| Identification | Back Directory | [Name]
1H-Imidazole-2-carboxamide, 4-[2-(2-chloro-3-methyl-4-pyridinyl)ethynyl]-5-methyl-1-(3-pyridinyl)- | [CAS]
2648837-04-9 | [Synonyms]
RO-275
1H-Imidazole-2-carboxamide, 4-[2-(2-chloro-3-methyl-4-pyridinyl)ethynyl]-5-methyl-1-(3-pyridinyl)- | [Molecular Formula]
C18H14ClN5O | [MOL File]
2648837-04-9.mol | [Molecular Weight]
351.79 |
| Chemical Properties | Back Directory | [Boiling point ]
647.8±65.0 °C(predicted) | [density ]
1.33±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
14.88±0.50(predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
RO-275 (compound 29) is a potent, selective and orally active HCN1 inhibitor with IC50 values of 0.046, 14.3, 4.6, 13.9 μM for HCN1, HCN2, HCN3, HCN4, respectively. RO-275 rescues decremented working memory. RO-275 has the potential for the research of cognitive dysfunction in brain disorder[1][2]. | [in vivo]
RO-275 (3, 10, 30 mg/kg; i.p.) rescues decremented working memory in rats[2]. | Animal Model: | Male Sprague Dawley rats[2] | | Dosage: | 3, 10, 30 mg/kg | | Administration: | I.p. | | Result: | Improved performance in a translationally relevant touchscreen task of working memory (WM), tended to improve performance, but only at the longest delay of 6 s at the 10 mg/kg dose level, and led to a significant reduction in incorrect trials at 30 mg/kg in trial-unique, delayed non-matching-to-location (TUNL). |
| [References]
[1] Bjoern Bartels, et al. Alkynyl-(heteroaryl)-carboxamide hcn1 inhibitors. WO2021110574A1.
[2] Harde E, et al. Selective and brain-penetrant HCN1 inhibitors reveal links between synaptic integration, cortical function, and working memory. Cell Chem Biol. 2024 Mar 21;31(3):577-592.e23. DOI:10.1016/j.chembiol.2023.11.004 |
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