1. Immunology/Inflammation Membrane Transporter/Ion Channel
  2. NOD-like Receptor (NLR) Interleukin Related Potassium Channel
  3. AZD4144

AZD4144 is an orally active NLRP3 inhibitor (EC50: 0.082 μM). AZD4144 effectively inhibits the release of IL-1β when NLRP3 is overactivated, exerting an anti-inflammatory effect. AZD4144 has low inhibitory effect on hERG and low cardiotoxicity. AZD4144 has the potential to study diseases and conditions associated with NLRP3 inflammasome activation.

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

AZD4144 Chemical Structure

AZD4144 Chemical Structure

CAS No. : 2890191-41-8

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Description

AZD4144 is an orally active NLRP3 inhibitor (EC50: 0.082 μM). AZD4144 effectively inhibits the release of IL-1β when NLRP3 is overactivated, exerting an anti-inflammatory effect. AZD4144 has low inhibitory effect on hERG and low cardiotoxicity. AZD4144 has the potential to study diseases and conditions associated with NLRP3 inflammasome activation[1].

In Vitro

AZD4144 (Example 1) inhibits Nigericin (HY-127019)- and Lipopolysaccharides (HY-D1056) (LPS)-induced human NLRP3 puncta formation in THP-ASC-GFP cells (EC50: 0.082 μM)[1].
AZD4144 effectively inhibits Nigericin-induced IL-1β release from THP-1 human monocytes (IC50: 0.027 μM)[1].
AZD4144 effectively inhibits BzATP (HY-136254)-induced IL-1β release from THP-1 human monocytes (IC50: 0.01 μM)[1].
AZD4144 has a low inhibitory effect on hERG in Chinese hamster ovary K1 cells expressing hERG (IC50: > 40 μM), has no cardiotoxicity, and is highly safe[1].

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

In Vivo

AZD4144 (Example 1) (3 mg/kg, p.o., one dose) effectively inhibits IL-1β production in LPS/ATP-induced BALB/cAJcl mice[1].

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

Animal Model: BALB/cAJcl mice (male, aged 7 weeks) injected with LPS (0.5 mL of 4 pg/mL) and ATP (0.5 mL of 30 pmol/L)[1]
Dosage: 3 mg/kg
Administration: p.o. one dose
Result: Showed an inhibition rate of 82% on IL-1β.
Clinical Trial
Molecular Weight

379.33

Formula

C18H16F3N3O3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

OC1=C(C2=C(C=CC=C3)C3=C(NC[C@H](O)CO)N=N2)C=CC(C(F)(F)F)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (329.53 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 2.6362 mL 13.1811 mL 26.3623 mL
5 mM 0.5272 mL 2.6362 mL 5.2725 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.67%

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 2.6362 mL 13.1811 mL 26.3623 mL 65.9057 mL
5 mM 0.5272 mL 2.6362 mL 5.2725 mL 13.1811 mL
10 mM 0.2636 mL 1.3181 mL 2.6362 mL 6.5906 mL
15 mM 0.1757 mL 0.8787 mL 1.7575 mL 4.3937 mL
20 mM 0.1318 mL 0.6591 mL 1.3181 mL 3.2953 mL
25 mM 0.1054 mL 0.5272 mL 1.0545 mL 2.6362 mL
30 mM 0.0879 mL 0.4394 mL 0.8787 mL 2.1969 mL
40 mM 0.0659 mL 0.3295 mL 0.6591 mL 1.6476 mL
50 mM 0.0527 mL 0.2636 mL 0.5272 mL 1.3181 mL
60 mM 0.0439 mL 0.2197 mL 0.4394 mL 1.0984 mL
80 mM 0.0330 mL 0.1648 mL 0.3295 mL 0.8238 mL
100 mM 0.0264 mL 0.1318 mL 0.2636 mL 0.6591 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:
AZD4144
Cat. No.:
HY-162877
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