C17H21F2N7O
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SMILES
O=C1NCCC12CCN(C3=NC(NC4=CN(C(F)F)N=C4)=NC=C3C)CC2
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JAK1/TYK2-IN-3 Related Classifications
HY-143885 Related Classifications
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