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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 25 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
FC(F)(C(O)=O)F.CC1=C(ON=C1C)NS(C2=CC=C(NC(C3=CC(C4=CC=CC=N4)=NC5=C3C=C(C)C=C5C)=O)C=C2)(=O)=O
生化/生理作用
ML193 is a potent and selective piperadinyloxadiazolone antagonist for G protein-coupled receptor (GPCR) GPR55, a receptor for L-α-lysophosphatidylinositol (LPI) which also binds synthetic cannabinoids, and signals through several endogenous pathways. GPR55 is highly abundant in the CNS as well as in intestine, bone marrow, spleen, platelets, immune and endothelial cells. Its role is not completely understood, but has been implicated in inflammatory pain, neuropathic pain, metabolic disorder, bone development, and cancer. Selective antagonists are needed to further elucidate the role of GPR55 in physiology and pathobiology. ML193 (CID1261822) has 221 nM potency for GPR55 and >145-fold, >27-fold and >145-fold antagonist selectivity against GPR35, cannabinoid receptors CB1 and CB2, respectively and >145-fold agonist selectivity against GPR35, CB1 and CB2. ML193 is inhibits the downstream responses of ERK phosphorylation with an IC50 of 65 nM and PKC βII translocation with an IC50 of 10 μM.
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
The Journal of biological chemistry, 288(31), 22481-22492 (2013-07-03)
The L-α-lysophosphatidylinositol (LPI)-sensitive receptor GPR55 is coupled to Ca(2+) signaling. Low levels of GPR55 expression in the heart have been reported. Similar to other G protein-coupled receptors involved in cardiac function, GPR55 may be expressed both at the sarcolemma and
Biochemistry, 52(52), 9456-9469 (2013-11-28)
GPR55 is a class A G protein-coupled receptor (GPCR) that has been implicated in inflammatory pain, neuropathic pain, metabolic disorder, bone development, and cancer. Initially deorphanized as a cannabinoid receptor, GPR55 has been shown to be activated by non-cannabinoid ligands
International journal of molecular sciences, 20(12) (2019-06-20)
Endocannabinoids are key-players of female fertility and potential biomarkers of reproductive dysfunctions. Here, we investigated localization and expression of cannabinoid receptor type-1 and -2 (CB1R and CB2R), G-protein coupled receptor 55 (GPR55), and transient receptor potential vanilloid type 1 channel
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