| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
Foliglurax monohydrochloride targets the metabotropic glutamate receptor 4 (mGluR4), a G protein-coupled receptor that modulates neurotransmitter release in the central nervous system. It acts as a positive allosteric modulator (PAM), enhancing the receptor's response to its endogenous ligand, glutamate. By potentiating mGluR4 signaling, the compound modulates neurotransmission and has shown antiparkinsonian effects. The compound is brain-penetrant, making it suitable for studying central nervous system disorders.
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| ln Vitro |
The field of mGlu4 receptor drug uptake to treat disorders of the central nervous system may undergo a revolution thanks to foliglurax monoHClide, a highly selective and potent mGlu4 receptor PAM with notable brain penetration properties [2].
In vitro, Foliglurax monohydrochloride demonstrates highly selective and potent modulation of mGluR4 with an EC₅0 of 79 nM. It enhances mGluR4 signaling, thereby modulating neurotransmitter release. The compound's brain-penetrant properties make it a valuable tool for studying mGluR4 function in the central nervous system. Its antiparkinsonian effect has been observed in preclinical studies, supporting its potential for treating Parkinson's disease. |
| ln Vivo |
In vivo, Foliglurax monohydrochloride has shown antiparkinsonian effects in animal models. As a brain-penetrant mGluR4 PAM, it is expected to modulate neurotransmitter release and improve motor function. The compound may be used to study the role of mGluR4 in Parkinson's disease and other neurological disorders. Further in vivo studies are needed to fully characterize its efficacy, safety, and pharmacokinetic profile.
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| Enzyme Assay |
For in vitro enzyme/receptor binding assays, Foliglurax monohydrochloride can be evaluated using binding studies to measure its affinity for mGluR4. Radioligand binding or fluorescence-based assays can be used to determine binding affinity. Functional activity as a PAM is assessed using cell-based assays that measure mGluR4-mediated signaling, such as calcium mobilization, cAMP inhibition, or IP1 accumulation. EC₅0 values for potentiation of glutamate-induced responses are determined from dose-response curves.
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| Cell Assay |
For in vitro cellular experiments, Foliglurax monohydrochloride is typically tested in cells expressing mGluR4, such as CHO or HEK293 cells stably transfected with the receptor. Cells are cultured in appropriate media and treated with various concentrations of the compound in the presence or absence of glutamate. Receptor activation is measured using calcium-sensitive dyes or other functional readouts. The compound's effects on downstream signaling pathways are further investigated.
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| Animal Protocol |
For in vivo animal experiments, Foliglurax monohydrochloride can be administered to rodents via various routes, including oral gavage, intravenous injection, or intraperitoneal injection. The compound's antiparkinsonian effects can be evaluated in animal models of Parkinson's disease, such as the 6-OHDA or MPTP models. Behavioral tests, such as those measuring motor function and coordination, are used to assess the compound's efficacy. Pharmacodynamic markers and brain penetration are also measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Foliglurax monohydrochloride include brain penetration, supporting its use in central nervous system studies. As a small molecule with a molecular weight of 457.97, it is likely to have reasonable oral bioavailability and tissue distribution. The compound is soluble in DMSO at 5 mg/mL. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies.
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| Toxicity/Toxicokinetics |
Toxicological data for Foliglurax monohydrochloride are limited, as it is primarily a research tool. As an mGluR4 PAM, its toxicity would depend on the importance of mGluR4 signaling for normal neurological function. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity assessments would be needed for further development. Appropriate safety precautions should be taken when handling this compound.
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| References |
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| Additional Infomation |
Foliglurax monohydrochloride is a research compound used to study mGluR4 biology and develop therapies for Parkinson's disease and other neurological disorders. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is a highly selective and potent mGluR4 PAM with an EC₅0 of 79 nM and has antiparkinsonian effects.
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| Molecular Formula |
C23H24CLN3O3S
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|---|---|
| Molecular Weight |
457.97296333313
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| Exact Mass |
457.122
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| CAS # |
2133294-96-7
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| Related CAS # |
Foliglurax;1883329-51-8
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| PubChem CID |
135565464
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
652
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.S1C=CC2=CN=C(C=C12)C1=C/C(/C2=C(C=CC(=C2)CCCN2CCOCC2)O1)=N/O
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| InChi Key |
LOBGNYCFXPNFJB-LUINMZRLSA-N
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| InChi Code |
InChI=1S/C23H23N3O3S.ClH/c27-25-19-13-22(20-14-23-17(15-24-20)5-11-30-23)29-21-4-3-16(12-18(19)21)2-1-6-26-7-9-28-10-8-26;/h3-5,11-15,27H,1-2,6-10H2;1H/b25-19+;
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| Chemical Name |
(NE)-N-[6-(3-morpholin-4-ylpropyl)-2-thieno[3,2-c]pyridin-6-ylchromen-4-ylidene]hydroxylamine;hydrochloride
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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: Please store this product in a sealed and protected environment, 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) |
H2O : ~25 mg/mL (~54.59 mM)
DMSO : ~5 mg/mL (~10.92 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1835 mL | 10.9177 mL | 21.8355 mL | |
| 5 mM | 0.4367 mL | 2.1835 mL | 4.3671 mL | |
| 10 mM | 0.2184 mL | 1.0918 mL | 2.1835 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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