2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. REV-ERB ROR
  4. SR1001

SR1001 is a selective RORα and RORγt inverse agonist with Kis 172 and 111 nM, respectively.

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

SR1001 Chemical Structure

SR1001 Chemical Structure

CAS No. : 1335106-03-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 106 In-stock
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Solid
5 mg USD 96 In-stock
10 mg USD 180 In-stock
50 mg USD 640 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

SR1001 Related Antibodies

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RORγ RORα RORβ

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

SR1001 is a selective RORα and RORγt inverse agonist with Kis 172 and 111 nM, respectively.

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
4 μM
Compound: SR1001
Inverse agonist activity at GAL4-fused ROR alpha (unknown origin) expressed in HEK293 cells assessed as inhibition of transcriptional activity after 24 hrs by luciferase reporter gene assay
Inverse agonist activity at GAL4-fused ROR alpha (unknown origin) expressed in HEK293 cells assessed as inhibition of transcriptional activity after 24 hrs by luciferase reporter gene assay
10.1039/C3MD00005B
HEK293 EC50
4 μM
Compound: SR1001
Inverse agonist activity at GAL4-fused ROR gamma (unknown origin) expressed in HEK293 cells assessed as inhibition of transcriptional activity after 24 hrs by luciferase reporter gene assay
Inverse agonist activity at GAL4-fused ROR gamma (unknown origin) expressed in HEK293 cells assessed as inhibition of transcriptional activity after 24 hrs by luciferase reporter gene assay
10.1039/C3MD00005B
In Vitro

SR1001 inhibits the development of murine TH17 cells by inhibition of IL-17A gene expression and protein production. SR1001 reduces the interaction of a coactivator TRAP220 NR box 2 peptide with RORγ in a dose dependent manner (IC50 value≈117 nM). Additionally, SR1001 inhibits the expression of cytokines when added to differentiated murine or human TH17 cells[1].

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

SR1001 Related Antibodies
In Vivo

SR1001 effectively suppresses the clinical severity of autoimmune disease in mice. Administration of SR1001 to C57BL/6 mice suppresses the expression of hepatic ROR target genes, Cyp7b1, Rev-erbα, and Serpine 1[1]. SR1001 a RORα inverse agonist eliminats the circadian pattern of expression of citrate synthase mRNA in mice[2].

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

477.40

Formula

C15H13F6N3O4S2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CC(NC1=NC(C)=C(S(=O)(NC2=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C=C2)=O)S1)=O
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 : ≥ 39 mg/mL (81.69 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 2.0947 mL 10.4734 mL 20.9468 mL
5 mM 0.4189 mL 2.0947 mL 4.1894 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.

  • 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: ≥ 2.08 mg/mL (4.36 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 (4.36 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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

Purity: 99.89%

SDS (392 KB)

COA (255 KB) HNMR (257 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

HEK293 cells are plated in 96-well plates at a density of 15 x 103 cells/well. Transfections are performed using Lipofectamine 2000. 24 h post-transfection, the cells are treated with vehicle or compound (SR1001). 24 h post-treatment, the luciferase activity is measured using the Dual-Glo luciferase assay system[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Experimental autoimmune encephalomyelitis is induced in C57BL/6 wild-type mice by s.c. injection over four sites in the flank with 200 μg per mouse. The SR1001 is dissolved in DMSO at 25 mg/mL and the mice are treated (i.p.) with 25 mg/kg SR1001 (1 μL/g body weight of mouse) or vehicle (DMSO, 1 μL/g body weight of mouse) twice per day. The treatment is started 2 days before immunization and continued until the end of experiment[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
DMSO 1 mM 2.0947 mL 10.4734 mL 20.9468 mL 52.3670 mL
5 mM 0.4189 mL 2.0947 mL 4.1894 mL 10.4734 mL
10 mM 0.2095 mL 1.0473 mL 2.0947 mL 5.2367 mL
15 mM 0.1396 mL 0.6982 mL 1.3965 mL 3.4911 mL
20 mM 0.1047 mL 0.5237 mL 1.0473 mL 2.6183 mL
25 mM 0.0838 mL 0.4189 mL 0.8379 mL 2.0947 mL
30 mM 0.0698 mL 0.3491 mL 0.6982 mL 1.7456 mL
40 mM 0.0524 mL 0.2618 mL 0.5237 mL 1.3092 mL
50 mM 0.0419 mL 0.2095 mL 0.4189 mL 1.0473 mL
60 mM 0.0349 mL 0.1746 mL 0.3491 mL 0.8728 mL
80 mM 0.0262 mL 0.1309 mL 0.2618 mL 0.6546 mL
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SR1001 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:

SR10011335106-03-0SR 1001SR-1001REV-ERBRORRAR-related orphan receptorInhibitorinhibitorinhibit

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