GW842166X

製品コードS2778 バッチS277801

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₁₇Cl₂F₃N₄O₂

分子量

449.25

CAS No.

666260-75-9

Solubility (25°C)*

体外

DMSO

20 mg/mL (44.51 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.000mg/ml (2.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	GW842166Xは、カンナビノイド受容体CB2の強力で選択性の高いアゴニストであり、EC50は63 nMで、CB1受容体には有意な活性を示しません。フェーズ2。
in vitro	GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63nM, respectively. This compound exhibits full agonist potency with an EC50 of 133 nM and E_max of 101% in cyclase assays. It 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. This compound 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. It 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.
特徴	Possesses selective affinity for CB2 than CB1.

プロトコル(参考用のみ)

キナーゼアッセイ	Determination of cannabinoid CB2 Receptor Agonist Activity
キナーゼアッセイ	GW842166X is prepared as 10 mM stocks in DMSO. EC50 values (the concentration required to produce 50% maximal response) are estimated using dilutions of between 3- and 5-fold into DMSO. This compound in DMSO (1% final assay volume) is transferred into black, clear bottom, microtitre plates from NUNC (96- or 384-well). Cells are suspended at a density of 0.2 OD₁₀₀/ml in SC media lacking histidine, uracil, tryptophan, adenine and leucine and supplemented with 10 mM 3-aminotriazole, 0.1 M sodium phosphate pH 7.0, and 20 M fluorescein di-β-D-glucopyranoside (FDGlu). This mixture (50 μl per well for 384-well plates, 200μl per well for 96-well plates) is added to agonist in the assay plates. After incubation at 30 °C for 24 hours, fluorescence resulting from degradation of FDGlu to fluorescein due to exoglucanase, an endogenous yeast enzyme produced during agonist-stimulated cell growth, is determined using a Spectrofluor microtitre plate reader (excitation wavelength: 485nm; emission wavelength: 535nm). Fluorescence is plotted against compound concentration and iteratively curve fitted using a four parameter fit to generate a concentration effect value.
動物実験	動物モデル	rat model of neuropathic pain
	投薬量	15 mg/kg
	投与方法	Orally administrated once daily for 8 days

参考

https://pubmed.ncbi.nlm.nih.gov/17477516/
https://pubmed.ncbi.nlm.nih.gov/17994110/
http://www.pa2online.org/Vol2Issue4abst050P.pdf

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Integrative discovery of treatments for high-risk neuroblastoma. [ Nat Commun, 2020, 11(1):71]	PubMed: 31900415

Integrative discovery of treatments for high-risk neuroblastoma. [ Nat Commun, 2020, 11(1):71]

PubMed: 31900415

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。