| Identification | Back Directory | [Name]
1H-Benzimidazole-5-carboxamide, N-[2-(2-hydroxyethoxy)ethyl]-1-methyl-2-[[6-(trifluoromethyl)-2-benzothiazolyl]amino]- | [CAS]
1325721-55-8 | [Synonyms]
1H-Benzimidazole-5-carboxamide, N-[2-(2-hydroxyethoxy)ethyl]-1-methyl-2-[[6-(trifluoromethyl)-2-benzothiazolyl]amino]- | [Molecular Formula]
C21H20F3N5O3S | [MOL File]
1325721-55-8.mol | [Molecular Weight]
479.48 |
| Hazard Information | Back Directory | [Uses]
HPPE (compound 236) is an orally active, potential Bach1 inhibitor. Bach1 is a transcription factor of the cap'n'collar type alkaline region leucine zipper factor family (CNC-bZip) that regulates mitochondrial metabolism and reduces glucose utilization. HPPE can be used for research in psoriasis, multiple sclerosis, and COPD[1][2][3][4]. | [in vivo]
HPPE (5 and 10 mg/kg, oral gavage, twice a day for 6 days) ameliorates MPTP-induced dopaminergic neurodegeneration and associated oxidative stress and neuroinflammation in the acute MPTP mouse model[3].
| Animal Model: | The acute MPTP mouse model[2] | | Dosage: | 5 and 10 mg/kg | | Administration: | oral gavage, twice a day for 6 days | | Result: | Significantly protected SNpc dopaminergic neurons against MPTP neurotoxicity. |
| [References]
[1] Attucks, et al. Bach 1 inhibitors in combination with Nrf2 activators and pharmaceutical compositions thereof. World Intellectual Property Organization, WO2016089648 A1 2016-06-09.
[2] Zhang X, et al. Bach1: Function, Regulation, and Involvement in Disease. Oxid Med Cell Longev. 2018 Oct 2;2018:1347969. DOI:10.1155/2018/1347969
[3] Ahuja M, et al. Bach1 derepression is neuroprotective in a mouse model of Parkinson's disease. Proc Natl Acad Sci U S A. 2021 Nov 9;118(45):e2111643118. DOI:10.1073/pnas.2111643118
[4] Freeman R, et al. HPPE Activates NRF2 Signaling by Liberating Heavy Metal Stores. Chembiochem. 2024 Sep 6:e202400529. DOI:10.1002/cbic.202400529 |
|
|