Tyk2-IN-5
Based on 2 publication(s) in Google Scholar
Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis.
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- Purity : 99.35%
- CAS No.: 1797432-62-2
- 화학식: C21H19FN8O2
- 분자량:434.43
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tyk2-IN-5
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Biological Activity
제품 설명
IC50 & Target
[1]|
Tyk2 JH2 0.086 nM (Ki) |
IFNα 25 nM (IC50) |
In Vitro
Tyk2-IN-5 inhibits Jak1-3 with IC50 values of >2 μM and displays the Jak1-3 dependent cellular activities of >12.5 μM (IC50 values)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Tyk2-IN-5 (1, 10 mg/kg; p.o.; single) inhibits IL-12/IL-18 induced IFNγ production in a dose-dependent manner[1].
Tyk2-IN-5 (10 mg/kg; p.o.; single) shows a high oral exposure and bioavailability (114%) in rat[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lewis male rats (rat adjuvant arthritis model)[1].
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Dosage:5, 10 mg/kg
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Administration:Oral administration; twice daily for 20 days
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Result:Demonstrated full efficacy to prevent the rats′ paw from swelling.
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Animal Model:Lewis male rats (IL-12/IL-18-induced)[1].
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Dosage:1, 10 mg/kg
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Administration:Oral administration; single
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Result:Inhibited IL-12/IL-18 induced IFNγ production by 45% and 77% at doses of 1 and 10 mg/kg, respectively.
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Animal Model:Lewis male rats, mouse[1].
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Dosage:10 mg/kg
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Administration:Oral administration; single
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Result:
1.19 Pharmacokinetic Parameters of Tyk2-IN-5 in mouse and rat[1].
PO (10 mg/kg) mouse rat Cmax (μM) 15 9.4 AUC0-24 (μM•h) 19 57 CL (mL/min/kg) 16 7.8 F (%) 86 114
Chemical Information
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CAS No. 1797432-62-2
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Appearance Solid
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분자량 434.43
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화학식 C21H19FN8O2
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Color Light yellow to yellow
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SMILES
O=C1C(NC2=NN3C(C(NC)=C2)=NC=C3C(N[C@H]4[C@@H](F)C4)=O)=CC=CN1C5=CC=CC=N5
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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J Ethnopharmacol
"Shihu" promote T-cell immunity against breast cancer through bioactive constituent THMB enhancing JAK3-STAT1 signal. [Abstract]2026 Oct 28:369:121888. PMID: 42202911
용액&용해도
In Vitro:
DMSO : 43.33 mg/mL (99.74 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.17 mg/mL (5.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
순도&문서
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Data Sheet (285 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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3019 mL | 11.5093 mL | 23.0187 mL | 57.5467 mL |
| 5 mM | 0.4604 mL | 2.3019 mL | 4.6037 mL | 11.5093 mL | |
| 10 mM | 0.2302 mL | 1.1509 mL | 2.3019 mL | 5.7547 mL | |
| 15 mM | 0.1535 mL | 0.7673 mL | 1.5346 mL | 3.8364 mL | |
| 20 mM | 0.1151 mL | 0.5755 mL | 1.1509 mL | 2.8773 mL | |
| 25 mM | 0.0921 mL | 0.4604 mL | 0.9207 mL | 2.3019 mL | |
| 30 mM | 0.0767 mL | 0.3836 mL | 0.7673 mL | 1.9182 mL | |
| 40 mM | 0.0575 mL | 0.2877 mL | 0.5755 mL | 1.4387 mL | |
| 50 mM | 0.0460 mL | 0.2302 mL | 0.4604 mL | 1.1509 mL | |
| 60 mM | 0.0384 mL | 0.1918 mL | 0.3836 mL | 0.9591 mL | |
| 80 mM | 0.0288 mL | 0.1439 mL | 0.2877 mL | 0.7193 mL |
Tyk2-IN-5 Related Classifications
HY-111745 Related Classifications
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