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  3. RORγt Inverse agonist 10

RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R

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RORγt Inverse agonist 10 Chemical Structure

RORγt Inverse agonist 10 Chemical Structure

CAS No. : 2413986-35-1

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Description

RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R[1]

IC50 & Target[1]

RORγt

51 nM (IC50)

In Vitro

RORγt Inverse agonist 10 has a good liver microsome stability (human CLint=0.010 mL/min/mg, mouse CLint=0.030 mL/min/mg)[1].
RORγt Inverse agonist 10 suppresses the IL-17A production in a dose-dependent manner with an IC50 of 130 nM in a human whole-blood assay[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

RORγt Inverse agonist 10 (3-100 mg/kg; p.o.) shows robust and dose-dependent inhibitory effect on the IL-17A production in mouse IL-18/23-induced cytokine expression model[1].
RORγt Inverse agonist 10 (1.145 mg/kg; p.o.) shows a high AUC of 15000 nM*h and t1/2 of 3.6 hours[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57/BL6 male mice, mouse IL-18/23-induced cytokine expression model[1]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration: Oral administration
Result: Significantly inhibited the IL-17A production in a dose-dependent manner.
Animal Model: Mice[1]
Dosage: 1.145 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration
Result: AUC=15000 nM*h, t1/2=3.6 hours.
Molecular Weight

572.50

Formula

C25H26F6N6O3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

C[C@H](N(C(CC(C(F)(F)F)C(F)(F)F)=O)CC1)C[C@H]1OC2=C(C)C(NC(C3=CN=C(C)C=C3)=O)=CN4C2=NC=N4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (174.67 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7467 mL 8.7336 mL 17.4672 mL
5 mM 0.3493 mL 1.7467 mL 3.4934 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 (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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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: ≥ 10 mg/mL (17.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 10 mg/mL (17.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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 (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
DMSO 1 mM 1.7467 mL 8.7336 mL 17.4672 mL 43.6681 mL
5 mM 0.3493 mL 1.7467 mL 3.4934 mL 8.7336 mL
10 mM 0.1747 mL 0.8734 mL 1.7467 mL 4.3668 mL
15 mM 0.1164 mL 0.5822 mL 1.1645 mL 2.9112 mL
20 mM 0.0873 mL 0.4367 mL 0.8734 mL 2.1834 mL
25 mM 0.0699 mL 0.3493 mL 0.6987 mL 1.7467 mL
30 mM 0.0582 mL 0.2911 mL 0.5822 mL 1.4556 mL
40 mM 0.0437 mL 0.2183 mL 0.4367 mL 1.0917 mL
50 mM 0.0349 mL 0.1747 mL 0.3493 mL 0.8734 mL
60 mM 0.0291 mL 0.1456 mL 0.2911 mL 0.7278 mL
80 mM 0.0218 mL 0.1092 mL 0.2183 mL 0.5459 mL
100 mM 0.0175 mL 0.0873 mL 0.1747 mL 0.4367 mL
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RORγt Inverse agonist 10 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.

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RORγt Inverse agonist 10
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