1. Immunology/Inflammation Vitamin D Related/Nuclear Receptor Antibody-drug Conjugate/ADC Related
  2. Glucocorticoid Receptor ADC Cytotoxin
  3. Glucocorticoid receptor agonist-1

Glucocorticoid receptor agonist-1 

Cat. No.: HY-131974 Purity: 99.80%
COA Handling Instructions

Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM extracted from patent WO2017210471A1, compound 41.

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

Glucocorticoid receptor agonist-1 Chemical Structure

Glucocorticoid receptor agonist-1 Chemical Structure

CAS No. : 2166375-82-0

Size Price Stock Quantity
5 mg USD 670 In-stock
10 mg USD 940 In-stock
25 mg USD 1480 In-stock
50 mg USD 1995 In-stock
100 mg USD 2690 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM extracted from patent WO2017210471A1, compound 41[1].

IC50 & Target

IC50: 2.8 nM (Glucocorticoid receptor)[1]

In Vitro

Glucocorticoid receptor agonist immunoconjugates are useful for treating autoimmune diseases such as, but not limited to, rheumatoid arthritis, juvenile idiopathic arthritis, psoriatic arthritis, ankylosing spondylitis, adult Crohn's disease, pediatric Crohn's disease, ulcerative colitis, plaque psoriasis, hidradenitis suppurativa, uveitis, Behcets disease, a spondyloarthropathy, or psoriasis[1].

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

Molecular Weight

569.69

Formula

C35H39NO6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OCC([C@]12[C@@]3([C@@]([C@@]4([H])[C@]([C@@]5(C(CC4)=CC(C=C5)=O)C)([H])[C@H](C3)O)([H])C[C@@]1([H])O[C@](C6=CC=C(C=C6)CC7=CC(N)=CC=C7)([H])O2)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (175.53 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 1.7553 mL 8.7767 mL 17.5534 mL
5 mM 0.3511 mL 1.7553 mL 3.5107 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 (protect from light). 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 (4.39 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.80%

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 (protect from light). 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 1.7553 mL 8.7767 mL 17.5534 mL 43.8835 mL
5 mM 0.3511 mL 1.7553 mL 3.5107 mL 8.7767 mL
10 mM 0.1755 mL 0.8777 mL 1.7553 mL 4.3884 mL
15 mM 0.1170 mL 0.5851 mL 1.1702 mL 2.9256 mL
20 mM 0.0878 mL 0.4388 mL 0.8777 mL 2.1942 mL
25 mM 0.0702 mL 0.3511 mL 0.7021 mL 1.7553 mL
30 mM 0.0585 mL 0.2926 mL 0.5851 mL 1.4628 mL
40 mM 0.0439 mL 0.2194 mL 0.4388 mL 1.0971 mL
50 mM 0.0351 mL 0.1755 mL 0.3511 mL 0.8777 mL
60 mM 0.0293 mL 0.1463 mL 0.2926 mL 0.7314 mL
80 mM 0.0219 mL 0.1097 mL 0.2194 mL 0.5485 mL
100 mM 0.0176 mL 0.0878 mL 0.1755 mL 0.4388 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:
Glucocorticoid receptor agonist-1
Cat. No.:
HY-131974
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