RORγt Inverse agonist 10

Name: RORγt Inverse agonist 10
Brand: MedChemExpress
SKU: HY-133552
Rating: 4.5 (1 reviews)

Cat. No.: HY-133552 Purity: 99.13%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

For research use only. We do not sell to patients.

RORγt Inverse agonist 10 Chemical Structure

CAS No. : 2413986-35-1

Size	Price	Stock	Quantity
1 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1100	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2250	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3500	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 5600	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

RORγt

51 nM (IC₅₀)

In Vitro

RORγt Inverse agonist 10 has a good liver microsome stability (human CL_int=0.010 mL/min/mg, mouse CL_int=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 t_1/2 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, t_1/2=3.6 hours.

Molecular Weight

572.50

Formula

C₂₅H₂₆F₆N₆O₃

CAS No.

2413986-35-1

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
10 mM	0.1747 mL	0.8734 mL	1.7467 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 10 mg/mL (17.47 mM); Clear solution

This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.13%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (248 KB) HNMR (284 KB) RP-HPLC (265 KB) MS (70 KB)

Handling Instructions (2659 KB)

References

[1]. Ryota Nakajima, et al. Discovery of [1,2,4]Triazolo[1,5- a]pyridine Derivatives as Potent and Orally Bioavailable RORγt Inverse Agonists. ACS Med Chem Lett. 2020 Feb 27;11(4):528-534. [Content Brief]

Complete Stock Solution Preparation Table

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