Referencia número: HY-162877

AZD4144

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Based on 1 Customer Validation

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.

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Pureza: 99.67%
No. CAS: 2890191-41-8
Fòrmula: C₁₈H₁₆F₃N₃O₃
Peso molecular:379.33

Almacenamiento:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

AZD4144 Chemical Structure

No. CAS: 2890191-41-8

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Actividad biológica
- Descripciòn
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Ver todos los productos específicos de isoformas NOD-like Receptor (NLR) :

Ver todos los productos específicos de isoformas Interleukin Related :

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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 2890191-41-8
Appearance Solid
Peso molecular 379.33
Fòrmula C₁₈H₁₆F₃N₃O₃
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
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6362 mL

13.1811 mL

26.3623 mL

5 mM

0.5272 mL

2.6362 mL

5.2725 mL

10 mM

0.2636 mL

1.3181 mL

2.6362 mL

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Lars Anders Mikael Johansson, et al. NLRP3 INFLAMMASOME INHIBITORS. WO2023275366. JP. 2023-01-05.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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AZD4144

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Ver todos los productos específicos de isoformas NOD-like Receptor (NLR)

Ver todos los productos específicos de isoformas Interleukin Related

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

AZD4144 Related Classifications

HY-162877 Related Classifications