Iso-AS601245 TFA
Iso-AS601245 TFA is an orally active JNK inhibitor, with IC50 values of 0.15 μM, 0.22 μM and 0.07 μM against JNK1, JNK2 and JNK3, respectively. Iso-AS601245 TFA reduces plasma TNF-α levels in mice and inhibits IL-2 secretion in activated T cells. Iso-AS601245 TFA alleviates adjuvant-induced rheumatoid arthritis in mice. Iso-AS601245 TFA can be used in studies related to rheumatoid arthritis.
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- CAS No.: 1644386-60-6
- Formule: C24H18F6N6O4S
- Masse moléculaire:600.49
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
JNK1 0.15 μM (IC50) |
JNK2 0.22 μM (IC50) |
JNK3 0.07 μM (IC50) |
IL-2 |
In Vitro
Iso-AS601245 (Compound 59) (10 μM; 24.5 h) TFA inhibits IL-2 secretion by PMA (HY-18739)- and Ionomycin (HY-13434)-stimulated Jurkat human T lymphoblasts by 90% at a concentration of 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat human T lymphoblast cell line
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Concentration:10 μM
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Incubation Time:30-minute pre-incubation; 24-hour stimulation/incubation
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Result:Inhibited IL-2 secretion by PMA and ionomycin-stimulated Jurkat cells by 90%.
Showed no observed cell toxicity at 10 μM.
In Vivo
Iso-AS601245 (60 mg/kg; p.o.; daily; 7 days) TFA significantly reduces paw swelling, clinical scores, cartilage erosion, and synovium inflammation in a mouse model of collagen-induced arthritis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C3H/HEN mice (8-week-old)[1]
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Dosage:0.3 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Caused a dose-dependent decrease in plasma TNF-α levels.
Achieved an ED50 of 3 mg/kg.
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Animal Model:DBA/1 mice (8-12-week-old, male)[1]
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Dosage:20 mg/kg; 60 mg/kg
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Administration:p.o.; daily; 7 days
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Result:Elicited significant depression of paw swelling at 60 mg/kg.
Reduced total clinical score at 60 mg/kg.
Revealed significant preservation of joint areas (reduced cartilage erosion) and reduced synovium inflammation at 60 mg/kg.
Chemical Information
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CAS No. 1644386-60-6
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Masse moléculaire 600.49
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Formule C24H18F6N6O4S
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SMILES
OC(C(F)(F)F)=O.N#C/C(C1=NC(NCCC2=CN=CC=C2)=NC=C1)=C3NC4=CC=CC=C4S/3.OC(C(F)(F)F)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Iso-AS601245 TFA Related Classifications
HY-10612A Related Classifications
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