GW 405833

SKU: orb1299576

Description

GW 405833, also known as L-768242, is a selective cannabinoid CB2 receptor agonist. This research compound is utilized in both in vitro and in vivo studies to investigate CB2 receptor function in fields such as immunology, inflammation, and neuropathic pain research.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	180002-83-9
MW	447.35
Purity	99.93% (May vary between batches)
Formula	C₂₃H₂₄Cl₂N₂O₃
SMILES	COc1ccc2n(C(=O)c3cccc(Cl)c3Cl)c(C)c(CCN3CCOCC3)c2c1
Target	Cannabinoid Receptor
Solubility	DMSO:10 mg/mL (22.35 mM)

Bioactivity

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Target IC50	CB1:16.1 μM (EC50)\|CB2:50.7 nM (EC50)
In Vivo	GW405833 (3, 10, and 30 mg/kg i.p.) dose dependently reversed established mechanical allodynia in both pain models in WT mice; however, the antiallodynic effects of GW405833 were fully preserved in CB2KO mice and absent in CB1KO mice. Furthermore, the antiallodynic efficacy of GW405833 (30 mg/kg i.p.) was completely blocked by the CB1 antagonist rimonabant (10 mg/kg i.p.) but not by the CB2 antagonist SR144528 (10 mg/kg i.p.). Thus, the antinociceptive properties of GW405833 are dependent on CB1 receptors. GW405833 (30 mg/kg i.p.) was also inactive in a tetrad of tests measuring cardinal signs of CB1 activation. Additionally, unlike rimonabant (10 mg/kg i.p.), GW405833 (10 mg/kg, i.p.) did not act as a CB1 antagonist in vivo to precipitate withdrawal in mice treated chronically with Δ9-tetrahydrocannabinol. Read more...
Animal Research	Baseline mechanical paw withdrawal thresholds were measured in each paw for each animal before performing either PSNL or injecting CFA. Another predrug baseline was then taken after painful peripheral neuropathy or inflammatory pain was fully established. GW405833 was administered (i.p.) 30 minutes before evaluation of the impact of drug manipulations on mechanical paw withdrawal thresholds. Different doses of GW405833 were injected (i.p.) within subjects in the order of vehicle (0), 3, 10, and 30 mg/kg. Sufficient time was allowed to lapse between each dose to verify that mechanical paw withdrawal thresholds returned to the predrug levels before dose escalation. . In the groups where CB1 or CB2 antagonists were tested, rimonabant or SR144528 (10 mg/kg i.p.) was administered 20 minutes before GW405833 injection. Read more...

Storage & Handling

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Storage	keep away from moisture \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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GW 405833, GW405833, GW-405833, Inhibitor, L768242, L-768242, L 768242, inhibit, neuropathic pain, CannabinoidReceptor, Cannabinoid Receptor, anti-inflammatory, CB2

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Compound Identifiers

PubChem CID

9911463 ↗

Key Properties

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No computed properties available.

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GW 405833 (orb1299576)

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GW 405833

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

Request a Document

Protocol Information

GW 405833 (orb1299576)

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