| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
mGluR4 (metabotropic glutamate receptor 4).
|
|---|---|
| ln Vitro |
VU0080241 is a positive allosteric modulator (PAM) of mGluR4 with an EC50 of 4.6 μM. It enhances receptor signaling by potentiating the response to glutamate, making it a valuable tool for studying mGluR4 function in the central nervous system.
|
| ln Vivo |
No detailed in vivo activity data is available for this compound. As an mGluR4 PAM, it is expected to have activity in models of neurological and psychiatric disorders, but specific in vivo efficacy studies have not been reported.
|
| Enzyme Assay |
The compound's modulation of mGluR4 is assessed in cell-free membrane preparations using radioligand binding assays to confirm binding to the receptor and determine the nature of allosteric modulation.
|
| Cell Assay |
VU0080241 is evaluated in cell-based functional assays using cells expressing recombinant mGluR4 receptors. Calcium mobilization or other second messenger assays measure the compound's ability to potentiate glutamate-induced receptor activation, with an EC50 of 4.6 μM.
|
| Animal Protocol |
No detailed in vivo animal experimental protocol is available for this compound. For mGluR4 PAMs, typical in vivo studies involve rodent models of Parkinson's disease, anxiety, or other CNS disorders to assess therapeutic potential.
|
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is available for VU0080241. With a molecular weight of 321.42, the compound is expected to have reasonable drug-like properties, but specific PK parameters have not been reported.
|
| Toxicity/Toxicokinetics |
No detailed toxicological data is available for this compound. As a research-grade chemical probe, standard preclinical toxicity assessments have not been published.
|
| References | |
| Additional Infomation |
VU0080241 has a molecular formula of C19H23N5 and a molecular weight of 321.42. The compound is a selective mGluR4 positive allosteric modulator with a favorable pharmacological profile for neuroscience research. It has not advanced to clinical trials and is not FDA-approved.
|
| Molecular Formula |
C19H23N5
|
|---|---|
| Molecular Weight |
321.4194
|
| Exact Mass |
321.195
|
| CAS # |
393845-24-4
|
| PubChem CID |
3260619
|
| Appearance |
Yellow to orange solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
447.5±45.0 °C at 760 mmHg
|
| Flash Point |
224.4±28.7 °C
|
| Vapour Pressure |
0.0±1.1 mmHg at 25°C
|
| Index of Refraction |
1.672
|
| LogP |
4.41
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
24
|
| Complexity |
430
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1CCCN(C1)C2=NC=NC3=C2C=NN3C4=C(C=C(C=C4)C)C
|
| InChi Key |
CLQVVBPDAXJGBV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H23N5/c1-13-6-7-17(15(3)9-13)24-19-16(10-22-24)18(20-12-21-19)23-8-4-5-14(2)11-23/h6-7,9-10,12,14H,4-5,8,11H2,1-3H3
|
| Chemical Name |
1-(2,4-dimethylphenyl)-4-(3-methylpiperidin-1-yl)pyrazolo[3,4-d]pyrimidine
|
| 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 |
| 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 : ~50 mg/mL (~155.56 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.78 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.78 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 25.0 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 | 3.1112 mL | 15.5560 mL | 31.1119 mL | |
| 5 mM | 0.6222 mL | 3.1112 mL | 6.2224 mL | |
| 10 mM | 0.3111 mL | 1.5556 mL | 3.1112 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
