Rugocrixan
Based on 24 publication(s) in Google Scholar
AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.
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- Purity: 99.54%
- CAS No.: 911715-90-7
- 화학식: C19H25N5OS2
- 분자량:403.56
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
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Publications Citing Use of MedChemExpress (MCE) Rugocrixan
More- Sci Immunol. 2024 May 31;9(95):eadl2171. [Abstract]
- Nat Commun. 2024 Jun 26;15(1):5402. [Abstract]
- Osteoarthritis Cartilage. 2022 Aug;30(8):1140-1153. [Abstract]
- Cell Rep. 2023 Aug 13;42(8):112984. [Abstract]
- Cell Rep. 2021 Mar 23;34(12):108882. [Abstract]
- EMBO Rep. 2023 Aug 3;24(8):e55884. [Abstract]
- Cell Mol Life Sci. 2022 Apr 7;79(5):224. [Abstract]
- Ecotoxicol Environ Saf. 2026 Jun 1:317:120195. [Abstract]
- Ecotoxicol Environ Saf. 2025 Dec 9:309:119545. [Abstract]
- Front Immunol. 2022 Mar 10;13:805420. [Abstract]
- J Thromb Haemost. 2026 May 12:S1538-7836(26)00287-4. [Abstract]
- J Nutr Biochem. 2024 Jan:123:109512. [Abstract]
- Mol Cancer Res. 2023 Jul 5;21(7):726-740. [Abstract]
- Toxicology. 2026 Aug:524:154476. [Abstract]
- Mol Neurobiol. 2025 Apr 25. [Abstract]
- ACS Pharmacol Transl Sci. 2024 Apr 18;7(5):1533-1545. [Abstract]
- J Cancer. 2018 Sep 8;9(19):3603-3612. [Abstract]
- Microsc Microanal. 2023 Dec 21;29(6):2161-2173. [Abstract]
- Behav Brain Res. 2024 Mar 12:461:114837. [Abstract]
- Uppsala University. 2025.
- SSRN. 2025 Nov 5.
- bioRxiv. 2025 Sep 12.
- Patent. US20250228895A1.
- Research Square Preprint. 2011 Dec.
Customer Validation & Images
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Cell Migration/Invasion Assay
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In Vivo Efficacy Study
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Cell Imaging/Staining
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Biological Activity
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CX3CR1 3.9 nM (Ki, 125I-CX3CL-CX3CR1 in HEK293S cells) |
125I-IL-8-CXCR2 2800 nM (Ki, in HEK293S cells) |
In a flow adhesion assay, AZD8797 antagonizes the natural ligand, fractalkine (CX3CL1), in both human whole blood (hWB) and in a B-lymphocyte cell line with IC50 values of 300 and 6 nM respectively. AZD8797 also prevents G-protein activation in a [35S]GTPγS accumulation assay. AZD8797 positively modulates the CX3CL1 response at sub-micromolar concentrations in a β-arrestin recruitment assay. In equilibrium saturation binding experiments, AZD8797 reduces the maximal binding of 125I-CX3CL1 without affecting Kd[1]. AZD8797 binds selectively with high affinity to human and rat CX3CR1 (Ki of hCX3CR1, 4 nM; Ki of rCX3CR1, 7 nM, respectively). The equilibrium dissociation constant, KB, demonstrates that AZD8797 is a very potent inhibitor for human CX3CR1 (10 nM). The potency is threefold lower for rat CX3CR1 (29 nM) and decreases even further at mouse CX3CR1 (54 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 911715-90-7
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Appearance Solid
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분자량 403.56
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화학식 C19H25N5OS2
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Color Light yellow to yellow
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SMILES
CC(C)C[C@@H](NC1=NC(S[C@@H](C)C2=CC=CC=C2)=NC3=C1SC(N)=N3)CO
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Synonyms
AZD8797; KAND567
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (24)
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Journal Impact Factor
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Most Recent
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Sci Immunol
2024 May 31;9(95):eadl2171. PMID: 38820140
Rugocrixan purchased from MedChemExpress. Usage Cited in: Sci Immunol. 2024 May 31;9(95):eadl2171. [Abstract]
The migration cell number of BMDMs induced by WT or Ythdf2-KO B16-OVA tumor cell culture supernatants with or without AZD8797 (Rugocrixan, 10 μM) was measured using a transwell assay (n = 3). DMSO, dimethyl sulfoxide.
