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A-836339

Catalog No. T7375 CAS 959746-77-1

A-836339 acts as a potent cannabinoid receptor full agonist which has a higher affinity for the peripheral CB2 receptor (Ki = 0.64 nM) over the central CB1 receptor (Ki = 270 nM). It displays analgesic, anti-inflammatory, and anti-hyperalgesic effects in mice.

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A-836339, CAS 959746-77-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
5 mg	In stock	$ 155.00
10 mg	In stock	$ 278.00
25 mg	In stock	$ 468.00
50 mg	In stock	$ 688.00
100 mg	In stock	$ 978.00
1 mL * 10 mM (in DMSO)	In stock	$ 143.00

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Purity: 98%

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Description	A-836339 acts as a potent cannabinoid receptor full agonist which has a higher affinity for the peripheral CB2 receptor (Ki = 0.64 nM) over the central CB1 receptor (Ki = 270 nM). It displays analgesic, anti-inflammatory, and anti-hyperalgesic effects in mice.
In vivo	A-836339 was characterized extensively in various animal pain models. 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. Furthermore, no tolerance was developed in the CCI model after subchronic treatment with A-836339 for 5 days[1].
Animal Research	The plantar aspect of the rat left hind paw was exposed through a hole in a sterile plastic drape, and a 1-cm longitudinal incision was made through the skin and fascia, starting 0.5 cm from the proximal edge of the heel and extending toward the toes. The plantaris muscle was elevated and incised longitudinally, leaving the muscle origin and insertion points intact. After homeostasis by application of gentle pressure, the skin was apposed with two mattress sutures using 5-0 nylon. Animals were then allowed to recover for 2 or 24 h after surgery, at which time mechanical allodynia was assessed.To test drug effects, rats were first acclimated for 20 min in inverted individual plastic containers (2012.520 cm) on top of a suspended wire mesh grid, and A-836339 was injected intraperitoneally 30 min before testing for mechanical allodynia using calibrated von Frey filaments . von Frey filaments were presented perpendicularly to the plantar surface of the selected hind paw and then held in this position for approximately 8 s, with enough force to cause a slight bend of the filament. Positive responses included an abrupt withdrawal of the hind paw from the stimulus or flinching behavior immediately after removal of the stimulus. A 50% withdrawal threshold was determined using an up-down procedure[1].

Molecular Weight	310.45
Formula	C16H26N2O2S
CAS No.	959746-77-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12 mg/mL (38.65 mM)

References and Literature

1. 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 Pain Models, and Pharmacological Magnetic Resonance Imaging[J]. Journal of Pharmacology and Experimental Therapeutics, 2009, 328(1):141-151. 2. Mcgaraughty S , Chu K M , Yao B , 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[J]. Neuroscience, 2009, 158(4):1652-1661.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Bioactive Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Anti-Fibrosis Compound Library NO PAINS Compound Library Immunology/Inflammation Compound Library Anti-Aging Compound Library

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Keywords

A-836339 959746-77-1 GPCR/G Protein Cannabinoid Receptor A836339 inhibit Inhibitor A 836339 inhibitor

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