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GW842166X

Catalog No. T6527   CAS 666260-75-9

GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.

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GW842166X Chemical Structure
GW842166X, CAS 666260-75-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 30.00
2 mg In stock $ 43.00
5 mg In stock $ 70.00
10 mg In stock $ 125.00
25 mg In stock $ 235.00
50 mg In stock $ 348.00
100 mg In stock $ 518.00
1 mL * 10 mM (in DMSO) In stock $ 68.00
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Purity: 99.88%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.
Targets&IC50 CB2:63 nM(EC50)
In vitro GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63 nM, respectively. [1] GW-842166X exhibits full agonist potency with an EC50 of 133 nM and Emax of 101% in cyclase assays. GW-842166X exhibits weak agonist potency with an EC50 of 7.780 μM and Emax of 84% in FLIPR assays. [2]
In vivo GW842166X has an oral bioavailability of 58% and a half-life of 3 h when dosed orally in the rat. GW842166X has extremely high potency with an oral ED50 of 0.1 mg/kg and shows full reversal of hyperalgesia at 0.3 mg/kg in the FCAa model of inflammatory pain. [1] GW842166X orally administrated at a dose of 15 mg/kg for 8 days produced a significant reversal of the CCI induced decrease in paw withdrawal threshold in a rat model of neuropathic pain. [3]
Molecular Weight 449.25
Formula C18H17Cl2F3N4O2
CAS No. 666260-75-9

Storage

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

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 16 mg/mL (35.6 mM)

TargetMolReferences and Literature

1. Giblin GM, et al. J Med Chem, 2007, 50(11), 2597-2600. 2. Yao BB, et al. Br J Pharmacol, 2008, 153(2), 390-401. 3. Clayton NM, et al. Proceedings of the British Pharmacological Society at https://www.pA2online.org/Vol2Issue4abst050P.html

TargetMolCitations

1. He Y, Jia H, Yang Q, et al.Specific Activation of CB2R Ameliorates Psoriasis-Like Skin Lesions by Inhibiting Inflammation and Oxidative Stress.Inflammation.2023: 1-17.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Target-Focused Phenotypic Screening Library Neuronal Signaling Compound Library NO PAINS Compound Library Anti-Fibrosis Compound Library Bioactive Compound Library Clinical Compound Library Bioactive Compounds Library Max Drug Repurposing Compound Library

Related Products

Related compounds with same targets
CB2R/FAAH modulator-2 CB1 antagonist 2 EHP-101 2,3-Butanediol CB1-IN-1 Taranabant BAY 38-7271 Rimonabant hydrochloride

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Keywords

GW842166X 666260-75-9 GPCR/G Protein Cannabinoid Receptor inhibit GW-842166X Inhibitor inhibitor

 

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