CID16020046

製品コードS8694 バッチS869401

印刷

化学情報

Synonyms

C390-0219

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₅H₁₉N₃O₄

分子量

425.44

CAS No.

834903-43-4

Solubility (25°C)*

体外

DMSO

85 mg/mL (199.79 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。	4.250mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 85 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	CID16020046 (C390-0219) は、酵母において0.15 μMのIC50でGPR55の構成的活性を阻害する選択的なGPR55アンタゴニストです。それは、他のGPCR、イオンチャネル、キナーゼ、および核内受容体の幅広いスペクトルに対して弱い活性を示します。
in vitro	In yeast cells expressing human GPR55, CID16020046 antagonized agonist-induced receptor activation. In human embryonic kidney (HEK293) cells stably expressing human GPR55, this compound behaved as an antagonist on LPI-mediated Ca2+ release and extracellular signal-regulated kinases activation, but not in HEK293 cells expressing cannabinoid receptor 1 or 2 (CB1 or CB2). It concentration dependently inhibited lysophosphatidylinositol (LPI)-induced activation of nuclear factor of activated T-cells (NFAT), nuclear factor κ of activated B cells (NF-κB) and serum response element, translocation of NFAT and NF-κB, and GPR55 internalization.
in vivo	CID16020046 improves inflammation in models of intestinal inflammation and reduces proinflammatory cytokines. This compound does not change the locomotor and anxiety behavior of healthy mice.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	J774A.1 cells
	濃度	1, 5 and 10 μM
	反応時間	30 min
	実験の流れ	2 × 10⁶ cells were transferred into 500 μL PBS and preincubated for 30 mins with 1, 5, and 10 μM CID16020046 or vehicle (DMSO). Cells were then stimulated with 1 nM of monocyte chemotactic protein 1 (MCP-1) for another 30 mins at 37°C. Alexa Fluor 647 anti-mouse CD11b was added 15 min before the end of the incubation time. After adding the fixative solution, cells were measured on a FACSCalibur flow cytometer. Experiments were performed in triplicates and data were expressed as percentage change to the vehicle treatment.
動物実験	動物モデル	C57BL/6 mice
	投薬量	20 mg/kg
	投与方法	s.c.

参考

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4587547/
https://pubmed.ncbi.nlm.nih.gov/23639801/

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：

Cannabidiol and positive effects on object recognition memory in an in vivo model of Fragile X Syndrome: Obligatory role of hippocampal GPR55 receptors [ Pharmacol Res, 2024, 203:107176]	PubMed: 38583687

Cannabidiol and positive effects on object recognition memory in an in vivo model of Fragile X Syndrome: Obligatory role of hippocampal GPR55 receptors [ Pharmacol Res, 2024, 203:107176]

PubMed: 38583687

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。