| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Auglurant targets the metabotropic glutamate receptor 5 (mGluR5). It acts as a negative allosteric modulator, binding to a site on the receptor different from the active site and decreasing the receptor's activity.
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| ln Vitro |
In HEK293A cells, the IC50 value of auglurant (VU0424238) is 14 nM. Additionally, it binds to a K i value of 4.4 nM in HEK293A cells, which is a recognized allosteric site.
In vitro, Auglurant is a potent mGluR5 antagonist with IC50 values of 11 nM (rat) and 14 nM (human). This high potency is a key feature of its in vitro profile. |
| ln Vivo |
At an oral dose of 0.8 mg/kg, auglurant (VU0424238) displays 50% mGlu5 PET ligand occupancy in rats and has a clearance of 19.3 mL/min/kg. Additionally, at an oral dosage of 0.06 mg/kg, it exhibits 50% mGlu5 PET ligand occupancy in baboons and a clearance of 15.5 mL/min/kg in cynomolgus monkeys [1].
In vivo activity data for Auglurant is not detailed in the available literature. As a CNS-penetrant mGluR5 NAM, its effects would be studied in animal models of neuropsychiatric disorders, but specific studies are not cited. |
| Enzyme Assay |
The binding affinity and potency of Auglurant are determined using standard radioligand binding or functional assays. The IC50 values of 11 nM and 14 nM for rat and human mGluR5, respectively, were established in such assays.
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| Cell Assay |
Auglurant is used in cell-based assays to study mGluR5 function. Its activity as a negative allosteric modulator is confirmed by measuring its ability to inhibit mGluR5-mediated signaling, such as calcium mobilization, in cells expressing the receptor.
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| Animal Protocol |
Specific in vivo animal models are not detailed. As a CNS-active compound, relevant models would include those for anxiety, depression, Parkinson's disease, and other neuropsychiatric disorders where mGluR5 is a therapeutic target.
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| ADME/Pharmacokinetics |
Auglurant has acceptable CNS penetration. Specific pharmacokinetic data, such as half-life and oral bioavailability, are not detailed, but its CNS penetration is a key feature for its intended use.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Auglurant is not provided. As a research compound, its safety profile would be a critical consideration for further development.
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| References | |
| Additional Infomation |
Auglurant is a research tool for studying the role of mGluR5 in the central nervous system. Its high potency and selectivity make it a valuable compound for investigating mGluR5-mediated signaling and for validating mGluR5 as a therapeutic target for various neuropsychiatric and inflammatory diseases.
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| Molecular Formula |
C16H12FN5O2
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|---|---|
| Molecular Weight |
325.297185897827
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| Exact Mass |
325.098
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| Elemental Analysis |
C, 59.08; H, 3.72; F, 5.84; N, 21.53; O, 9.84
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| CAS # |
1396337-04-4
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| PubChem CID |
60168069
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.831
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
421
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RBAHIIPVJVMACF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12FN5O2/c1-10-4-12(24-13-7-18-9-19-8-13)5-14(21-10)16(23)22-15-3-2-11(17)6-20-15/h2-9H,1H3,(H,20,22,23)
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| Chemical Name |
N-(5-fluoropyridin-2-yl)-6-methyl-4-pyrimidin-5-yloxypyridine-2-carboxamide
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| Synonyms |
Auglurant; VU0424,238, VU 0424238, VU-0424238; 1396337-04-4; N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide; VU0424238; GRN8X62ZW2;
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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 |
| 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 : ~22.73 mg/mL (~69.87 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0741 mL | 15.3704 mL | 30.7409 mL | |
| 5 mM | 0.6148 mL | 3.0741 mL | 6.1482 mL | |
| 10 mM | 0.3074 mL | 1.5370 mL | 3.0741 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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