2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. Cintirorgon

Cintirorgon  (Synonyms: LYC-55716)

Cat. No.: HY-104037 Purity: 98.53%
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Cintirorgon (LYC-55716) est un agoniste de RORγ premier de sa catégorie, sélectif et biodisponible par voie orale. Cintirorgon (LYC-55716) module l'expression génique des cellules immunitaires des lymphocytes T exprimant RORγ, ce qui entraîne une fonction effectrice améliorée, ainsi qu'une diminution de l'immunosuppression, entraînant une diminution de la croissance tumorale et une amélioration de la survie.

Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.

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

Cintirorgon Chemical Structure

Cintirorgon Chemical Structure

CAS No. : 2055536-64-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 263 In-stock
Solution
10 mM * 1 mL in DMSO USD 263 In-stock
Solid
1 mg USD 99 In-stock
5 mg USD 198 In-stock
10 mg USD 275 In-stock
50 mg USD 869 In-stock
100 mg USD 1540 In-stock
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Based on 7 publication(s) in Google Scholar

Other Forms of Cintirorgon:

Cintirorgon Related Antibodies

Top Publications Citing Use of Products

View All ROR Isoform Specific Products:

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RORγ RORα RORβ

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Description

Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival[1][2].

IC50 & Target

RORγ[1]
In Vivo

Upon oral administration of RORγ agonist Cintirorgon (LYC-55716), this agent selectively binds to the nuclear receptor transcription factor RORγ, forming a receptor complex that translocates to the nucleus, and binds to ROR response elements (ROREs), enhancing the function, proliferation and survival of type 17 T cells, including Th17 (helper T cells) and Tc17 (cytotoxic T cells). RORγ, the nuclear receptor transcription factor that is involved in Th17/Tc17 differentiation, plays a key role in immune activation. Cintirorgon (LYC-55716) is also orally bioavailable, while the new generation of immuno-oncology drugs-ncluding PD-1/PD-L1 inhibitors are delivered by injection[1].

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

603.53

Formula

C27H23F6NO6S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C(C)(C)C[C@@H]1OC2=CC=C(C3=CC(F)=CC(OC(F)F)=C3)C=C2N(S(=O)(C4=CC=CC(C(F)(F)F)=C4)=O)C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 113.3 mg/mL (187.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (165.69 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6569 mL 8.2846 mL 16.5692 mL
5 mM 0.3314 mL 1.6569 mL 3.3138 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.6569 mL 8.2846 mL 16.5692 mL 41.4230 mL
5 mM 0.3314 mL 1.6569 mL 3.3138 mL 8.2846 mL
10 mM 0.1657 mL 0.8285 mL 1.6569 mL 4.1423 mL
15 mM 0.1105 mL 0.5523 mL 1.1046 mL 2.7615 mL
20 mM 0.0828 mL 0.4142 mL 0.8285 mL 2.0711 mL
25 mM 0.0663 mL 0.3314 mL 0.6628 mL 1.6569 mL
30 mM 0.0552 mL 0.2762 mL 0.5523 mL 1.3808 mL
40 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0356 mL
50 mM 0.0331 mL 0.1657 mL 0.3314 mL 0.8285 mL
60 mM 0.0276 mL 0.1381 mL 0.2762 mL 0.6904 mL
80 mM 0.0207 mL 0.1036 mL 0.2071 mL 0.5178 mL
100 mM 0.0166 mL 0.0828 mL 0.1657 mL 0.4142 mL
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Cintirorgon 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:

Cintirorgon2055536-64-4LYC-55716LYC55716LYC 55716RORRAR-related orphan receptorInhibitorinhibitorinhibit

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