2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. A-836339

A-836339 is a selective CB2 receptor agonist, with Ki values of 0.4 nM and 0.8 nM in humans and rats, respectively. A-836339 exhibits multiple effects such as analgesia, gastric protection, anti-inflammation, and antioxidant activity. A-836339 produces antinociceptive and analgesic activities by activating CB2 receptors in the dorsal root ganglia and spinal cord. A-836339 can also exert gastric protective effects through anti-inflammatory mechanisms (reducing TNF-α and IL-1β) and antioxidant mechanisms (enhancing the activities of CAT and SOD, and reducing H2O2). Radioactively labeled A-836339 can serve as a CB2-specific radioligand for autoradiography and PET imaging. A-836339 can be used in research on inflammatory pain, neuropathic pain, gastric ulcers, cerebral ischemia, etc.

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A-836339

A-836339 Chemical Structure

CAS No. : 959746-77-1

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

A-836339 is a selective CB2 receptor agonist, with Ki values of 0.4 nM and 0.8 nM in humans and rats, respectively. A-836339 exhibits multiple effects such as analgesia, gastric protection, anti-inflammation, and antioxidant activity. A-836339 produces antinociceptive and analgesic activities by activating CB2 receptors in the dorsal root ganglia and spinal cord. A-836339 can also exert gastric protective effects through anti-inflammatory mechanisms (reducing TNF-α and IL-1β) and antioxidant mechanisms (enhancing the activities of CAT and SOD, and reducing H2O2). Radioactively labeled A-836339 can serve as a CB2-specific radioligand for autoradiography and PET imaging. A-836339 can be used in research on inflammatory pain, neuropathic pain, gastric ulcers, cerebral ischemia, etc[1][2][3][4][5].

In Vitro

A-836339 (20 µM; 20 min; brain sections) decreases [11C]A-836339 binding in the ipsilateral hemisphere after LPS and AMPA injection[4].

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

A-836339 Related Antibodies
In Vivo

A-836339 (5 mg/kg; oral) demonstrates co-localization of CB2 receptors and COX-2 in gastric tissue of EtOH-induced ulcer model in mice[3].
A-836339 (0.3 µmol/kg; i.t.) reverses neuropathic pain by acting at spinal cord sites[1].
A-836339 (0.3 µmol/kg; intra-DRG) reverses inflammatory pain by acting at dorsal root ganglion sites[1].
A-836339 (0.3 µmol/kg; intra-DRG) reverses neuropathic pain by acting at dorsal root ganglion sites[1].
A-836339 (1-10 µmol/kg; IP) reverses inflammatory pain by acting through CB2 receptors[1].
A-836339 (3-30 µmol/kg; IP) reverses neuropathic pain in the CCI model via CB2 receptor activation and without opioid dependency[1].
A-836339 (1-5 mg/kg; oral) reduces ulcer index and ULI in EtOH-induced gastric ulcer model in mice by enhancing gastroprotection and reversing histological damage, reduces TNF-α levels, and enhances antioxidant defense mechanisms by increasing CAT and SOD activities and reducing H2O2 levels[3].
A-836339 (1-5 mg/kg; oral) reduces ulcer index and ULI in NSAID-induced gastric ulcer model in mice, enhances CAT activity, and reduces H2O2 levels, while also reducing TNF-α levels[3].

