1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. ROR
  3. SR2211

SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.

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

SR2211 Chemical Structure

SR2211 Chemical Structure

CAS No. : 1359164-11-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 151 In-stock
Solution
10 mM * 1 mL in DMSO USD 151 In-stock
Solid
5 mg USD 130 In-stock
10 mg USD 230 In-stock
25 mg USD 350 In-stock
50 mg USD 480 In-stock
100 mg USD 680 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.

IC50 & Target

IC50: ~320 nM (RORγ), Ki: 105 nM (RORγ)[1][2].

Cellular Effect
Cell Line Type Value Description References
CWR22R IC50
10.13 μM
Compound: 1; SR2211
Antiproliferative activity against human 22Rv1 cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay
Antiproliferative activity against human 22Rv1 cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay
[PMID: 34121397]
CWR22R IC50
6.42 μM
Compound: 2; SR2211
Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by celltiter-glo assay
Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by celltiter-glo assay
[PMID: 30964293]
DU-145 IC50
45.69 μM
Compound: 2; SR2211
Antiproliferative activity against human DU145 cells measured after 72 hrs by celltiter-glo assay
Antiproliferative activity against human DU145 cells measured after 72 hrs by celltiter-glo assay
[PMID: 30964293]
HEK293 EC50
320 nM
Compound: 13, SR2211
Agonist activity at RoRc-LBD (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 reporter assay
Agonist activity at RoRc-LBD (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 reporter assay
[PMID: 24502334]
HEK-293T IC50
0.11 μM
Compound: 2; SR2211
Inhibition of Gal4-RORgamma-LBD (180 to 507 residues) (unknown origin) expressed in HEK293T cells after 24 hrs by dual-luciferase reporter assay
Inhibition of Gal4-RORgamma-LBD (180 to 507 residues) (unknown origin) expressed in HEK293T cells after 24 hrs by dual-luciferase reporter assay
[PMID: 27043267]
HEK-293T IC50
320 nM
Compound: SR2211
Inhibition of GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells assessed as suppression of transcriptional activity after 20 hrs
Inhibition of GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells assessed as suppression of transcriptional activity after 20 hrs
10.1039/C3MD00005B
HepG2 IC50
150 nM
Compound: 13, SR2211
Displacement of [3H]T0901317 from human RoRc expressed in HepG2 cells by scintillation proximity binding assay
Displacement of [3H]T0901317 from human RoRc expressed in HepG2 cells by scintillation proximity binding assay
[PMID: 24502334]
LNCaP IC50
5.38 μM
Compound: 1; SR2211
Antiproliferative activity against human LNCaP cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay
Antiproliferative activity against human LNCaP cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay
[PMID: 34121397]
LNCaP IC50
6.79 μM
Compound: 2; SR2211
Antiproliferative activity against human LNCAP cells measured after 96 hrs by celltiter-glo assay
Antiproliferative activity against human LNCAP cells measured after 96 hrs by celltiter-glo assay
[PMID: 30964293]
LNCaP C4-2B IC50
10.06 μM
Compound: 2; SR2211
Antiproliferative activity against human C4-2B cells measured after 96 hrs by celltiter-glo assay
Antiproliferative activity against human C4-2B cells measured after 96 hrs by celltiter-glo assay
[PMID: 30964293]
LNCaP C4-2B IC50
5.38 μM
Compound: 1; SR2211
Antiproliferative activity against human LNCaP C4-2B cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay
Antiproliferative activity against human LNCaP C4-2B cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay
[PMID: 34121397]
PC-3 IC50
24.82 μM
Compound: 2; SR2211
Antiproliferative activity against human PC3 cells measured after 72 hrs by celltiter-glo assay
Antiproliferative activity against human PC3 cells measured after 72 hrs by celltiter-glo assay
[PMID: 30964293]
In Vitro

The treatment of EL4 with SR2211 represses the IL-17 gene expression. Similarly, the expression of IL-23 receptor (Il23r) is significantly inhibited by SR2211. Treatment of EL-4 cells with SR2211 results in significant inhibition of IL-17 intracellular staining as compared to vehicle treated cells[1].

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

Molecular Weight

527.48

Formula

C26H24F7N3O

CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

FC1=C(C2=CC=C(CN3CCN(CC4=CC=NC=C4)CC3)C=C2)C=CC(C(C(F)(F)F)(O)C(F)(F)F)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (189.58 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 1.8958 mL 9.4790 mL 18.9581 mL
5 mM 0.3792 mL 1.8958 mL 3.7916 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
=
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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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)

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

Purity: 99.67%

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 1.8958 mL 9.4790 mL 18.9581 mL 47.3952 mL
5 mM 0.3792 mL 1.8958 mL 3.7916 mL 9.4790 mL
10 mM 0.1896 mL 0.9479 mL 1.8958 mL 4.7395 mL
15 mM 0.1264 mL 0.6319 mL 1.2639 mL 3.1597 mL
20 mM 0.0948 mL 0.4740 mL 0.9479 mL 2.3698 mL
25 mM 0.0758 mL 0.3792 mL 0.7583 mL 1.8958 mL
30 mM 0.0632 mL 0.3160 mL 0.6319 mL 1.5798 mL
40 mM 0.0474 mL 0.2370 mL 0.4740 mL 1.1849 mL
50 mM 0.0379 mL 0.1896 mL 0.3792 mL 0.9479 mL
60 mM 0.0316 mL 0.1580 mL 0.3160 mL 0.7899 mL
80 mM 0.0237 mL 0.1185 mL 0.2370 mL 0.5924 mL
100 mM 0.0190 mL 0.0948 mL 0.1896 mL 0.4740 mL
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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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Product Name:
SR2211
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