2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. JNJ-61803534

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.

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JNJ-61803534 Chemical Structure

JNJ-61803534 Chemical Structure

CAS No. : 1917306-14-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
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Based on 1 publication(s) in Google Scholar

JNJ-61803534 Related Antibodies

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Description

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[1].

IC50 & Target[1]

RORγt

 

In Vitro

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 Related Antibodies
In Vivo

JNJ-61803534 (100 mg/kg, p.o.) inhibits ex vivo stimulated IL-17A production in the blood of mice[1].
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.

Animal Model: Mouse collagen-induced arthritis (CIA) model[1]
Dosage: 3-100 mg/kg BID or 60 mg/kg QD
Administration: Oral administration (p.o.)
Result: Decreased clinical arthritis scores and hind paw histopathology scores.
Molecular Weight

622.41

Formula

C23H23Cl2F6N3O4S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
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 : 300 mg/mL (482.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6067 mL 8.0333 mL 16.0666 mL
5 mM 0.3213 mL 1.6067 mL 3.2133 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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
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
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JNJ-61803534 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNJ-618035341917306-14-9JNJ61803534JNJ 61803534RORRAR-related orphan receptorCollagen-induced arthritisCIAanti-inflammatoryTh17CD4+ T cellIL-17AInhibitorinhibitorinhibit

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