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Chemical Structure| 911715-90-7 Chemical Structure| 911715-90-7

Structure of AZD8797
CAS No.: 911715-90-7

Chemical Structure| 911715-90-7

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AZD8797 (KAND567) is an allosteric, non-competitive, orally active antagonist of the human CX3CR1 receptor, with Kis of 3.9 nM and 2800 nM for CX3CR1 and CXCR2, respectively.

Synonyms: KAND567

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Product Details of AZD8797

CAS No. :911715-90-7
Formula : C19H25N5OS2
M.W : 403.56
SMILES Code : CC(C)C[C@@H](NC1=C(SC(N)=N2)C2=NC(S[C@H](C3=CC=CC=C3)C)=N1)CO
Synonyms :
KAND567
MDL No. :MFCD28139065

Safety of AZD8797

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P313-P337+P313-P362-P403+P233-P405-P501

Related Pathways of AZD8797

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
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.
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.

In Vivo:

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 Cancers (Basel). 2024 Nov 5;16(22):3728
Nude mice OVCAR-4 xenograft model Oral gavage 0.625 mg/mouse (AZD8797), 0.25 mg/mouse (olaparib) Once daily for three weeks 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 Int J Mol Med. 2020 May;45(5):1373-1384

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2.48mL

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0.25mL

12.39mL

2.48mL

1.24mL

24.78mL

4.96mL

2.48mL

 

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