Rugocrixan (Synonyms: AZD8797; KAND567)

Name: Rugocrixan
Brand: MedChemExpress
SKU: HY-13848
Rating: 5.0 (21 reviews)

Cat. No.: HY-13848 Pureza: 99.54%: Ficha de datos
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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.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS : 911715-90-7

Tamaño	Stock	Cantidad

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
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Revisión del cliente

Based on 21 publication(s) in Google Scholar

21 Publications Citing Use of MCE Rugocrixan

Cell Migration/Invasion Assay

Cell Imaging/Staining

In Vivo Efficacy Study

Histological Imaging/Staining

: 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).

: 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).

: 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).

: 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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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

Actividad biológica
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Descripciòn

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)

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.

Ensayo clínico

Peso molecular

403.56

Fòrmula

C₁₉H₂₅N₅OS₂

No. CAS

911715-90-7

Appearance

Solid

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Calculadora de molaridad
Calculadora de dilución

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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.

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Pureza y Documentación

Purity: 99.54%

Select Batch:

Ficha de datos (278 KB) SDS (393 KB)

COA (252 KB) HNMR (168 KB) LCMS (94 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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]

Administraciòn de animales
^[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].

MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

Referencias

[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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rugocrixan911715-90-7AZD8797 KAND567AZD 8797AZD-8797KAND567KAND 567KAND-567CX3CR1CXCRCX3C chemokine receptor1GPR13fractalkine receptor CXC chemokine receptorsC-X-C motif chemokine receptorsInhibitorinhibitorinhibit

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Rugocrixan (Synonyms: AZD8797; KAND567)

Revisión del cliente

Rugocrixan Related Antibodies

21 Publications Citing Use of MCE Rugocrixan

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas CXCR:

Actividad biológica

Protocolo

Pureza y Documentación

Referencias

Revisión del cliente

Rugocrixan Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Rugocrixan Related Classifications

Keywords:

Productos vistos recientemente:

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