Rugocrixan purchased from MedChemExpress. Usage Cited in: Sci Immunol. 2024 May 31;9(95):eadl2171. [Abstract]
WT C57BL/6 mice were subcutaneously injected with 1 × 106 WT or Ythdf2-KO B16-OVA tumor cells. Tumor-inoculated C57BL/6 mice received either an intraperitoneal injection of AZD8797 (Rugocrixan, 1 mg/kg) or an equal amount of PBS daily for 13 days. Tumor sizes were measured every other day starting from the seventh day after tumor inoculation (n = 5).
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Nat Commun
Microglia contribute to neuronal synchrony despite endogenous ATP-related phenotypic transformation in acute mouse brain slices. [Abstract]2024 Jun 26;15(1):5402. PMID: 38926390
Rugocrixan purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 26;15(1):5402. [Abstract]
Comparison of ATP flash/surge characteristics of control, PSB0739 and AZD8797 (Rugocrixan, 10 µM ) treatment. Two-way ANOVA, Tukey’s multiple comparisons, Intensity: F(1, 206) = 92.31, Duration: F(1, 206) = 133, Area: F(1, 206) = 115.8, p < 0.0001 (N = 9 animals, n = 6 ctrl, 8 PSB, 5 AZD-treated slices).
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Osteoarthritis Cartilage
Chondrocyte apoptosis in temporomandibular joint osteoarthritis promotes bone resorption by enhancing chemotaxis of osteoclast precursors. [Abstract]2022 Aug;30(8):1140-1153. PMID: 35513247
Rugocrixan purchased from MedChemExpress. Usage Cited in: Osteoarthritis Cartilage. 2022 Aug;30(8):1140-1153. [Abstract]
AZD8797 (Rugocrixan, 125 μg). Representative sagittal view and 3-dimensional reconstruction of samples harvested at 1 week and 2 weeks after MIA injection.
Rugocrixan purchased from MedChemExpress. Usage Cited in: Osteoarthritis Cartilage. 2022 Aug;30(8):1140-1153. [Abstract]
AZD8797 (Rugocrixan, 125 μg). Bone deterioration related parameters in the VOI of all samples.
Rugocrixan purchased from MedChemExpress. Usage Cited in: Osteoarthritis Cartilage. 2022 Aug;30(8):1140-1153. [Abstract]
AZD8797 (Rugocrixan, 125 μg). HE, SOFG and TRAP staining showing the pathology feature of MIA and MIA + AZD group, cartilage degradation and bone resorption are marked by white and black arrows respectively. The activation of osteoclasts was quantified by the number of TRAP positive cells in each view.
Rugocrixan purchased from MedChemExpress. Usage Cited in: Osteoarthritis Cartilage. 2022 Aug;30(8):1140-1153. [Abstract]
AZD8797 (Rugocrixan, 2 μM). The MIA-induced migration of BMMs canceled by knock-down of CX3CL1 and inhibition of CX3CR1, quantified by the number of migrated cells in each view. Data are presented by mean ± SD (n = 6).
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Cell Rep
Synergy of 5-aminolevulinate supplement and CX3CR1 suppression promotes liver regeneration via elevated IGF-1 signaling. [Abstract]2023 Aug 13;42(8):112984. PMID: 37578861 -
Cell Rep
Microglial identity and inflammatory responses are controlled by the combined effects of neurons and astrocytes. [Abstract]2021 Mar 23;34(12):108882. PMID: 33761343 -
EMBO Rep
Plasma fractalkine contributes to systemic myeloid diversity and PD-L1/PD-1 blockade in lung cancer. [Abstract]2023 Aug 3;24(8):e55884. PMID: 37366231 -
Cell Mol Life Sci
Neuron derived fractalkine promotes microglia to absorb hematoma via CD163/HO-1 after intracerebral hemorrhage. [Abstract]2022 Apr 7;79(5):224. PMID: 35389112 -
Ecotoxicol Environ Saf
Bisphenol A potentiates ischemia-reperfusion-induced endothelial and blood-brain barrier dysfunction associated with CX3CL1-CX3CR1 signaling. [Abstract]2026 Jun 1:317:120195. PMID: 42085735 -
Ecotoxicol Environ Saf
Single-cell transcriptomics unveils atrazine's impact on neurons and microglia in C57BL/6 mice. [Abstract]2025 Dec 9:309:119545. PMID: 41371109 -
Front Immunol
Analysis of Mononuclear Phagocytes Disclosed the Establishment Processes of Two Macrophage Subsets in the Adult Murine Kidney. [Abstract]2022 Mar 10;13:805420. PMID: 35359928 -
