Blovacitinib
Based on 1 Customer Validation
Blovacitinib (TUL01101) is a potent, selective and orally active JAK1 inhibitor, with an IC50s of 3, 37, 1517 and 36 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Blovacitinib can be used for the research of rheumatoid arthritis.
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- Purity: 99.71%
- CAS No.: 2411222-97-2
- 화학식: C22H25F2N5O2
- 분자량:429.46
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보관:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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JAK1 3 nM (IC50) |
JAK2 37 nM (IC50) |
JAK3 1517 nM (IC50) |
Tyk2 36 nM (IC50) |
Blovacitinib (TUL01101, compound 36) (pretreatment for 1 h) inhibits cytokine-induced pSTAT in human whole blood assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Blovacitinib (15 mg/kg; p.o. twice daily for 14 d) inhibits rheumatoid arthritis in collagen-induced arthritis models[1].
Blovacitinib (15 mg/kg; p.o.) exhibits T1/2 of 2.01 h, Cmax of 5105 nM, and oral bioavailability of 38.1% in mice[1].
Blovacitinib (10 mg/kg; p.o.) exhibits T1/2 of 3.06 h, Cmax of 4965 nM, and oral bioavailability of 121% in rats[1].
Blovacitinib (5 mg/kg; p.o.) exhibits T1/2 of 4.49 h, Cmax of 2750 nM, and oral bioavailability of 106.5% in dogs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat adjuvant-induced arthritis (AIA) model[1]
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Dosage:1, 3, 10, 30 mg/kg
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Administration:Orally administered twice daily for 14 days
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Result:Decreased the incidence in a dose-dependent manner.
Chemical Information
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CAS No. 2411222-97-2
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Appearance Solid
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분자량 429.46
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화학식 C22H25F2N5O2
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Color White to off-white
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SMILES
O=C(NC1=NN2C(C=CC=C2C3CCC4(CC3)CN(C4)C([C@@H]5CC5(F)F)=O)=N1)C6CC6
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Synonyms
TUL01101
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
용액&용해도
DMSO : ≥ 200 mg/mL (465.70 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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)
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 (5.82 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.82 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). 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 | 2.3285 mL | 11.6425 mL | 23.2851 mL | 58.2126 mL |
| 5 mM | 0.4657 mL | 2.3285 mL | 4.6570 mL | 11.6425 mL | |
| 10 mM | 0.2329 mL | 1.1643 mL | 2.3285 mL | 5.8213 mL | |
| 15 mM | 0.1552 mL | 0.7762 mL | 1.5523 mL | 3.8808 mL | |
| 20 mM | 0.1164 mL | 0.5821 mL | 1.1643 mL | 2.9106 mL | |
| 25 mM | 0.0931 mL | 0.4657 mL | 0.9314 mL | 2.3285 mL | |
| 30 mM | 0.0776 mL | 0.3881 mL | 0.7762 mL | 1.9404 mL | |
| 40 mM | 0.0582 mL | 0.2911 mL | 0.5821 mL | 1.4553 mL | |
| 50 mM | 0.0466 mL | 0.2329 mL | 0.4657 mL | 1.1643 mL | |
| 60 mM | 0.0388 mL | 0.1940 mL | 0.3881 mL | 0.9702 mL | |
| 80 mM | 0.0291 mL | 0.1455 mL | 0.2911 mL | 0.7277 mL | |
| 100 mM | 0.0233 mL | 0.1164 mL | 0.2329 mL | 0.5821 mL |
Blovacitinib Related Classifications
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