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Cat. No.: HY-110262

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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 No.: 1124381-43-6
Formule: C₁₆H₁₃F₃N₆O
Masse moléculaire:362.31

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

MSC 2032964A Chemical Structure

CAS No.: 1124381-43-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

ASK1

96 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform MAP3K :

Voir tous les produits spécifiques à Isoform p38 MAPK :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	13 nM Compound: 3; MSC2032964A	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	[PMID: 31710475]

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

mouse astrocytes
Concentration:

10 μM
Incubation Time:

90 min
Result:

Inhibited phosphorylation of ASK1 and p38.

In Vivo

MSC 2032964A (5 mg/kg, p.o.) exhibits an oral bioavailability of 82%, a clearance of 1.1 L/kg/ h, a half-life of 5.2 h and a volume of distribution V_ss of 1.0 L/kg in SPrague Dawley rats^[1].
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.

Animal Model:

MOG (35-55)-induced autoimmune encephalomyelitis in C57BL/6J mice^[1]
Dosage:

30 mg/kg
Administration:

p.o., once daily for 40 days
Result:

Reduced demyelination in optic nerve, decreased astrocyte and microglia activation in spinal cord.

Chemical Information

CAS No. 1124381-43-6
Masse moléculaire 362.31
Formule C₁₆H₁₃F₃N₆O
SMILES

O=C(C1=CC=CN=C1)NC2=NN3C(NC4CC4)=CC(C(F)(F)F)=CC3=N2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Guo X, et al., Regulation of the severity of neuroinflammation and demyelination by TLR-ASK1-p38 pathway. EMBO Mol Med. 2010 Dec;2(12):504-15. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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MSC 2032964A

High-Throughput Bioactive Compound Library

Voir tous les produits spécifiques à Isoform MAP3K

Voir tous les produits spécifiques à Isoform p38 MAPK

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

MSC 2032964A Related Classifications

HY-110262 Related Classifications