2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. AZ084

AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a Ki of 0.9 nM. Has potential to treat asthma. AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer.

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AZ084 Chemical Structure

AZ084 Chemical Structure

CAS No. : 929300-19-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
1 mg USD 166 In-stock
5 mg USD 350 In-stock
10 mg USD 550 In-stock
50 mg USD 1650 In-stock
100 mg USD 2250 In-stock
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Based on 2 publication(s) in Google Scholar

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Description

AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a Ki of 0.9 nM. Has potential to treat asthma[1]. AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer[1][2].

IC50 & Target[1]

CCR8

0.9 nM (Ki)

In Vitro

AZ084 (5 μg/mL; single daily for 4 days) suppresses proportion of Tregs and reduces T cells that expresses CCR8 (co-cultured in vitro with LLC-exo MPF CM)[1].
? AZ084 (0-10 μM) inhibits AML, DC and T cells with IC50s of 1.3, 4.6 and 5.7 nM, respectively[2].

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

AZ084 Related Antibodies

Cell Viability Assay[1]

Cell Line: Splenic T cells
Concentration: 5 μg/mL (single daily)
Incubation Time: 4 days
Result: Reversed the increased proportion of Tregs among the CD4+ T cells co-cultured in vitro with LLC-exo MPF CM.
Reduced T cells that expressed CCR8 (cultured in vitro with by LLC-exo MPF CM).

Cell Viability Assay[2]

Cell Line: AML, DC and T cells
Concentration: 0-10 µM
Incubation Time:
Result: Showed high potency with pronounced dose-response dependent inhibition of chemotaxis with an IC50 of 1.3 nM in AML cells.
In Vivo

AZ084 (5 mg/kg; i.p.; every third day for 9 or 21 days) restrains the formation of the immunologically tolerant PMN and tumor cells metastasis in lung by downregulating Treg differentiation[1].
? AZ084 (434.57-869.14 mg/kg; i.v.; single) shows a bioavailability >70% in rats[2].

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

Animal Model: C57BL/6 J mice (subcutaneous LLC tumor model)[1].
Dosage: 5 mg/kg
Administration: Intraperitoneal injection, every third day for 9 or 21 days.
Result: Inhibited Treg differentiation and tumor cell colonization of the lungs and reduced the number of CD4+Foxp3+ Tregs in the lungs of LLC-exo pre-injected mice (every third day for 9 days).
Inhibited the LLC-exo-induced LLC cell seeding in lung and also significantly reduced Treg accumulation in LLC-exo stimulated mouse lungs(every third day for 21 days).
Animal Model: Female Balb/C mice, male Wistar rats and female Beagle dogs[2].
Dosage: 434.57-869.14 mg/kg (in 0.9% NaCl)
Administration: Intravenous injection, single.
Result: 1.19 Pharmacokinetic Parameters of AZ084 in Female Balb/C mice, male Wistar rats and female Beagle dogs[2].
IV (434.57-869.14 mg/kg)
Dog plasma protein binding (% free) 45.7
Mu plasma protein binding (% free) 55.6
Hu plasma protein binding (% free) 31.0
Rat plasma protein binding (% free) 47.0
Rat HW plasma PK CL (mL/min/kg) 15.0
Rat HW plasma PK Vss (L/kg) 6.0
Rat HW plasma PK T1/2 (h) 5.4
Rat HW plasma PK Cmax (µM) 0.5
Rat HW plasma PK bioavailability (%) 68.0
Molecular Weight

434.57

Formula

C26H34N4O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NC=C(N)C=C1)N2CCC3(CCN(CC4=C5CC(C)(C)OC5=CC=C4)CC3)CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (575.28 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 2.3011 mL 11.5056 mL 23.0113 mL
5 mM 0.4602 mL 2.3011 mL 4.6023 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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: ≥ 2.08 mg/mL (4.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

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.
Purity & Documentation
References

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 2.3011 mL 11.5056 mL 23.0113 mL 57.5281 mL
5 mM 0.4602 mL 2.3011 mL 4.6023 mL 11.5056 mL
10 mM 0.2301 mL 1.1506 mL 2.3011 mL 5.7528 mL
15 mM 0.1534 mL 0.7670 mL 1.5341 mL 3.8352 mL
20 mM 0.1151 mL 0.5753 mL 1.1506 mL 2.8764 mL
25 mM 0.0920 mL 0.4602 mL 0.9205 mL 2.3011 mL
30 mM 0.0767 mL 0.3835 mL 0.7670 mL 1.9176 mL
40 mM 0.0575 mL 0.2876 mL 0.5753 mL 1.4382 mL
50 mM 0.0460 mL 0.2301 mL 0.4602 mL 1.1506 mL
60 mM 0.0384 mL 0.1918 mL 0.3835 mL 0.9588 mL
80 mM 0.0288 mL 0.1438 mL 0.2876 mL 0.7191 mL
100 mM 0.0230 mL 0.1151 mL 0.2301 mL 0.5753 mL
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AZ084 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:

AZ084929300-19-6AZ 084AZ-084CCRCC chemokine receptorasthmaTregs differentiationtumor metastasisPMNT cellsInhibitorinhibitorinhibit

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