JN0002

Loreclezole

≥98% (HPLC)

• Synonym(s): 1-[(1Z)-2-Chloro-2-(2,4-dichlorophenyl)ethenyl]-1H-1,2,4-triazole, 1-[(Z)-2-Chloro-2-(2,4-dichlorophenyl)vinyl]-1,2,4-triazole, R 72063, R-72063, R72063
• Empirical Formula (Hill Notation): C₁₀H₆Cl₃N₃
• CAS Number: 117857-45-1
• Molecular Weight: 274.53
• UNSPSC Code: 12352202
• NACRES: NA.77
• MDL number: MFCD00865331
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: room temp
• SMILES string: Cl/C(C1=CC=C(Cl)C=C1Cl)=C\N2N=CN=C2
• InChI: 1S/C10H6Cl3N3/c11-7-1-2-8(9(12)3-7)10(13)4-16-6-14-5-15-16/h1-6H/b10-4-
• InChI key: XGLHZTBDUXXHOM-WMZJFQQLSA-N

Description

Biochem/physiol Actions

Loreclezole (R72063) is a sedative and anticonvulsant that exerts subtype-selective positive allosteric modulator (PAM) potency toward beta2 (β₂)- or β₃-containing GABA_A gamma-aminobutyric acid (GABA) receptors (% potentiation by 1 μM Loreclezole of GABA EC20-stimulated current/human α₁βγ₂ = 100/α₁β₂γ₂, 120/α₁β₃γ₂, 13/α₁β₁γ₂; α₁β₂γ₂ EC50 = 1 μM) with >300-fold lower β₁ affinity, while acting as a negative allosteric modulator (NAM) against the homomeric rho1 (ρ1) GABA_A-rho receptor (rat GABA_C IC50 = 0.5 μM against GABA EC10-induced current).

Sedative & anticonvulsant with beta2-/beta3- (β₂-/β₃-) selective GABA_A receptor PAM and GABA_C (GABA_A-rho receptor) NAM activity.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable