AZD8797 (Synonyms: KAND567) |
Catalog No.GC31653
One-Click Copy Product Info
|
AZD8797 is a selective, high-affinity small-molecule inhibitor of CX3CR1, with a Ki value of 7nM for rat CX3CR1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 911715-90-7
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
AZD8797 is a selective, high-affinity small-molecule inhibitor of CX3CR1, with a Ki value of 7nM for rat CX3CR1 [1]. AZD8797 has been widely used to inhibit inflammatory responses in different animal models by binding to receptors at different sites of CX3CL1 to affect CX3CL1 interaction with CX3CR1[2].
In vitro, AZD8797 pretreatment (2mM) for 1 hour significantly decreased the expression levels of CX3CR1 and MMP13 in rat chondrocytes after 24h lipopolysaccharide (LPS) stimulation[3]. Co-treatment of 5μM AZD8797 with 5μM olaparib for 48 hours significantly inhibited Caov-3 cell colony formation and inhibited cell proliferation[4]. Treatment with 10μM AZD8797 for 12 hours resulted in down-regulation of 5-HTR2a expression and decreased phosphorylation of P65 and IκB proteins in PC-12 cells[5].
In vivo, AZD8797 treatment via intraperitoneal injection at a dose of 10mg/kg/day for 10 days reduced spleen mass and cardiac levels of CCL2 and IL-15, with an increase of IL-4 in the mice with acute Trypanosoma cruzi infection[6]. Daily intraperitoneal injection of AZD8797 at a dose of 80μg/kg/day for 10 days can enhance the early behavioral recovery, inhibit the activation of apoptosis, and reduce the inflammatory response in a rat spinal cord injury model[7]. AZD8797 (2mg/kg/day) administered via the tail vein for 5 days reduced proteinuria, cell proliferation, and inflammation of glomerulus in rats with mesangial proliferative glomerulonephritis (MsPGN)[8].
References:
[1] Ridderstad Wollberg A, Ericsson-Dahlstrand A, Juréus A, et al. Pharmacological inhibition of the chemokine receptor CX3CR1 attenuates disease in a chronic-relapsing rat model for multiple sclerosis[J]. Proceedings of the National Academy of Sciences, 2014, 111(14): 5409-5414.
[2] Huang J M, Zhao N, Hao X N, et al. CX3CL1/CX3CR1 signaling mediated neuroglia activation is implicated in the retinal degeneration: a potential therapeutic target to prevent photoreceptor death[J]. Investigative Ophthalmology & Visual Science, 2024, 65(1): 29-29.
[3] Huang J, Zheng X, Meng J, et al. Experimental study on the role and biomarker potential of CX3CR1 in osteoarthritis[J]. Annals of medicine, 2025, 57(1): 2529577.
[4] Xie J, Barbolina M V. Dual Targeting of CX3CR1 and PARP in Models of High-Grade Serous Ovarian Carcinoma[J]. Cancers, 2024, 16(22): 3728.
[5] Pei J, Zou Y, Wan C, et al. CX3CR1 mediates motor dysfunction in mice through 5-HTR2a[J]. Behavioural brain research, 2024, 461: 114837.
[6] Pio S, Menezes T P, Louise V, et al. Role of the CX3CL1/CX3CR1 axis in iron metabolism and immune regulation during acute Trypanosoma cruzi infection[J]. Frontiers in Immunology, 2025, 16: 1585883.
[7] Chen G, Zhou Z, Sha W, et al. A novel CX3CR1 inhibitor AZD8797 facilitates early recovery of rat acute spinal cord injury by inhibiting inflammation and apoptosis[J]. International journal of molecular medicine, 2020, 45(5): 1373-1384.
[8] Zhang J, Fang Q, Huang Y, et al. CX3CR1+ Monocytes/Macrophages Promote Regional Immune Injury in Mesangial Proliferative Glomerulonephritis through Crosstalk with Activated Mesangial Cells[J]. Research, 2025, 8: 0716.
| Cell experiment [1]: | |
Cell lines | Rat chondrocytes |
Preparation Method | Rat chondrocytes were cultured in DMEM medium supplemented with 10% fetal bovine serum and 1% penicillin/streptomycin at 37 °C in 5% CO2. The third passage of chondrocytes was used for subsequent experiments. An in vitro OA model was established by exposing chondrocytes to 1mg/ml lipopolysaccharide (LPS) for 24 hours. The experimental conditions were divided into three groups: (1) untreated control group; (2) OA group, LPS stimulation (1mg/ml); (3) OA+AZD8797 group, preincubated with 2mM AZD8797 for 1 hour before LPS treatment. After that, qRT-PCR and immunoblot analysis were performed. |
Reaction Conditions | 2mM; 1h |
Applications | AZD8797 treatment significantly decreased the expression levels of CX3CR1 and MMP13 in chondrocytes after LPS stimulation. |
| Animal experiment [2]: | |
Animal models | Male Wistar rats |
Preparation Method | Male Wistar rats (6-8 weeks old, 200-250g) were maintained under constant temperature (20°C), constant humidity (70%), and alternating day and night. The MsPGN model was established by injecting anti-Thy1 antibody (2.5mg/kg) through the tail vein, and the control group was injected with the same volume of normal saline. AZD8797 (2mg/kg/day) was injected daily through the tail vein from day 3 to day 7 after the model establishment. On days 7, 10, and 14 after modeling, the rats were sacrificed after pentobarbital anesthesia, and blood, urine, and kidney tissue were collected for analysis. |
Dosage form | 2mg/kg/day for 5 days; tail vein injection |
Applications | AZD8797 treatment ameliorated proteinuria, cell proliferation, and inflammation of the glomerulus in the rats. |
References: | |
| Cas No. | 911715-90-7 | SDF | |
| Synonyms | KAND567 | ||
| Canonical SMILES | CC(C)C[C@@H](NC1=NC(S[C@@H](C)C2=CC=CC=C2)=NC3=C1SC(N)=N3)CO | ||
| Formula | C19H25N5OS2 | M.Wt | 403.56 |
| Solubility | DMSO : ≥ 150 mg/mL (371.69 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4779 mL | 12.3897 mL | 24.7795 mL |
| 5 mM | 495.6 μL | 2.4779 mL | 4.9559 mL |
| 10 mM | 247.8 μL | 1.239 mL | 2.4779 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)