CID 16020046

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CID16020046 是一种选择性 GPR55 拮抗剂，在酵母中抑制 GPR55 组成型活性，IC50 为 0.15 μM。

CID16020046 is a selective GPR55 inverse agonist. CID16020046 is a G protein-coupled receptor that is weakly activated by some cannabinoids at nM concentrations. CID16020046 has been shown to block GPR55-mediated endothelial wound healing and reverse LPI-inhibited platelet aggregation.(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.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.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.CID16020046 (2.5 μM) antagonizes GPR55-mediated activation and nuclear translocation of transcription factors but has no effect on CB1-mediated CREB activation.Pretreatment CID16020046 (1 μM) abolished the LPI-induced stimulation of wound healing in HMVEC-Ls.

Western Blot Analysis Cell Line:HEK-CB1 and HEK-CB2 cells 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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CID16020046 | CID-16020046

Others

Other Targets

GPR55

Others-Field

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834903-43-4

425.44

C25H19N3O4

>98% (HPLC)

DMSO : ≥ 28 mg/mL; 65.81 mM

CC1=CC=C(C=C1)C2=NNC3=C2C(N(C3=O)C4=CC=C(C=C4)C(=O)O)C5=CC(=CC=C5)O

4-[4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1,4-dihydropyrrolo[3,4-d]pyrazol-5-yl]benzoic acid

(-20℃)

With Ice Pack

≥ 2 years