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

Animal Model: Sprague Dawley rats (male, 250-300 g); inflammatory model, induced by CFA injection[1]
Dosage: 1 µmol/kg, 3 µmol/kg, 10 µmol/kg
Administration: IP
Result: Significantly reversed CFA-induced thermal hyperalgesia in a dose-dependent manner, with an ED50 of 1.8 µmol/kg. The effect was blocked by a CB2 antagonist but not a CB1 antagonist.
Animal Model: Sprague Dawley rats (male, 250-300 g); neuropathic model, induced by SNL[1]
Dosage: 3 µmol/kg, 10 µmol/kg, 30 µmol/kg
Administration: IP
Result: Systemic A-836339 dose-dependently reversed SNL-induced mechanical allodynia (67% at 30 µmol/kg, ED50 14.5 µmol/kg). The effect was not blocked by naloxone.
Animal Model: Sprague Dawley rats (male, 250-300 g); neuropathic model, induced by CCI[1]
Dosage: 3 µmol/kg, 10 µmol/kg, 30 µmol/kg
Administration: IP
Result: Systemic A-836339 attenuated CCI-induced mechanical allodynia (71% at 30 µmol/kg). The effect was blocked by a CB2 antagonist.
Animal Model: Sprague Dawley rats (male, 250-300 g); inflammatory model, induced by CFA injection[1]
Dosage: 0.3 µmol/kg
Administration: Others (intra-DRG)
Result: Intra-DRG administration of A-836339 significantly reversed CFA-induced thermal hyperalgesia (65%).
Animal Model: Sprague Dawley rats (male, 250-300 g); inflammatory model, induced by CFA injection[1]
Dosage: 0.3 µmol/kg
Administration: Others (i.t.)
Result: Intrathecal administration of A-836339 did not significantly reverse CFA-induced thermal hyperalgesia (14%).
Animal Model: Sprague Dawley rats (male, 250-300 g); inflammatory model, induced by CFA injection[1]
Dosage: 0.2 µmol/kg, 0.6 µmol/kg
Administration: Others (i.paw)
Result: Ipsilateral intraplantar administration of A-836339 showed a weak effect (27% reversal at 0.6 µmol/kg), with similar effects observed on the contralateral paw.
Animal Model: Sprague Dawley rats (male, 250-300 g); neuropathic model, induced by SNL[1]
Dosage: 0.3 µmol/kg
Administration: Others (intra-DRG)
Result: Intra-DRG administration of A-836339 significantly attenuated SNL-induced mechanical allodynia (45%).
Animal Model: Sprague Dawley rats (male, 250-300 g); neuropathic model, induced by SNL[1]
Dosage: 0.3 µmol/kg
Administration: Others (i.t.)
Result: Intrathecal administration of A-836339 reversed SNL-induced mechanical allodynia (33%).
Animal Model: Balb/C mice (male, 21-23 g); EtOH-induced gastric ulcer model, induced by 80% EtOH[3]
Dosage: 1 mg/kg, 3 mg/kg, 5 mg/kg
Administration: Oral
Result: Reduced ulcer index and ULI in a dose-dependent manner. Administration of the CB2 antagonist AM630 (1 mg/kg, i.p.) before A836339 (5 mg/kg, p.o.) significantly reversed its gastroprotective effect. Histological analysis showed reversed damage after A836339 administration. Reduced TNF-α levels compared to EtOH-treated group. Partial reversal of anti-inflammatory effect by AM630 (1 mg/kg, i.p.), though not statistically significant. IL-1β levels showed non-significant reduction. Increased catalase (CAT) and superoxide dismutase (SOD) activities in a dose-dependent manner. Reduced H2O2 levels, with the highest dose (5 mg/kg) showing statistical significance. Effects reversed by AM630 (1 mg/kg, i.p.).
Animal Model: Balb/C mice (male, 21-23 g); EtOH-induced gastric ulcer model, induced by 80% EtOH[3]
Dosage: 5 mg/kg
Administration: Oral
Result: Co-localization of CB2 receptors and COX-2 in non-neuronal gastric tissue observed via immunohistochemistry (IHC).
Animal Model: Balb/C mice (male, 21-23 g); NSAID-induced gastric ulcer model, induced by diclofenac 30 mg/kg p.o.[3]
Dosage: 1 mg/kg, 3 mg/kg, 5 mg/kg
Administration: Oral
Result: Reduced ulcer index and ULI in a dose-dependent manner, though differences were not statistically significant. Histological damage reversed by A836339 administration. CAT activity increased, H2O2 levels reduced. GSH levels decreased. Reduced TNF-α levels compared to NSAID-treated group. IL-1β levels showed no significant change.
Molecular Weight

310.45

Formula

C16H26N2O2S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=C(C)S/C(N1CCOC)=N\C(C2C(C)(C)C2(C)C)=O
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 : 12 mg/mL (38.65 mM; Need ultrasonic and warming; 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 3.2211 mL 16.1057 mL 32.2113 mL
5 mM 0.6442 mL 3.2211 mL 6.4423 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.

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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: ≥ 0.71 mg/mL (2.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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: ≥ 0.71 mg/mL (2.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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:

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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 3.2211 mL 16.1057 mL 32.2113 mL 80.5283 mL
5 mM 0.6442 mL 3.2211 mL 6.4423 mL 16.1057 mL
10 mM 0.3221 mL 1.6106 mL 3.2211 mL 8.0528 mL
15 mM 0.2147 mL 1.0737 mL 2.1474 mL 5.3686 mL
20 mM 0.1611 mL 0.8053 mL 1.6106 mL 4.0264 mL
25 mM 0.1288 mL 0.6442 mL 1.2885 mL 3.2211 mL
30 mM 0.1074 mL 0.5369 mL 1.0737 mL 2.6843 mL
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A-836339 Related Classifications

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  • 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:

A-836339959746-77-1A836339A 836339Cannabinoid Receptorneuropathic painanalgesic effectsantinociceptionCB2spinal cordup-regulationpositron-emission tomography (PET)intraplantar administration[11C]A-836339CFAAPPswe/PS1dE9 miceAbeta amyloid plaqueDRGendocannabinoidsneuroinflammationintrathecal administrationCB2 receptorpositron emission tomographycerebral ischemiaCB2 receptorslipopolysaccharide (LPS)[18F]DPA-714CB2 agonistintra-DRG administrationinflammatory painSNLquantitative RT-PCRmouse modelsradioligandpawcannabinoid type 2 receptorsAlzheimer's diseaseInhibitorinhibitorinhibit

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