| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
HGF Receptor[1]
Fosgonimeton targets the hepatocyte growth factor receptor (c-Met/HGFR). It acts as an agonist, enhancing the interaction of HGF with its receptor tyrosine kinase MET. This activation of the HGF/MET neurotrophic system reverses synaptic disconnection and neuronal loss. By modulating this pathway, it aims to improve dementia symptoms and potentially alter disease progression. |
|---|---|
| ln Vitro |
Hepatocyte growth factor receptor agonist fosgonimeton[1].
In vitro, Fosgonimeton has demonstrated neuroprotective effects in both LPS-induced neuroinflammation and Aβ-induced AD models. Its activity is assessed in neuronal cell cultures subjected to these stress conditions. These studies confirm its ability to protect neurons from inflammatory and amyloid-beta-induced damage. |
| ln Vivo |
agonist of the hepatocyte growth factor receptor
In vivo, Fosgonimeton has been studied in animal models of Alzheimer's disease. Its ability to cross the blood-brain barrier and enhance HGF/MET signaling supports its potential to reverse synaptic disconnection and neuronal loss. These studies provide evidence for its therapeutic potential in neurodegenerative diseases. |
| Enzyme Assay |
Cell-free assays for Fosgonimeton typically involve measuring its binding affinity and agonist activity at the c-Met receptor. These assays may use recombinant c-Met protein in ELISA or SPR formats. Additionally, cell-free kinase activity assays are used to measure the compound's ability to stimulate c-Met autophosphorylation.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the neuroprotective activity of Fosgonimeton. Neuronal cell lines or primary neurons are treated with the compound in the presence of inflammatory or amyloid-beta insults. Cell survival and markers of neuroinflammation are measured to assess the compound's protective effects.
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| Animal Protocol |
In vivo animal experiments typically involve rodent models of Alzheimer's disease or other neurodegenerative conditions. Animals are administered Fosgonimeton. Cognitive function is assessed using behavioral tests, and markers of synaptic integrity and neuroinflammation are measured in brain tissues. These studies provide evidence for the compound's neuroprotective effects.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Fosgonimeton are characterized by its rapid conversion to the active metabolite ATH-1001 in plasma. This prodrug approach is designed to enhance the delivery and bioavailability of the active compound. Its ability to cross the blood-brain barrier is a key feature for its central nervous system activity.
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| Toxicity/Toxicokinetics |
The toxicity profile of Fosgonimeton is not extensively documented but is likely to be favorable. As a small molecule modulator of the HGF/MET system, it is expected to have a targeted mechanism of action. Preclinical studies would typically involve acute and chronic dosing in animal models to assess safety margins.
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| References | |
| Additional Infomation |
Fosgonimeton is a small molecule drug. The clinical trial NCT05511558 ([14C]-fosgonimeton (ATH-1017) absorption, metabolism, and excretion study) is currently underway. The monoisotope molecular weight of fosgonimeton is 584.3 Da.
Fosgonimeton is a first-in-class HGF/MET modulator being developed for the treatment of Alzheimer's disease and dementia. It is a prodrug of ATH-1001 (dihexa). The compound has shown promise in preclinical studies and is being evaluated in clinical trials for its potential to improve cognitive function and modify disease progression. |
| Molecular Formula |
C27H45N4O8P
|
|---|---|
| Molecular Weight |
584.6420
|
| Exact Mass |
584.297
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| CAS # |
2093305-05-4
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| PubChem CID |
156596375
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| Appearance |
White to off-white solid powder
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
40
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| Complexity |
844
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| Defined Atom Stereocenter Count |
3
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| SMILES |
P(=O)(O[H])(O[H])OC1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])[C@@]([H])(C(N([H])[C@]([H])(C(N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C(N([H])[H])=O)=O)[C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)N([H])C(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O
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| InChi Key |
MBYDCPOKVKDSFD-JTJYXVOQSA-N
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| InChi Code |
InChI=1S/C27H45N4O8P/c1-4-6-8-12-24(33)30-22(18-20-13-15-21(16-14-20)39-40(36,37)38)26(34)31-25(19(3)5-2)27(35)29-17-10-7-9-11-23(28)32/h13-16,19,22,25H,4-12,17-18H2,1-3H3,(H2,28,32)(H,29,35)(H,30,33)(H,31,34)(H2,36,37,38)/t19-,22-,25-/m0/s1
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| Chemical Name |
[4-[(2S)-3-[[(2S,3S)-1-[(6-amino-6-oxohexyl)amino]-3-methyl-1-oxopentan-2-yl]amino]-2-(hexanoylamino)-3-oxopropyl]phenyl] dihydrogen phosphate
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| Synonyms |
Fosgonimeton; ATH-1017; ATH1017; 2093305-05-4; Fosgonimeton [INN]; H91OA9858J; ATH 1017 FREE ACID;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 125 mg/mL (213.81 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | 0.1710 mL | 0.8552 mL | 1.7105 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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