2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Autophagy
  3. RAR/RXR Autophagy
  4. AGN 205728

AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/ 0.

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

AGN 205728 Chemical Structure

AGN 205728 Chemical Structure

CAS No. : 859498-05-8

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Customer Review

Based on 1 publication(s) in Google Scholar

AGN 205728 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/ 0.6 nM; no inhibiton on RARα and RARβ. IC50 value: 3 nM/ 0.6 nM(Ki/IC95) Target: RARγ antagonist More information can be found in the following patent, Compound 7a. Preparation of disubstituted chalcone oximes having RARγ retinoid receptor antagonist activity By Tsang, Kwok Yin; Sinha, Santosh; Liu, Xiaoxia; Bhat, Smita; Chandraratna, Roshantha A. From PCT Int. Appl. (2005), WO 2005066115 A2 20050721.

Molecular Weight

437.53

Formula

C29H27NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C=C1)=CC=C1C2=CCC(C)(C)C3=C2C=CC(C(/C=C/C4=CC=C(C(O)=O)C=C4)=N/O)=C3
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 (228.56 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 2.2856 mL 11.4278 mL 22.8556 mL
5 mM 0.4571 mL 2.2856 mL 4.5711 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 (5.71 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: 98.62%

SDS (251 KB)

COA (250 KB) HNMR (263 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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 2.2856 mL 11.4278 mL 22.8556 mL 57.1389 mL
5 mM 0.4571 mL 2.2856 mL 4.5711 mL 11.4278 mL
10 mM 0.2286 mL 1.1428 mL 2.2856 mL 5.7139 mL
15 mM 0.1524 mL 0.7619 mL 1.5237 mL 3.8093 mL
20 mM 0.1143 mL 0.5714 mL 1.1428 mL 2.8569 mL
25 mM 0.0914 mL 0.4571 mL 0.9142 mL 2.2856 mL
30 mM 0.0762 mL 0.3809 mL 0.7619 mL 1.9046 mL
40 mM 0.0571 mL 0.2857 mL 0.5714 mL 1.4285 mL
50 mM 0.0457 mL 0.2286 mL 0.4571 mL 1.1428 mL
60 mM 0.0381 mL 0.1905 mL 0.3809 mL 0.9523 mL
80 mM 0.0286 mL 0.1428 mL 0.2857 mL 0.7142 mL
100 mM 0.0229 mL 0.1143 mL 0.2286 mL 0.5714 mL
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AGN 205728 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:

AGN 205728859498-05-8AGN205728AGN-205728RAR/RXRAutophagyRetinoic acid receptorsRetinoid X receptorsInhibitorinhibitorinhibit

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