Envudeucitinibum hydrochloride
Envudeucitinibum (Envudeucitinib; ESK-001) hydrochloride is an orally active and selective TYK2 allosteric inhibitor with an IC50 range of 104-149 nM. Envudeucitinibum hydrochloride blocks JH1 catalytic activity by specifically binding to the JH2 domain of TYK2, thereby inhibiting downstream signaling pathways. Envudeucitinibum hydrochloride is used for research on plaque psoriasis, systemic lupus erythematosus, and other immune-mediated diseases.
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- CAS No.: 3009133-87-0
- Formule: C22H19D6ClN6O3
- Masse moléculaire:462.96
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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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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
Tyk2 104-149 nM (IC50) |
JAK1 30 μM (IC50) |
JAK2 30 μM (IC50) |
JAK3 30 μM (IC50) |
IL-13 |
IL-23 |
In Vitro
Envudeucitinibum (Envudeucitinib; ESK-001) hydrochloride significantly inhibits IL-12-, IL-23-, and IFNα-stimulated STAT phosphorylation and downstream IFNγ production in a concentration-dependent manner in human whole blood and peripheral blood mononuclear cells[1].
Envudeucitinibum hydrochloride is a highly selective allosteric TYK2 inhibitor with an IC50 of 104-149 nM in human whole blood and no off-target effects against JAK1-3 (IC50 >30 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 3009133-87-0
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Masse moléculaire 462.96
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Formule C22H19D6ClN6O3
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SMILES
COC1=C(C2=NN(C([2H])([2H])[2H])C=N2)C=CC=C1NC3=C(C(CC([2H])([2H])[2H])=O)C=NC(NC(C4CC4)=O)=C3.Cl
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Synonyms
Envudeucitinib hydrochloride; ESK-001 hydrochloride
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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
[1]. Ucpinar S, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamics of the oral allosteric TYK2 inhibitor ESK-001 using a randomized, double-blind, placebo-controlled study design. Clinical and translational science. 2024 Dec;17(12):e70094. [Content Brief]
[2]. Papp KA, et al. Safety and efficacy of envudeucitinib, a highly selective, oral allosteric TYK2 inhibitor, in patients with moderate-to-severe plaque psoriasis: Results from the 52-week open-label extension period of the phase 2 STRIDE study. Journal of the American Academy of Dermatology. 2026 Jan;94(1):187-195. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Envudeucitinibum hydrochloride Related Classifications
HY-153701S1 Related Classifications
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Keywords
- Envudeucitinibum
- 3009133-87-0
- Envudeucitinib
- ESK-001
- ESK001
- ESK 001
- JAK
- STAT
- Interleukin Related
- IFNAR
- Isotope-Labeled Compounds
- JH2-JH1 inhibitory interaction
- TYK2-mediated disorders
- plaque psoriasis
- pSTAT1 expression
- Type I IFN-induced gene signature
- SIGLEC1 expression
- catalytic JH1 domain signaling
- allosteric TYK2 inhibitor
- regulatory JH2 domain
- IFNα-stimulated whole blood T cells
- Inhibitor
- inhibitor
- inhibit