AZD-0284

Name: AZD-0284
Brand: MedChemExpress
SKU: HY-120384
Rating: 5.0 (2 reviews)

Cat. No.: HY-120384 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment.

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

AZD-0284 Chemical Structure

CAS No. : 2101291-07-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 323	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 323	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 940	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1250	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE AZD-0284

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RORγ RORα RORβ

Biological Activity
Purity & Documentation
References
Customer Review

Description

AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment^[1].

IC₅₀ & Target

pIC50: 7.4 (FRET RORγ)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Thymocyte	IC₅₀	229 nM Compound: 20	Apoptosis in C57BL/6NCrl mouse thymocytes assessed as survival incubated for 26 hrs by AnnexinV staining based by flow cytometry Apoptosis in C57BL/6NCrl mouse thymocytes assessed as survival incubated for 26 hrs by AnnexinV staining based by flow cytometry	[PMID: 34464130]

In Vitro

AZD0284 (0.37 μM; 5 days) inhibits IL-17A production in human T_H17 cells^[1].
AZD0284 reduces polarization of T_H17 into pathogenic T_H17/1 cells. AZD0284 decreases frequency of single IL-17⁺cell as well as double positive T_H17/1 cells. AZD0284 reduces IL-17A secretion and RNA expression of IL-17A, IL-17F, IL-22 and IL-23R^[1]^[2].

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

Clinical Trial

Molecular Weight

524.43

Formula

C₂₁H₁₈F₆N₂O₅S

CAS No.

2101291-07-8

Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H]1N(C(C)=O)CC2=C1C=CC(S(=O)(C)=O)=C2)NC3=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (190.68 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	1.9068 mL	9.5342 mL	19.0683 mL
5 mM	0.3814 mL	1.9068 mL	3.8137 mL
10 mM	0.1907 mL	0.9534 mL	1.9068 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 (stored under nitrogen). 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 0.83 mg/mL (1.58 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (1.58 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (1.58 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 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 (8.3 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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: 99.90%

Select Batch:

Data Sheet (280 KB) SDS (251 KB)

COA (258 KB) LCMS (270 KB)

Handling Instructions (2659 KB)

References

[1]. Narjes, F, et al. The discovery of AZD0284, an inverse agonist of the nuclear receptor RORg. American Chemical Society, 2017 Drug Design and Delivery Symposium 26 October 2017

[2]. Asimus S, et al. Pharmacokinetics, pharmacodynamics and safety of the inverse retinoic acid-related orphan receptor γ agonist AZD0284 [published online ahead of print, 2020 Feb 17]. Br J Clin Pharmacol. 2020;10.1111/bcp.14253. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9068 mL	9.5342 mL	19.0683 mL	47.6708 mL
	5 mM	0.3814 mL	1.9068 mL	3.8137 mL	9.5342 mL
	10 mM	0.1907 mL	0.9534 mL	1.9068 mL	4.7671 mL
	15 mM	0.1271 mL	0.6356 mL	1.2712 mL	3.1781 mL
	20 mM	0.0953 mL	0.4767 mL	0.9534 mL	2.3835 mL
	25 mM	0.0763 mL	0.3814 mL	0.7627 mL	1.9068 mL
	30 mM	0.0636 mL	0.3178 mL	0.6356 mL	1.5890 mL
	40 mM	0.0477 mL	0.2384 mL	0.4767 mL	1.1918 mL
	50 mM	0.0381 mL	0.1907 mL	0.3814 mL	0.9534 mL
	60 mM	0.0318 mL	0.1589 mL	0.3178 mL	0.7945 mL
	80 mM	0.0238 mL	0.1192 mL	0.2384 mL	0.5959 mL
	100 mM	0.0191 mL	0.0953 mL	0.1907 mL	0.4767 mL

AZD-0284 Related Classifications

Inflammation/Immunology

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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AZD-0284

Customer Review

AZD-0284 Related Antibodies

2 Publications Citing Use of MCE AZD-0284

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All ROR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

AZD-0284 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AZD-0284 Related Classifications

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Customer Review

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