GW842166X - 10mM in DMSO , Cannabinoid CB2 receptor agonist, CAS No.666260-75-9, Cannabinoid CB2 receptor agonist

CAS: 666260-75-9 Cat. No.: G408958 Molecular Weight: 449.25

GRADE & PURITY 10mM in DMSO

Synonyms

2-(2,4-dichlorophenylamino)-N-((tetrahydro-2H-pyran-4-yl)methyl)-4-(trifluoromethyl)pyrimidine-5-carboxamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

GW842166X is a potent and highly selective agonist ofcannabinoid receptor CB2receptor withEC50of 63 nM, shows no significant activity at CB1 receptor. Phase 2.
In vitro

GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63nM, respectively. GW-842166X exhibits full agonist potency with an EC50 of 133 nM and E_max of 101% in cyclase assays. GW-842166X exhibits weak agonist potency with an EC50 of 7.780 μM and E_max of 84% in FLIPR assays.

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. 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.
Cell Data

cell lines：SkBr3 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

2-(2, 4-dichlorophenylamino)-N-((tetrahydro-2H-pyran-4-yl)methyl)-4-(trifluoromethyl)pyrimidine-5-carboxamide

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

AGONIST

Mechanism of action

Cannabinoid CB2 receptor agonist

Product Properties

• ALogP: 4.1

Names and Identifiers

• Isomeric SMILES: C1COCCC1CNC(=O)C2=CN=C(N=C2C(F)(F)F)NC3=C(C=C(C=C3)Cl)Cl
• Molecular Weight: 449.25
• Reaxy-Rn: 11038408
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11038408&ln=

Associated Targets(Human)

CNR2 Tchem Cannabinoid receptor 2 (5 Activities)

Discover Target: CNR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 69 mg/mL (199.15 mM)