JAK1/3-IN-1
JAK1/3-IN-1 is a selective, orally active JAK1/3 inhibitor with IC50 values of 1.9 nM and 0.9 nM, respectively. JAK1/3-IN-1 significantly reduces the mean arterial blood pressure and significantly increases the heart rate in rabbits. JAK1/3-IN-1 decreases the mean arterial blood pressure in conscious telemetered rats and induces lethal cardiovascular effects.
For research use only. We do not sell to patients.
- CAS No.: 1400687-19-5
- Formula: C22H28N6O2
- Molecular Weight:408.51
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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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JAK1 1.9 nM (IC50) |
JAK3 0.9 nM (IC50) |
JAK2 15 nM (IC50) |
Tyk2 25 nM (IC50) |
ROCK1 95 nM (IC50) |
ROCK2 43 nM (IC50) |
JAK1/3-IN-1 (Compound 35) potently inhibits purified JAK1, JAK3, TYK2, JAK2, Rho kinase 1, and Rho kinase 2, with IC50 values of 1.9 nM, 0.9 nM, 25 nM, 15 nM, 95 nM, and 43 nM, respectively[1].
JAK1/3-IN-1 inhibits IL-2-induced IFN-γ production in whole blood with an IC50 of 100 nM[1].
JAK1/3-IN-1 (10 μM) exhibits moderate Caco-2 cell permeability, a long human microsomal half-life, and no PXR activation activity. At a concentration of 10 μM, it shows a 16% inhibition rate on Ca2+ channels and a 71% inhibition rate on Na+ channels, with moderate cross-species plasma protein binding levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Tmax | AUC | T1/2 | Bioavailability | CL | Vss |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | / | / | 4.9 μM·h | 6.5 h | / | 16.7 mL/min/kg | 8.2 L/kg |
| Mice[1] | 10 mg/kg | p.o. | 1.1 μM | 4 h | 17.9 μM·h | 10.2 h | 73 % | / | / |
| Rat[1] | 2 mg/kg | i.v. | / | / | 5.8 μM·h | 9.8 h | / | 14.1 mL/min/kg | 11.5 L/kg |
| Rat[1] | 10 mg/kg | p.o. | 0.6 μM | 7.3 h | 12.9 μM·h | 12.2 h | 44 % | / | / |
Single administration of JAK1/3-IN-1 (>3 mg/kg) significantly reduces the mean arterial blood pressure and increases the heart rate in rabbits[1].
JAK1/3-IN-1 (30-200 mg/kg; p.o.; single administration) reduces the mean arterial blood pressure of conscious telemetered rats and induces lethal cardiovascular effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD)[1]
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Dosage:30 mg/kg (blood pressure decrease); 200 mg/kg (lethal effects)
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Administration:p.o.; single dose
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Result:Caused a 14% decrease in mean arterial blood pressure at 30 mg/kg.
Resulted in a rapid decrease in mean arterial pressure leading to death (200 mg/kg) .
Chemical Information
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CAS No. 1400687-19-5
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Molecular Weight 408.51
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Formula C22H28N6O2
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SMILES
N(C=1C=2N(C=C(C2)C=3C=CC(OC)=NC3)N=CC1C(N)=O)[C@H]4C(C)(C)[C@@](C)(N)CC4
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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)
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