A-836339 |
Catalog No.GC18199 |
A-836339 is a synthetic cannabinoid (CB) which has a higher affinity for the peripheral CB2 receptor (Ki = 0.64 nM) over the central CB1 receptor (Ki = 270 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 959746-77-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
A-836339 is a cannabinoid CB2 receptor-selective agonist; exhibits high potencies at CB(2) and selectivity over CB(1) receptors.IC50 value: 1.6 nM(EC50) [1]Target: CB2 agonistin vitro: In radioligand binding assays, A-836339 displays high affinities at CB(2) receptors and selectivity over CB(1) receptors in both human and rat.In addition A-836339 exhibits a profile devoid of significant affinity at other G-protein-coupled receptors and ion channels [1].in vivo: In the complete Freund's adjuvant model of inflammatory pain, A-836339 exhibits a potent CB(2) receptor-mediated antihyperalgesic effect that is independent of CB(1) or mu-opioid receptors. A-836339 has also demonstrated efficacies in the chronic constrain injury (CCI) model of neuropathic pain, skin incision, and capsaicin-induced secondary mechanical hyperalgesia models [1]. Similar to systemic delivery, intra-spinal injection of A-836339 (0.3 and 1 nmol) also attenuated both von Frey-evoked and spontaneous firing of WDR neurons in neuropathic rats. Intra-spinal injections of A-836339 were ineffective in sham rats [2]. Systemic A-836339 and AM1241 produced dose-dependent efficacy in both inflammatory and neuropathic pain models. Local administration of CB agonists also produced significant analgesic effects in SNL (intra-DRG and i.t.) and CFA (intra-DRG) pain models [3].
References:
[1]. Yao BB, et al. Characterization of a cannabinoid CB2 receptor-selective agonist, A-836339 [2,2,3,3-tetramethyl-cyclopropanecarboxylic acid [3-(2-methoxy-ethyl)-4,5-dimethyl-3H-thiazol-(2Z)-ylidene]-amide], using in vitro pharmacological assays, in vivo pa
[2]. McGaraughty S, et al. A CB(2) receptor agonist, A-836339, modulates wide dynamic range neuronal activity in neuropathic rats: contributions of spinal and peripheral CB(2) receptors. Neuroscience. 2009 Feb 18;158(4):1652-61.
[3]. Hsieh GC, et al. Central and peripheral sites of action for CB receptor mediated analgesic activity in chronic inflammatory and neuropathic pain models in rats. Br J Pharmacol. 2011 Jan;162(2):428-40.
Cas No. | 959746-77-1 | SDF | |
Chemical Name | [N(Z)]-N-[3-(2-methoxyethyl)-4,5-dimethyl-2(3H)-thiazolylidene]-2,2,3,3-tetramethyl-cyclopropanecarboxamide | ||
Canonical SMILES | CC1=C(C)N(CCOC)/C(S1)=N/C(C2C(C)(C)C2(C)C)=O | ||
Formula | C16H26N2O2S | M.Wt | 310.5 |
Solubility | DMF: 20 mg/ml,DMSO: 5 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.2206 mL | 16.1031 mL | 32.2061 mL |
5 mM | 0.6441 mL | 3.2206 mL | 6.4412 mL |
10 mM | 0.3221 mL | 1.6103 mL | 3.2206 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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