SML3466
JHU37160
≥98% (HPLC)
Synonym(s):
8-Chloro-11-(4-ethylpiperazin-1-yl)-4-fluoro-5H-dibenzo[b,e][1,4]diazepine, J60, JH60, JHU 37160, JHU-37160
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About This Item
Empirical Formula (Hill Notation):
C19H20ClFN4
CAS Number:
Molecular Weight:
358.84
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
SMILES string
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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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