2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. REV-ERB
  4. SR12418

SR12418 is a REV-ERB-specific synthetic ligand with IC50s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research.

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

SR12418 Chemical Structure

SR12418 Chemical Structure

CAS No. : 1801185-08-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

SR12418 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SR12418 is a REV-ERB-specific synthetic ligand with IC50s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research[1][2].

IC50 & Target

IC50: 68 nM (REV-ERBα) and 119 nM (REV-ERBβ)[1]
In Vitro

SR12418 (5 μM; 96 h) inhibits the growth of TH17 cells[1].
SR12418 (5 and 10 μM; 4 d) inhibits cell differentiation under TH17 polarizing conditions[1].

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

SR12418 Related Antibodies

RT-PCR[1]

Cell Line: TH17 cells
Concentration: 5 μM
Incubation Time: 96 hours
Result: Repressed TH17-mediated gene expression and Nfil3.

Cell Differentiation Assay[1]

Cell Line: Mouse CD4+ T cells
Concentration: 5 and 10 μM
Incubation Time: 4 days
Result: Inhibited TH17 cell differentiation in a dose-dependent manner.
In Vivo

SR12418 (intraperitoneal injection; 50 mg/kg; twice a day) suppresses the development and severity of experimental autoimmune encephalomyelitis[1].
SR12418 (intraperitoneal injection; 50 mg/kg; twice a day; begin at day 18 post-immunization) shows effects in intervention studies of relapsing-remitting experimental autoimmune encephalomyelitis[1].

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

Animal Model: C57BL/6 mice inducing experimental autoimmune encephalomyelitis (EAE)[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; 50 mg/kg; twice a day
Result: Diminished the incidence of disease with approximately 20% mice developing disease.
Showed no overt signs of toxicity.
Animal Model: PLP139-151-induced relapsing-remitting EAE (R-EAE) in SJL/J mice[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; 50 mg/kg; twice a day; begin at day 18 post-immunization
Result: Resulted in a significant reduction in the relapse severity compared to the vehicle control.
Showed a significant decrease in the frequency and number of CD4+ and CD8+ effector cells (CD44hi).
Molecular Weight

483.57

Formula

C31H30FNO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CC2=C(C=C(F)C=C2)C[C@H]1COC3=CC=C(OC(C)(C)C)C=C3)C4=C5C=CC=CC5=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (206.80 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 2.0680 mL 10.3398 mL 20.6795 mL
5 mM 0.4136 mL 2.0680 mL 4.1359 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.17 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: 2.5 mg/mL (5.17 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. 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
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 2.0680 mL 10.3398 mL 20.6795 mL 51.6988 mL
5 mM 0.4136 mL 2.0680 mL 4.1359 mL 10.3398 mL
10 mM 0.2068 mL 1.0340 mL 2.0680 mL 5.1699 mL
15 mM 0.1379 mL 0.6893 mL 1.3786 mL 3.4466 mL
20 mM 0.1034 mL 0.5170 mL 1.0340 mL 2.5849 mL
25 mM 0.0827 mL 0.4136 mL 0.8272 mL 2.0680 mL
30 mM 0.0689 mL 0.3447 mL 0.6893 mL 1.7233 mL
40 mM 0.0517 mL 0.2585 mL 0.5170 mL 1.2925 mL
50 mM 0.0414 mL 0.2068 mL 0.4136 mL 1.0340 mL
60 mM 0.0345 mL 0.1723 mL 0.3447 mL 0.8616 mL
80 mM 0.0258 mL 0.1292 mL 0.2585 mL 0.6462 mL
100 mM 0.0207 mL 0.1034 mL 0.2068 mL 0.5170 mL
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SR12418 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:

SR124181801185-08-9SR 12418SR-12418REV-ERBexperimental autoimmune encephalomyelitisEAEcolitisMouse CD4+ TTH17Inhibitorinhibitorinhibit

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