ChemicalBook CAS DataBase List 2093305-05-4

2093305-05-4

Name	L-Isoleucinamide, O-(phosphono-κO)-N-(1-oxohexyl)-L-tyrosyl-N-(6-amino-6-oxohexyl)-
CAS	2093305-05-4
Molecular Formula	C27H45N4O8P
Molecular Weight	584.65
MOL File	2093305-05-4.mol

Chemical Properties

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

Safety Data

Symbol(GHS)	GHS07,GHS05,GHS09,GHS06
Signal word	Danger
Hazard statements	H311-H314-H411-H302
Precautionary statements	P280-P302+P352-P312-P322-P361-P363-P405-P501-P260-P264-P280-P301+P330+P331-P303+P361+P353-P363-P304+P340-P310-P321-P305+P351+P338-P405-P501-P264-P270-P301+P312-P330-P501

Hazard Information

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.

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.

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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