Art. -Nr.: HY-13848

Rugocrixan

(Synonyms: AZD8797; KAND567)

24 Cited Publications

Kundenbewertung

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 K_is of 3.9 and 2800 nM, respectively.

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Reinheit: 99.54%
CAS. Nr.: 911715-90-7
Formel: C₁₉H₂₅N₅OS₂
Molecular Weight:403.56

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Rugocrixan Chemical Structure

CAS. Nr.: 911715-90-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (24)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with K_is of 3.9 and 2800 nM, respectively^[1].

IC₅₀ & Target^[3]

CX3CR1

3.9 nM (Ki, ¹²⁵I-CX3CL-CX3CR1 in HEK293S cells)

¹²⁵I-IL-8-CXCR2

2800 nM (Ki, in HEK293S cells)

Alle CXCR Isoform-spezifische Produkte anzeigen :

In Vitro

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 K_d^[1]. AZD8797 binds selectively with high affinity to human and rat CX3CR1 (K_i of hCX3CR1, 4 nM; K_i of rCX3CR1, 7 nM, respectively). The equilibrium dissociation constant, K_B, 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.

In Vivo

AZD8797 treatment in Dark Agouti rats with myelin oligodendrocyte glycoprotein-induced EAE results in reduced paralysis, CNS pathology, and incidence of relapses. The compound is effective when starting treatment before onset, as well as after the acute phase^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

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

Chemical Information

CAS. Nr. 911715-90-7
Appearance Solid
Molecular Weight 403.56
Formel C₁₉H₂₅N₅OS₂
Color Light yellow to yellow
SMILES

CC(C)C[C@@H](NC1=NC(S[C@@H](C)C2=CC=CC=C2)=NC3=C1SC(N)=N3)CO
Synonyms

AZD8797; KAND567
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (24)

All Cell Migration/Invasion AssayCell Imaging/StainingIn Vivo Efficacy StudyHistological Imaging/StainingWB

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Journal Impact Factor

Sci Immunol

The tumor-intrinsic role of the m6A reader YTHDF2 in regulating immune evasion. [Abstract]

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).
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).
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).
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.
Microsc Microanal

SARS-CoV-2 Causes Brain Damage: Therapeutic Intervention with AZD8797. [Abstract]

2023 Dec 21;29(6):2161-2173. PMID: 37967299
Behav Brain Res

CX3CR1 mediates Motor Dysfunction in Mice through 5-HTR2a. [Abstract]

2024 Mar 12:461:114837. PMID: 38145872
Uppsala University

2025.
SSRN

2025 Nov 5.
bioRxiv

2025 Sep 12.
Patent

US20250228895A1.
Research Square Preprint

2011 Dec.

Lösungsmittel & Löslichkeit

In Vitro:

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)

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

2.4779 mL

12.3897 mL

24.7795 mL

5 mM

0.4956 mL

2.4779 mL

4.9559 mL

10 mM

0.2478 mL

1.2390 mL

2.4779 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

Add each solvent one by one: 20% HP-β-CD in Saline

Solubility: 5 mg/mL (12.39 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Animal Administration^[2]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
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)
Handling Instructions (2659 KB)

Verweise

[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]

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, 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

Keywords

Rugocrixan

24 Cited Publications

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Rugocrixan

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Small Molecule Immuno-Oncology Compound Library

Drug Repurposing Compound Library

Endocrinology Compound Library

Orally Active Compound Library

Targeted Diversity Library

Chemokine Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Rugocrixan

Alle CXCR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Rugocrixan

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Small Molecule Immuno-Oncology Compound Library

Drug Repurposing Compound Library

Endocrinology Compound Library

Orally Active Compound Library

Targeted Diversity Library

Chemokine Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Rugocrixan

Alle CXCR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Rugocrixan Related Classifications

HY-13848 Related Classifications