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Fosgonimeton Sale

(Synonyms: 肝细胞生长因子受体激动剂多肽,ATH-1017) 目录号 : GC64708

Fosgonimeton (ATH-1017) 是一种肝细胞生长因子受体激动剂 (WO2017210489)。

Fosgonimeton Chemical Structure

Cas No.:2093305-05-4

规格 价格 库存 购买数量
5 mg
¥4,050.00
现货
10 mg
¥7,200.00
现货

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产品描述

Fosgonimeton (ATH-1017) is a hepatocyte growth factor receptor agonist (WO2017210489)[1].

Fosgonimeton is a hepatocyte growth factor receptor agonist[1].

肝细胞生长因子受体激动剂

[1]. WO2017210489

Chemical Properties

Cas No. 2093305-05-4 SDF Download SDF
别名 肝细胞生长因子受体激动剂多肽,ATH-1017
分子式 C27H45N4O8P 分子量 584.64
溶解度 DMSO : 125 mg/mL (213.81 mM; Need ultrasonic) 储存条件 Store at -20°C, protect from light, stored under nitrogen
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1 mg 5 mg 10 mg
1 mM 1.7105 mL 8.5523 mL 17.1045 mL
5 mM 0.3421 mL 1.7105 mL 3.4209 mL
10 mM 0.171 mL 0.8552 mL 1.7105 mL
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Research Update

Fosgonimeton, a Novel Positive Modulator of the HGF/MET System, Promotes Neurotrophic and Procognitive Effects in Models of Dementia

Neurotherapeutics 2022 Dec 20.PMID:36538176DOI:10.1007/s13311-022-01325-5.

All types of dementia, including Alzheimer's disease, are debilitating neurodegenerative conditions marked by compromised cognitive function for which there are few effective treatments. Positive modulation of hepatocyte growth factor (HGF)/MET, a critical neurotrophic signaling system, may promote neuronal health and function, thereby addressing neurodegeneration in dementia. Here, we evaluate a series of novel small molecules for their ability to (1) positively modulate HGF/MET activity, (2) induce neurotrophic changes and protect against neurotoxic insults in primary neuron culture, (3) promote anti-inflammatory effects in vitro and in vivo, and (4) reverse cognitive deficits in animal models of dementia. Through screening studies, the compound now known as fosgonimeton-active metabolite (fosgo-AM) was identified by use of immunocytochemistry to be the most potent positive modulator of HGF/MET and was selected for further testing. Primary hippocampal neurons treated with fosgo-AM showed enhanced synaptogenesis and neurite outgrowth, supporting the neurotrophic effects of positive modulators of HGF/MET. Additionally, fosgo-AM protected against neurotoxic insults in primary cortical neuron cultures. In vivo, treatment with fosgo-AM rescued cognitive deficits in the rat scopolamine amnesia model of dementia. Although fosgo-AM demonstrated several procognitive effects in vitro and in vivo, a prodrug strategy was used to enhance the pharmacological properties of fosgo-AM, resulting in the development of Fosgonimeton (ATH-1017). The effect of Fosgonimeton on cognition was confirmed in a lipopolysaccharide (LPS)-induced neuroinflammatory mouse model of dementia. Together, the results of these studies support the potential of positive modulators of HGF/MET to be used as novel therapeutics and suggest the drug candidate Fosgonimeton might protect against neurodegeneration and be therapeutic in the management of Alzheimer's disease and other types of dementia.

Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Positive Modulator of HGF/MET, Fosgonimeton, in Healthy Volunteers and Subjects with Alzheimer's Disease: Randomized, Placebo-Controlled, Double-Blind, Phase I Clinical Trial

J Alzheimers Dis 2022;86(3):1399-1413.PMID:35180125DOI:10.3233/JAD-215511.

Background: Fosgonimeton (ATH-1017) is being developed as a first-in-class regenerative therapy for people with Alzheimer's disease (AD) and dementia; potentially improving dementia symptoms and altering disease progression by reversing synaptic disconnection and neuronal loss. Objective: This randomized, double-blind, placebo-controlled phase I trial (NCT03298672) evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of Fosgonimeton. Methods: Fosgonimeton was administered once daily via subcutaneous injection to 88 subjects. The single ascending dose study enrolled healthy young male subjects (n = 48; age, 33.4±6.3 years; dose, 2, 6, 20, 40, 60, or 90 mg); the multiple ascending dose study enrolled healthy elderly subjects (n = 29; age, 63.8±4.0 years; dose, 20, 40, 60, or 80 mg; 9-day duration); and the fixed-dose study enrolled AD subjects (n = 11; age, 69.2±7.1 years; dose, 40 mg; 9-day duration). Quantitative electroencephalogram (qEEG) and event-related potential (ERP) P300 measured neurophysiological signals following Fosgonimeton treatment, supporting brain penetration and target engagement. Results: Fosgonimeton and placebo were shown to be safe and well-tolerated across all doses. Pharmacokinetic results for Fosgonimeton were dose-proportional, with no sex effect or accumulation over 9 days. The main effect of Fosgonimeton on qEEG was acute and sustained gamma power induction. In AD subjects, there was a significant effect toward ERP P300 latency normalization compared with placebo (p = 0.027; n = 7 at 40 mg Fosgonimeton versus n = 4 placebo). Conclusion: These results support the continued development of Fosgonimeton as a novel therapeutic for people with AD and dementia. The fast-onset normalization of ERP P300 latency in AD subjects suggests enhancement of synaptic function and potential procognitive effects.