| Identification | Back Directory | [Name]
10H-Phenothiazine-3,7-diamine, N3,N3,N7,N7-tetraethyl-, hydrochloride (1:2) | [CAS]
951131-13-8 | [Synonyms]
10H-Phenothiazine-3,7-diamine, N3,N3,N7,N7-tetraethyl-, hydrochloride (1:2) |
| Hazard Information | Back Directory | [Uses]
LETC is an orally active α-synuclein (α-Syn) aggregation inhibitor with an EC50 of 66 nM in transfected DH60.21 neuroblastoma cells. LETC can cross the blood-brain barrier. LETC can be used for the study of synucleinopathies[1]. | [in vivo]
LETC (10 mg/kg; po; for 5 days per week; for 6 weeks) significantly decreases α-Syn-positive neurons in multiple brain regions and this resulted in a rescue of movement deficits in the open field in these mice. LETC does not improve activity deficits of L62 mice in the home cage environment[1].
In α-Syn transgenic L62 mice, LETC accumulated in the brain with a half-life of about 6 h after oral administration[1].
Pharmacokinetic parameters obtained in L62 mice after a single oral dose of LETC (15 mg/kg).
1.19 | parameter | Plasma | Brain | | Cmax (ng/mL) | 155.0 | 1013.5 | | Tmax (h) | 1.0 | 1.0 |
| Animal Model: | Full-length human α-Syn overexpressing Line 62 (L62) mice mice[1] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage; for 5 days per week; for 6 weeks | | Result: | Significantly decreased α-Syn-positive neurons in multiple brain regions. |
| [IC 50]
α-synuclein Aggregation | [References]
[1] Karima Schwab, et al. LETC inhibits α-Syn aggregation and ameliorates motor deficiencies in the L62 mouse model of synucleinopathy. Eur J Pharmacol. 2024 May 5:970:176505. DOI:10.1016/j.ejphar.2024.176505 |
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