J Thromb Haemost
CX3CR1+ synovial macrophages accumulate in the joint during experimental hemophilic arthropathy but are not required for acute synovitis. [Abstract]2026 May 12:S1538-7836(26)00287-4. PMID: 42128059 -
J Nutr Biochem
Hypothalamic FTO promotes high-fat diet-induced leptin resistance in mice through increasing CX3CL1 expression. [Abstract]2024 Jan:123:109512. PMID: 37907171 -
Mol Cancer Res
Triple-negative breast cancer-derived extracellular vesicles promote a hepatic pre-metastatic niche via a cascade of microenvironment remodeling. [Abstract]2023 Jul 5;21(7):726-740. PMID: 37040163 -
Toxicology
Targeting CX3CR1 inhibits silica-induced epithelial-mesenchymal transition and pulmonary fibrosis in mice via the NF-κB signaling pathway. [Abstract]2026 Aug:524:154476. PMID: 42034183 -
Mol Neurobiol
TREK- 1 Ameliorates Secondary Brain Injury by Regulating Inflammatory Microenvironment via CX3 CL1-CX3 CR1 Pathway After Intracerebral Hemorrhage. [Abstract]2025 Apr 25. PMID: 40279035 -
ACS Pharmacol Transl Sci
Development of a Fluorescent Ligand for the Intracellular Allosteric Binding Site of the Neurotensin Receptor 1. [Abstract]2024 Apr 18;7(5):1533-1545. PMID: 38751637 -
J Cancer
CX3CL1 involves in breast cancer metastasizing to the spine via the Src/FAK signaling pathway. [Abstract]2018 Sep 8;9(19):3603-3612. PMID: 30310518
Rugocrixan purchased from MedChemExpress. Usage Cited in: J Cancer. 2018 Sep 8;9(19):3603-3612. [Abstract]
MDA-MB-231 cells are pretreated with the CX3CR1 antagonist AZD8797, and stimulated by CX3CL1 for 30 mins, the phosphorylation levels of Src and FAK are detected. CX3CL1-only group as control.
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Microsc Microanal
2023 Dec 21;29(6):2161-2173. PMID: 37967299 -
Behav Brain Res
2024 Mar 12:461:114837. PMID: 38145872 -
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용액&용해도
DMSO : 100 mg/mL (247.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 20% HP-β-CD in Saline
Solubility: 5 mg/mL (12.39 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Rats: AZD8797 is formulated in 30–35% (wt/wt) hydroxy-propyl-beta-cyklodextrin and administered s.c. through osmotic minipumps. Treatment is blinded to the operator. The plasma concentration of AZD8797 is analyzed twice from each rat[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Cederblad L, et al. AZD8797 is an allosteric non-competitive modulator of the human CX3CR1 receptor. Biochem J. 2016 Mar 1;473(5):641-9. [Content Brief]
[2]. Ridderstad Wollberg A, et al. Pharmacological inhibition of the chemokine receptor CX3CR1 attenuates disease in a chronic-relapsing rat model for multiple sclerosis. Proc Natl Acad Sci U S A. 2014 Apr 8;111(14):5409-14. [Content Brief]
[3]. Sofia Karlströ, et al. Substituted 7-amino-5-thio-thiazolo[4,5-d]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1). J Med Chem. 2013 Apr 25;56(8):3177-90. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4779 mL | 12.3897 mL | 24.7795 mL | 61.9487 mL |
| 5 mM | 0.4956 mL | 2.4779 mL | 4.9559 mL | 12.3897 mL | |
| 10 mM | 0.2478 mL | 1.2390 mL | 2.4779 mL | 6.1949 mL | |
| 15 mM | 0.1652 mL | 0.8260 mL | 1.6520 mL | 4.1299 mL | |
| 20 mM | 0.1239 mL | 0.6195 mL | 1.2390 mL | 3.0974 mL | |
| 25 mM | 0.0991 mL | 0.4956 mL | 0.9912 mL | 2.4779 mL | |
| 30 mM | 0.0826 mL | 0.4130 mL | 0.8260 mL | 2.0650 mL | |
| 40 mM | 0.0619 mL | 0.3097 mL | 0.6195 mL | 1.5487 mL | |
| 50 mM | 0.0496 mL | 0.2478 mL | 0.4956 mL | 1.2390 mL | |
| 60 mM | 0.0413 mL | 0.2065 mL | 0.4130 mL | 1.0325 mL | |
| 80 mM | 0.0310 mL | 0.1549 mL | 0.3097 mL | 0.7744 mL | |
| 100 mM | 0.0248 mL | 0.1239 mL | 0.2478 mL | 0.6195 mL |
Rugocrixan Related Classifications
HY-13848 Related Classifications
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