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

CAS: 666260-75-9 Cat. No.: G408958 분자식: C₁₈H₁₇Cl₂F₃N₄O₂ 분자량: 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

개요

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

동의어

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

사양 및 순도

10mM in DMSO

생화학 및 생리적 메커니즘

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.

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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작업 유형

AGONIST

작동 메커니즘

Cannabinoid CB2 receptor agonist

제품 특성

• ALogP: 4.1

이름과 식별자

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

관련 대상(인간)

CNR2 Tchem Cannabinoid receptor 2 (5 Activities)

Discover Target: CNR2

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

화학 및 물리적 특성

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

자주 묻는 질문

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 666260-75-9, the molecular formula is C18H17Cl2F3N4O2, and the molecular weight is 449.25 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.