CID 16020046 是一种有效的,选择性GPR55拮抗剂,抑制 GPR55 的组成型活性,IC50为 0.15 μM。CID 16020046 抑制 GPR55 介导的 Ca2+信号传导和 GPR55 介导的 ERK1/2 磷酸化。CID 16020046 降低了内皮细胞的伤口愈合,并参与了血小板功能的调节。
生物活性 | CID 16020046 is a potent and selectiveGPR55antagonist and inhibitsGPR55constitutive activity with anIC50of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca2+signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function[1]. |
体外研究 (In Vitro) | CID 16020046 has weak activities close for inhibition of the acetylcholinesterase (pIC50=4.4), antagonism of the m-opioid receptor (pIC50=4.6), and blockade of KCNH2, the hERG channel (pIC50=4.6) 6 in human embryonic kidney (HEK)-G protein–coupled receptor 55 (GPR55) cells[1]. CID 16020046 (2.5 μM; for ≥25 minutes) significantly inhibits the lysophosphatidylinositol (LPI; 2.5 μM) induced ERK1/2 phosphorylation. CID 16020046 alone fails to induce intracellular Ca2+release in HEK-GPR55, HEKCB1 cells and shows no ERK1/2 phosphorylation[1]. Pretreatment with CID16020046 (0.01, 0.1, 1, 10 μM) leads to a concentration-dependent decrease in GPR55-mediated NFAT activation, NF-kB activation, and SRE induction in response to 1 μM LPI or GSK319197A in HEKGPR55 and HEK-CB1 cells[1]. CID16020046 (2.5 μM) antagonizes GPR55-mediated activation and nuclear translocation of transcription factors but has no effect on CB1-mediated CREB activation[1]. Pretreatment CID16020046 (1 μM) abolished the LPI-induced stimulation of wound healing in HMVEC-Ls[1].
Western Blot Analysis Cell Line: | HEK-CB1 and HEK-CB2 cells[1] | Concentration: | 2.5 μM | Incubation Time: | For ≥25 minutes | Result: | Significantly inhibited the LPI (2.5 μM) induced ERK1/2 phosphorylation. Treatment alone showed no ERK1/2 phosphorylation and did not alter WIN55,212-2 (2.5 μM) induced ERK1/2 phosphorylation in HEK-CB1 and HEK-CB2 cells. |
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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 | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(235.05 mM;Need ultrasonic) 配制储备液 1 mM | 2.3505 mL | 11.7525 mL | 23.5051 mL | 5 mM | 0.4701 mL | 2.3505 mL | 4.7010 mL | 10 mM | 0.2351 mL | 1.1753 mL | 2.3505 mL |
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此方案可获得 ≥ 2.5 mg/mL (5.88 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.88 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.88 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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