| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
VU0483605 targets metabotropic glutamate receptor 1 (mGluR1), a class C G protein-coupled receptor that is activated by the major excitatory neurotransmitter glutamate. It acts as a positive allosteric modulator (PAM), binding to an allosteric site distinct from the orthosteric glutamate binding site to potentiate receptor activity. VU0483605 displays EC₅₀ values of 0.39 μM at the human receptor and 0.36 μM at the rat receptor.
|
|---|---|
| ln Vitro |
It was shown that VU0483605 had negligible mGlu4 PAM activity (EC50 > 10 μM) and excellent mGlu1 PAM activity in both humans (EC50 = 390 nM) and rats (EC50 = 356 nM, pEC50 = 6.45 ± 0.11, 113 ± 5% Glu Max)[1].
In vitro, VU0483605 potentiates glutamate-induced responses in wild-type cell lines stably expressing mGluR1. It shows no activity as a mGluR4 PAM (EC₅₀ >10 μM), confirming its selectivity for mGluR1. In a mutant cell model of schizophrenia, VU0483605 partially restores the reduction in glutamate-mediated calcium signaling, demonstrating its potential to modulate aberrant mGluR1 function. |
| ln Vivo |
In vivo activity data for VU0483605 are not extensively reported in the available literature. As a research compound, its primary application is in in vitro and ex vivo studies of mGluR1 function. The compound's ability to potentiate mGluR1-mediated calcium signaling in a schizophrenia model cell line suggests potential for in vivo studies of neurological disorders, but systematic in vivo efficacy data are lacking.
|
| Enzyme Assay |
In vitro receptor binding and functional assays for VU0483605 involve measuring its ability to potentiate mGluR1-mediated calcium signaling in cell lines expressing the receptor. Calcium mobilization is measured using fluorescence-based calcium indicators. EC₅₀ values are determined from concentration-response curves. Selectivity is assessed by testing the compound against other mGluR subtypes such as mGluR4.
|
| Cell Assay |
In vitro cellular assays for VU0483605 are performed using cell lines stably expressing human or rat mGluR1. Cells are treated with glutamate (the orthosteric agonist) in the presence of increasing concentrations of the compound. Receptor activity is measured by assessing calcium mobilization using fluorescent calcium indicators. The EC₅₀ for potentiation of glutamate-induced responses is calculated from concentration-response curves.
|
| Animal Protocol |
In vivo animal experimental protocols for VU0483605 are not extensively documented. For potential in vivo applications, the compound would likely be administered via intraperitoneal or oral routes in rodent models of neurological disorders. Efficacy would be assessed by measuring behavioral outcomes, electrophysiological recordings, or biochemical markers of mGluR1 activation.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of VU0483605 have not been systematically characterized. The compound has a molecular weight of 446.67 and molecular formula C₂₀H₁₀Cl₃N₃O₃. It is soluble in DMF and DMSO at 20 mg/mL and in DMSO:PBS (pH 7.2) (1:2) at 0.3 mg/mL. It should be stored at -20°C and shipped at room temperature. Further PK studies are needed.
|
| Toxicity/Toxicokinetics |
Toxicological data for VU0483605 are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
|
| References | |
| Additional Infomation |
VU0483605 is a research compound supplied with purity ≥98%. It is a crystalline solid with λmax at 219 and 280 nm. The compound is a selective positive allosteric modulator of mGluR1 developed for studying glutamate receptor function and neurological disorders. It is not approved for clinical use.
|
| Molecular Formula |
C20H10CL3N3O3
|
|---|---|
| Molecular Weight |
446.670701503754
|
| Exact Mass |
444.978
|
| CAS # |
1623101-11-0
|
| PubChem CID |
91885483
|
| Appearance |
Light yellow to orange solid powder
|
| Density |
1.6±0.1 g/cm3
|
| Index of Refraction |
1.728
|
| LogP |
3.87
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
29
|
| Complexity |
679
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC2=C(C(=C1)Cl)C(=O)N(C2=O)C3=C(C=C(C=C3)NC(=O)C4=C(C=CC=N4)Cl)Cl
|
| InChi Key |
HJQXPBKPTGWZCF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H10Cl3N3O3/c21-12-4-1-3-11-16(12)20(29)26(19(11)28)15-7-6-10(9-14(15)23)25-18(27)17-13(22)5-2-8-24-17/h1-9H,(H,25,27)
|
| Chemical Name |
3-chloro-N-[3-chloro-4-(4-chloro-1,3-dioxoisoindol-2-yl)phenyl]pyridine-2-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~223.88 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2388 mL | 11.1939 mL | 22.3879 mL | |
| 5 mM | 0.4478 mL | 2.2388 mL | 4.4776 mL | |
| 10 mM | 0.2239 mL | 1.1194 mL | 2.2388 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
