R243|688352-84-3|-陌孚医药/Medlife

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R243

目录号: PL02531 纯度: ≥98%

CAS No. :688352-84-3

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中文名称	R243
英文名称	R243
英文别名	R243;7,8-Dihydro-7-[2-(tricyclo[3.3.1.1(3,7)]dec-1-yloxy)ethyl]-6H-1,3-dioxolo[4,5-g][1,3]benzoxazine;STK404917;ST50641739;7-[2-(1-adamantyloxy)ethyl]-7,8-dihydro-6H-[1,3]dioxolo[4,5-g][1,3]benzoxazine;2-(2H,6H,8H-1,3-oxazaperhydroino[5',6'-1,2]benzo[4,5-d]1,3-dioxolen-7-yl)-1-ad amantanyloxyethane;7-[2-(tricyclo[3.3.1.1~3,7~]dec-1-yloxy)ethyl]-7,8-dihydro-6H-[1,3]dioxolo[4,5-g][1,3]benzoxazine
Cas No.	688352-84-3
分子式	C₂₁H₂₇NO₄
分子量	357.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	R243 是一种有效的选择性的 CCR8 拮抗剂。R243 可抑制 CCL₁/CCR8 的相互作用，并抑制 CCR8 信号传导和趋化性。R243 具有抗伤害感受和抗炎作用。
生物活性	R243 is a potent and selective CCR8 antagonist. R243 inhibits CCL 1 /CCR8 interaction and inhibits CCR8 signaling and chemotaxis. R243 has antinociceptive and anti-inflammatory effects.
性状	Solid
IC50 & Target[1][2]	CCR8
体外研究(In Vitro)	R243 has CCR8-antagonistic effects on CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation. R243 attenuates secretion of TNF-α, IL-6, and most strikingly IL-10 from wild-type peritoneal macrophages (WT PMφ). R243-treated WT PMφ shows suppressed c-jun N-terminal kinase activity and NF-κB signaling after lipopolysaccharide (LPS) treatment when compared with WT PMφ. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	R243 (0.1-1 mg/kg; intraperitoneal injection; once; male Swiss mice) treatment inhibits the analgesic effect evoked by CCL 1 in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Tomoyuki Oshio, et al. Chemokine Receptor CCR8 Is Required for Lipopolysaccharide-Triggered Cytokine Production in Mouse Peritoneal Macrophages. PLoS One. 2014 Apr 8;9(4):e94445. [2]. Mario García-Domínguez, et al. The Systemic Administration of the Chemokine CCL1 Evokes Thermal Analgesia in Mice Through the Activation of the Endocannabinoid System. Cell Mol Neurobiol. 2019 Nov;39(8):1115-1124.

溶解度数据	In Vitro: DMSO : 125 mg/mL (349.71 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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