Glucocorticoid receptor agonist

Name: Glucocorticoid receptor agonist
Brand: MedChemExpress
SKU: HY-14234
Rating: 4.5 (1 reviews)

Cat. No.: HY-14234 Purity: 99.56%: FAQs
Data Sheet SDS COA Handling Instructions

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Glucocorticoid receptor agonist is a Glucocorticoid receptor agonist that acts on Glucocorticoid receptor (GR), progesterone receptor (PR) and mineralocorticoid receptor (MR) with the IC₅₀ values of 2.1 , 1200 and 210 nM, respectively. Glucocorticoid receptor agonist has steroid-like anti-inflammatory properties and may be used to improve metabolism and reduce increased levels of body fat and serum insulin.

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

Glucocorticoid receptor agonist Chemical Structure

CAS No. : 1245526-82-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 330	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 330	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1500	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE Glucocorticoid receptor agonist

•Patent. US20220047602A1.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

In Vitro

Glucocorticoid receptor agonist ((R)-16) has effect on IL-6 and MMTV with the IC₅₀ values of 3.3 and 80 nM, respectively, also has effect on aromatase with the EC₅₀ value of 11 nM^[1].

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

In Vivo

Glucocorticoid receptor agonist ((R)-16) exhibits good pharmacokinetic properties in Sprague-Dawley rats^[1].
Glucocorticoid receptor agonist ((R)-16) (30 and 10 mg/kg, p.o., daily, 5 weeks) can reduce the increased levels of body fat and serum insulin and shows an effective inhibition of TNF-α production in LPS-stimulated mouse model^[1].
The pharmacokinetic parameters of Glucocorticoid receptor agonist ((R)-16) in Sprague-Dawley rat (5 mg/kg i.v. or 30 mg/kg p.o.)^[1].

Parameters	Cl (i.v.)(mL/min/kg)	V_SS(iv) (L/kg)	T_1/2(iv)(h)	C_max(po) (ng/mL)	AUC_inf(po) (h·ng/mL)	F(po)%
(R)-16	49	7.6	1.85	509	4879	48

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

Molecular Weight

396.38

Formula

C₂₀H₂₀F₄N₂O₂

CAS No.

1245526-82-2

Appearance

Solid

Color

White to yellow

SMILES

OC1=CC=C(C=C1C(C)(C[C@](O)(C(F)(F)F)CC2=CC3=C(C=NC=C3)N2)C)F

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 : ≥ 100 mg/mL (252.28 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	2.5228 mL	12.6142 mL	25.2283 mL
5 mM	0.5046 mL	2.5228 mL	5.0457 mL
10 mM	0.2523 mL	1.2614 mL	2.5228 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.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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 (6.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.31 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)

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: 99.56%

Select Batch:

Data Sheet (276 KB) SDS (0 KB)

COA (250 KB) LCMS (111 KB)

Handling Instructions (2659 KB)

References

[1]. Doris Riether, et al. Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics. J Med Chem. 2010 Sep 23;53(18):6681-98. [Content Brief]

Animal Administration

Animal administration [1] Female Balb/c mice weighing approximately 20 g were used. Mice were administered the test compound and in Cremophor (po) approximately 60 min prior to LPS/D-gal administration. The volume of oral gavage was 0.15 mL. Then mice were administered LPS (E. coli LPS 055:85, 1.0 μg/mouse) plus D-gal (50 mg/kg) intravenously in 0.2 mL of pyrogen-free saline. One hour after LPS/D-gal, each mouse was anesthetized, bled by cardiac puncture, and collected for serum TNF-R and compound levels. Blood samples were centrifuged at 2500 rpm for 10-15 min, the serum was decanted, and samples were stored frozen at -70°C until transfer either for TNF-R determination or to Drug Metabolism and Pharmacokinetics for plasma concentration analysis by HPLC. The concentration of TNF-R in the serum was measured by a commercially available ELISA kit. ELISA was performed. All samples are assayed in duplicate.

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

References

[1]. Doris Riether, et al. Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics. J Med Chem. 2010 Sep 23;53(18):6681-98. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5228 mL	12.6142 mL	25.2283 mL	63.0708 mL
	5 mM	0.5046 mL	2.5228 mL	5.0457 mL	12.6142 mL
	10 mM	0.2523 mL	1.2614 mL	2.5228 mL	6.3071 mL
	15 mM	0.1682 mL	0.8409 mL	1.6819 mL	4.2047 mL
	20 mM	0.1261 mL	0.6307 mL	1.2614 mL	3.1535 mL
	25 mM	0.1009 mL	0.5046 mL	1.0091 mL	2.5228 mL
	30 mM	0.0841 mL	0.4205 mL	0.8409 mL	2.1024 mL
	40 mM	0.0631 mL	0.3154 mL	0.6307 mL	1.5768 mL
	50 mM	0.0505 mL	0.2523 mL	0.5046 mL	1.2614 mL
	60 mM	0.0420 mL	0.2102 mL	0.4205 mL	1.0512 mL
	80 mM	0.0315 mL	0.1577 mL	0.3154 mL	0.7884 mL
	100 mM	0.0252 mL	0.1261 mL	0.2523 mL	0.6307 mL