[CAS NO. 2101291-07-8]  AZD-0284

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PRODUCTS SPECIFICATIONS [2101291-07-8]

Distributor
Catalog
AS948116
Brand
Arctom Scientific
CAS
2101291-07-8

DESCRIPTION [2101291-07-8]

Overview

MDL-
Molecular Weight524.43
Molecular FormulaC21H18F6N2O5S
SMILESO=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

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

Summary

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]


In Vitro

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

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT03029741 AstraZeneca
Plaque Psoriasis Vulgaris
February 21, 2017 Phase 1
NCT03310320 AstraZeneca
Plaque Psoriasis Vulgaris
November 29, 2017 Phase 1
NCT02976831 AstraZeneca|Parexel
Plaque Psoriasis Vulgaris
December 9, 2016 Phase 1

Appearance

Solid


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)

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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.