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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
Fc1c2c(ccc1)C(=Nc4c(ccc(c4)Cl)N2)N3CCN(CC3)CC
InChI
1S/C19H20ClFN4/c1-2-24-8-10-25(11-9-24)19-14-4-3-5-15(21)18(14)22-16-7-6-13(20)12-17(16)23-19/h3-7,12,22H,2,8-11H2,1H3
InChI key
SWSCWOSASZXIRK-UHFFFAOYSA-N
生化/生理作用
JHU37160 (J60) is a potent DREADDs (Designer Receptors Exclusively Activated by Designer Drugs) ligand (hM3Dq/hM4Di Ki = 1.9/3.6 nM using mouse brain tissue, 18.5/0.2 nM by celluar BRET assays) with ~25-fold improved affinity than C21 and high in vivo potency for CNS applications. J60 selectively competes against clozapine at DREADDs, but not other clozapine-binding sites in mouse brain tissue ex vivo (10 nM), increases hM3Dq-stimulated locomotion in TH-hM3Dq rats (0.01-0.3 mg/kg i.p.) and selectively inhibits locomotor activity of D1-hM3Dq and D1-hM4Di transgenic, but not wild-type, mice (0.01-1 mg/kg i.p.).
Potent DREADDs (Designer Receptors Exclusively Activated by Designer Drugs) ligand with greatly improved affinity than C21 and in vivo CNS potency.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
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历史批次信息供参考:
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