SML3466

JHU37160

≥98% (HPLC)

• Synonym(e): 8-Chloro-11-(4-ethylpiperazin-1-yl)-4-fluoro-5H-dibenzo[b,e][1,4]diazepine, J60, JH60, JHU 37160, JHU-37160
• Empirische Formel (Hill-System): C₁₉H₂₀ClFN₄
• CAS-Nummer: 2369979-68-8
• Molekulargewicht: 358.84
• MDL-Nummer: MFCD34167517
• UNSPSC-Code: 51111800
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: -10 to -25°C
• 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

Beschreibung

Biochem./physiol. Wirkung

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.).

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable