2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. RAR/RXR
  4. RXR antagonist 1

RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA2 of 8.06. RXR antagonist 1 can be used for type 2 diabetes research.

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

RXR antagonist 1 Chemical Structure

RXR antagonist 1 Chemical Structure

CAS No. : 3010910-40-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 564 In-stock
Solution
10 mM * 1 mL in DMSO USD 564 In-stock
Solid
5 mg USD 510 In-stock
10 mg USD 815 In-stock
25 mg USD 1630 In-stock
50 mg USD 2610 In-stock
100 mg USD 4180 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

RXR antagonist 1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA2 of 8.06. RXR antagonist 1 can be used for type 2 diabetes research[1].

In Vitro

RXR antagonist 1 (compound 6a) shows potent RXR-antagonistic activities at 1 μM[1].
RXR antagonist 1 shows competitive binding to the LBP in hRXRα-LBD, with Ki of 0.384 ± 0.072, Kd of 0.277 ± 0.038, and Ki/Kd of 1.39[1].
The cell permeability of RXR antagonist 1 shows no correlation with RXR-antagonistic activity[1].

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

RXR antagonist 1 Related Antibodies
Molecular Weight

502.57

Formula

C28H33F3N2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCCCCOC1=CC2=C(C(C)(CCC2(C)C)C)C=C1N3C(C(F)(F)F)=NC4=C3C=CC(C(O)=O)=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 (198.98 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 1.9898 mL 9.9489 mL 19.8977 mL
5 mM 0.3980 mL 1.9898 mL 3.9795 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 (4.97 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 (4.97 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 1.9898 mL 9.9489 mL 19.8977 mL 49.7443 mL
5 mM 0.3980 mL 1.9898 mL 3.9795 mL 9.9489 mL
10 mM 0.1990 mL 0.9949 mL 1.9898 mL 4.9744 mL
15 mM 0.1327 mL 0.6633 mL 1.3265 mL 3.3163 mL
20 mM 0.0995 mL 0.4974 mL 0.9949 mL 2.4872 mL
25 mM 0.0796 mL 0.3980 mL 0.7959 mL 1.9898 mL
30 mM 0.0663 mL 0.3316 mL 0.6633 mL 1.6581 mL
40 mM 0.0497 mL 0.2487 mL 0.4974 mL 1.2436 mL
50 mM 0.0398 mL 0.1990 mL 0.3980 mL 0.9949 mL
60 mM 0.0332 mL 0.1658 mL 0.3316 mL 0.8291 mL
80 mM 0.0249 mL 0.1244 mL 0.2487 mL 0.6218 mL
100 mM 0.0199 mL 0.0995 mL 0.1990 mL 0.4974 mL
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RXR antagonist 1 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:

RXR antagonist 13010910-40-1RXR antagonist1RXR antagonist-1RAR/RXRRetinoic acid receptorsRetinoid X receptorsType 2 diabetesRXR-antagonistic activitiesInhibitorinhibitorinhibit

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