Envudeucitinibum
Based on 1 Customer Validation
Envudeucitinibum (Envudeucitinib; ESK-001) is an orally active and selective TYK2 allosteric inhibitor with an IC50 range of 104-149 nM. Envudeucitinibum blocks JH1 catalytic activity by specifically binding to the JH2 domain of TYK2, thereby inhibiting downstream signaling pathways. Envudeucitinibum is used for research on plaque psoriasis, systemic lupus erythematosus, and other immune-mediated diseases.
For research use only. We do not sell to patients.
- Purity : 99.56%
- CAS No.: 2417135-66-9
- Formula: C22H18D6N6O3
- Molecular Weight:426.50
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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 |
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. 2417135-66-9
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Unlabeled CAS 2417134-93-9
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Appearance Solid
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Molecular Weight 426.50
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Formula C22H18D6N6O3
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Color White to off-white
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SMILES
COC1=C(C2=NN(C([2H])([2H])[2H])C=N2)C=CC=C1NC3=CC(NC(C4CC4)=O)=NC=C3C(CC([2H])([2H])[2H])=O
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Synonyms
Envudeucitinib; ESK-001
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (234.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Imiquimod-Induced Psoriasiform Dermatitis
Imiquimod (IMQ)-induced psoriasiform dermatitis is a widely used murine model in which topical application of IMQ, a Toll-like receptor 7 (TLR7) agonist, triggers innate immune activation in the skin and induces a psoriasis-like inflammatory cascade characterized by epidermal hyperplasia, immune cell infiltration, and cytokine production dominated by the IL-23/IL-17 axis. This inflammatory response is mediated through activation of dendritic cells and downstream induction of IL-23, IL-17A, IL-22, and related pro-inflammatory mediators, recapitulating key features of human plaque psoriasis and enabling mechanistic and therapeutic studies. The model is commonly induced using Aldara (5% IMQ cream) applied topically to murine skin, resulting in rapid onset of erythema, scaling, and thickening that can be quantified as disease severity indices and validated histologically.
Purity & Documentation
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Data Sheet (287 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3447 mL | 11.7233 mL | 23.4467 mL | 58.6166 mL |
| 5 mM | 0.4689 mL | 2.3447 mL | 4.6893 mL | 11.7233 mL | |
| 10 mM | 0.2345 mL | 1.1723 mL | 2.3447 mL | 5.8617 mL | |
| 15 mM | 0.1563 mL | 0.7816 mL | 1.5631 mL | 3.9078 mL | |
| 20 mM | 0.1172 mL | 0.5862 mL | 1.1723 mL | 2.9308 mL | |
| 25 mM | 0.0938 mL | 0.4689 mL | 0.9379 mL | 2.3447 mL | |
| 30 mM | 0.0782 mL | 0.3908 mL | 0.7816 mL | 1.9539 mL | |
| 40 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.4654 mL | |
| 50 mM | 0.0469 mL | 0.2345 mL | 0.4689 mL | 1.1723 mL | |
| 60 mM | 0.0391 mL | 0.1954 mL | 0.3908 mL | 0.9769 mL | |
| 80 mM | 0.0293 mL | 0.1465 mL | 0.2931 mL | 0.7327 mL | |
| 100 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.5862 mL |
Envudeucitinibum Related Classifications
HY-153701S Related Classifications
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Keywords
- Envudeucitinibum
- 2417135-66-9
- Envudeucitinib
- ESK-001
- ESK001
- ESK 001
- 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