Evaluate the inhibitory effect of AZD8797 on CX3CL1-induced [35S]GTPγS accumulation, results showed AZD8797 effectively inhibited G-protein activation.
Biochem J. 2016 Mar 1;473(5):641-9.
CHO-hCX3CR1 cells
340 nM (IC50)
1 hour
Evaluate the inhibitory effect of AZD8797 on CX3CL1-induced [35S]GTPγS accumulation, results showed AZD8797 effectively inhibited G-protein activation.
Biochem J. 2016 Mar 1;473(5):641-9.
RPMI-8226 cells
5.8 nM (IC50)
15 minutes
Evaluate the inhibitory effect of AZD8797 on the adhesion of RPMI-8226 cells to CX3CL1, results showed AZD8797 effectively inhibited cell adhesion.
Biochem J. 2016 Mar 1;473(5):641-9.
RPMI-8226 cells
5.8 nM (IC50)
15 minutes
Evaluate the inhibitory effect of AZD8797 on the adhesion of RPMI-8226 cells to CX3CL1, results showed AZD8797 effectively inhibited cell adhesion.
Biochem J. 2016 Mar 1;473(5):641-9.
Alveolar macrophages
10 ng/ml or 100 ng/ml
24 hours
IL-21 significantly upregulated M2 macrophage polarization and Fizz1 protein levels
Respir Res. 2024 Dec 4;25(1):428.
Human whole blood leucocytes
330 nM (IC50)
60 minutes
Evaluate the inhibitory effect of AZD8797 on the adhesion of human whole blood leucocytes to CX3CL1, results showed AZD8797 effectively inhibited cell adhesion.
Biochem J. 2016 Mar 1;473(5):641-9.
Human whole blood leucocytes
330 nM (IC50)
60 minutes
Evaluate the inhibitory effect of AZD8797 on the adhesion of human whole blood leucocytes to CX3CL1, results showed AZD8797 effectively inhibited cell adhesion.
Biochem J. 2016 Mar 1;473(5):641-9.
AZD8797 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
OVCAR-4 xenograft model
Oral gavage
0.625 mg/mouse
Once daily for three weeks
The combination of AZD8797 and olaparib showed synergy in reducing tumor burden
The combination of AZD8797 and olaparib showed synergy in reducing tumor burden
Cancers (Basel). 2024 Nov 5;16(22):3728
Sprague-Dawley rats
Status epilepticus model
Intraperitoneal injection
1 mg/kg
Once per day for four days
AZD8797 reversed the decline in nociceptive behaviour in comorbid rats and reduced the number of iba1-positive microglia and microglial activation in rats with migraine after seizures
J Headache Pain. 2022 Apr 5;23(1):42
C57BL/6 mice
Intracerebral hemorrhage model
Lateral ventricular injection
100 μmol/μl
Single injection, lasting for 3 days
AZD8797 increased hematoma volume and worsened neurological deficit score
Cell Mol Life Sci. 2022 Apr 7;79(5):224
Sprague-Dawley rat pups
Bacterial collagenase-induced GMH model
Intracerebroventricular injection
39 μmol/kg
Single dose
AZD8797 reversed the protective effects of r-FKN, increased hemoglobin content, reduced M2 microglia polarization, and increased pro-inflammatory cytokine expression.
Stroke. 2023 Sep;54(9):2420-2433
Dark Agouti rats
MOG 1-125-induced EAE model
Subcutaneous injection
60-78 μmol/kg/24h
Continuous for 14-28 days
AZD8797 treatment significantly reduced paralysis, CNS pathology, and incidence of relapses in EAE rats.
Proc Natl Acad Sci U S A. 2014 Apr 8;111(14):5409-14
C57BL/6J mice
Pharmacologically induced retinal degeneration model
Intravitreal injection
3.125 ng/μL
Single injection, evaluated at 14 and 28 days post-treatment
AZD8797 preserved retinal structure and enhanced photoreceptor survival by inhibiting CX3CL1/CX3CR1 expressions. Fundus photography showed clear retinal vessel distribution and reduced lesion severity. Morphological improvements translated into functional enhancements, as evidenced by behavioral tests and electroretinogram (mf-ERG) examinations. Mechanistic studies showed AZD8797 mitigated microglial activation and migration in degenerative retinas. Müller cell hyper-reaction and secondary gliosis were also suppressed by AZD8797.
Invest Ophthalmol Vis Sci. 2024 Jan 2;65(1):29
Adult male Sprague-Dawley rats
Spinal cord injury model
Intraperitoneal injection
80 µg/kg
Once per day until the rats were sacrificed
AZD8797 improved locomotive recovery after spinal cord injury by suppressing apoptosis, necrosis, and inflammatory responses
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