JNJ-61803534
Based on 1 Customer Validation
JNJ-61803534 is a potent and orally active RORγt inverse agonist with an IC50 of 9.6 nM. JNJ-61803534 has anti-inflammatory activity. JNJ-61803534 inhibits IL-17A production in human CD4+ T cells under Th17 differentiation conditions.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 1917306-14-9
- Formula: C23H23Cl2F6N3O4S
- Molecular Weight:622.41
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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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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RORγt |
JNJ-61803534 inhibits RORγt transcription in HEK-293 T cells transfected with vectors encoding RORγt, with an IC50 of 9.6 nM[1].
JNJ-61803534 (1 nM-1 μM) inhibits IL-17A, IL-17F IFNγ and IL-22 production in CD4+ T cells isolated from human blood[1].
JNJ-61803534 does not impact in vitro Treg differentiation in CD4+ T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
JNJ-61803534 (3-100 mg/kg BID or 60 mg/kg QD, p.o.) alleviates inflammation, cartilage damage, bone destruction in mouse collagen-induced arthritis (CIA) model[1].
JNJ-61803534 (30 and 100 mg/kg, p.o.) alleviates Imiquimod (HY-B0180)-induced dermal psoriatic-like inflammation in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse collagen-induced arthritis (CIA) model[1]
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Dosage:3-100 mg/kg BID or 60 mg/kg QD
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Administration:Oral administration (p.o.)
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Result:Decreased clinical arthritis scores and hind paw histopathology scores.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1917306-14-9
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Appearance Solid
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Molecular Weight 622.41
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Formula C23H23Cl2F6N3O4S
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Color White to off-white
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SMILES
O=C(C1=NC(C(N2[C@H](C)CCC2)=O)=C(C3=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C(Cl)=C3Cl)S1)NCC(C)(O)C
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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
DMSO : 300 mg/mL (482.00 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)
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: ≥ 2.08 mg/mL (3.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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. 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 | 1.6067 mL | 8.0333 mL | 16.0666 mL | 40.1665 mL |
| 5 mM | 0.3213 mL | 1.6067 mL | 3.2133 mL | 8.0333 mL | |
| 10 mM | 0.1607 mL | 0.8033 mL | 1.6067 mL | 4.0166 mL | |
| 15 mM | 0.1071 mL | 0.5356 mL | 1.0711 mL | 2.6778 mL | |
| 20 mM | 0.0803 mL | 0.4017 mL | 0.8033 mL | 2.0083 mL | |
| 25 mM | 0.0643 mL | 0.3213 mL | 0.6427 mL | 1.6067 mL | |
| 30 mM | 0.0536 mL | 0.2678 mL | 0.5356 mL | 1.3389 mL | |
| 40 mM | 0.0402 mL | 0.2008 mL | 0.4017 mL | 1.0042 mL | |
| 50 mM | 0.0321 mL | 0.1607 mL | 0.3213 mL | 0.8033 mL | |
| 60 mM | 0.0268 mL | 0.1339 mL | 0.2678 mL | 0.6694 mL | |
| 80 mM | 0.0201 mL | 0.1004 mL | 0.2008 mL | 0.5021 mL | |
| 100 mM | 0.0161 mL | 0.0803 mL | 0.1607 mL | 0.4017 mL |
JNJ-61803534 Related Classifications
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