MSC 2032964A
MSC 2032964A is an orally active, selective inhibitor for apoptosis signal-regulating kinase 1(ASK1) with IC50 of 96 nM. MSC 2032964A preserves the visual responses in EAE mice model and exhibits potency in ameliorating the neuroinflammation.
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- CAS. Nr.: 1124381-43-6
- Formel: C16H13F3N6O
- Molecular Weight:362.31
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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ASK1 96 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | IC50 |
13 nM
Compound: 3; MSC2032964A
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Inhibition of V5 tagged human ASK1 expressed in HEK-293T cells assessed as reduction in T838 autophosphorylation incubated for 1 hr
Inhibition of V5 tagged human ASK1 expressed in HEK-293T cells assessed as reduction in T838 autophosphorylation incubated for 1 hr
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[PMID: 31710475] |
MSC 2032964A (10 μM) reveals a good metabolic stability with microsomal clearance <4 ml/min/mg, and a good apparent permeability[1].
MSC 2032964A (10 μM) inhibits Lipopolysaccharide (LPS, HY-D1056)-induced ASK1 and p38 phosphorylation in mouse astrocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mouse astrocytes
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Concentration:10 μM
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Incubation Time:90 min
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Result:Inhibited phosphorylation of ASK1 and p38.
MSC 2032964A (30 mg/kg, p.o., once daily for 40 days) attenuates neurological symptoms in both spinal cord and optic nerve lesions, and thus ameliorates the MOG (35-55) (HY-P1240)-induced autoimmune encephalomyelitis in C57BL/6J mice model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MOG (35-55)-induced autoimmune encephalomyelitis in C57BL/6J mice[1]
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Dosage:30 mg/kg
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Administration:p.o., once daily for 40 days
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Result:Reduced demyelination in optic nerve, decreased astrocyte and microglia activation in spinal cord.
Chemical Information
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CAS. Nr. 1124381-43-6
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Molecular Weight 362.31
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Formel C16H13F3N6O
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SMILES
O=C(C1=CC=CN=C1)NC2=NN3C(NC4CC4)=CC(C(F)(F)F)=CC3=N2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)