| Identification | Back Directory | [Name]
L-Isoleucinamide, O-(phosphono-κO)-N-(1-oxohexyl)-L-tyrosyl-N-(6-amino-6-oxohexyl)- | [CAS]
2093305-05-4 | [Synonyms]
ATH-1017
Fosgonimeton
Fosgonimeton（ATH-1017）
L-Isoleucinamide, O-(phosphono-κO)-N-(1-oxohexyl)-L-tyrosyl-N-(6-amino-6-oxohexyl)- | [Molecular Formula]
C27H45N4O8P | [MOL File]
2093305-05-4.mol | [Molecular Weight]
584.65 |
| Chemical Properties | Back Directory | [density ]
1.212±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C, protect from light, stored under nitrogen | [solubility ]
DMSO : 125 mg/mL (213.81 mM; Need ultrasonic) | [form ]
Solid | [pka]
1.27±0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Fosgonimeton (ATH-1017) is a hepatocyte growth factor receptor (c-Met/HGFR) agonist. Fosgonimeton has neuroprotective effects in both LPS (HY-D1056) -induced neuroinflammation and Aβ-induced AD models[1][2][3][4]. | [in vivo]
Fosgonimeton (0.125-2 mg/kg; Subcutaneous injection; 14 days) improves cognitive dysfunction in rat models of AD induced by Aβ[2].
Fosgonimeton (0.125-1.25 mg/kg; Subcutaneous injection; 14 days) improves cognitive impairment in a LPS (HY-D1056) -induced neuroinflammation model of dementia mice[3]. | Animal Model: | Aβ peptides treated adult male Wistar rats (approximately 210 g)[2] | | Dosage: | 0.125 mg/kg, 0.25 mg/kg, 0.5 mg/kg, 1 mg/kg and 2 mg/kg | | Administration: | Subcutaneous injection (s.c.); 14 days | | Result: | Significantly restored cognitive function at all doses tested.
The maximum average degree of recovery was 88% recovery in 0.125 mg/kg treated group.
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| Animal Model: | LPS (HY-D1056) treated CD-1 mice aged four to five weeks old[3] | | Dosage: | 0.125 mg/kg, 0.25 mg/kg, 0.5 mg/kg and 1.25 mg/kg | | Administration: | Subcutaneous injection (s.c.); 14 days | | Result: | Significantly ameliorated cognitive deficits at all doses tested, except for the lowest dose (0.125 mg/kg) tested.
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| [References]
[1] Reda S, et al. Fosgonimeton, a novel, small molecule positive modulator of the HGF/MET system is neuroprotective in primary neuron culture. Alzheimer's Dement. 2022 18: e065874.
[2] Reda SM, et al. Fosgonimeton attenuates amyloid-beta toxicity in preclinical models of Alzheimer's disease. Neurotherapeutics. 2024 Jul;21(4):e00350. DOI:10.1016/j.neurot.2024.e00350
[3] Johnston JL, et al. Fosgonimeton, a Novel Positive Modulator of the HGF/MET System, Promotes Neurotrophic and Procognitive Effects in Models of Dementia. Neurotherapeutics. 2023 Mar;20(2):431-451. DOI:10.1007/s13311-022-01325-5
[4] Leen H. KAWAS, et al. WO2017210489. 2021. |
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