| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
The efficacy of the cis regioisomer of VU0155041 was similar in human and rat receptors (798±58 nM for human mGluR4 and 693±140 nM for rat mGluR4). In contrast, the concentration response curve for the trans regioisomer (VU0155040) did not approach a plateau at the maximum measured concentration. Fold-shift tests with 30 μM VU0155041 also demonstrated that the cis regioisomer at this dose was more effective against both human and rat mGluR4. VU0155041 induced a concentration-dependent shift in the baseline when investigated experimentally using thallium flux tests for fold shifts. VU0155041 generated a response that reached approximately 45% of the maximal glutamate response. VU0155041 is a partial agonist of mGluR4 and activates the receptor by engaging with a region different from the glutamate binding site. VU0155041 exhibits selectivity for mGluR4 against 67 other targets and does not influence the function of striatal NMDA receptors [1].
|
|---|---|
| ln Vivo |
VU0155041: Soluble in aqueous solutions, rats' haloperidol- and reserpine-induced akinesia is dose-dependently decreased by intracerebroventricular injection of 31 to 316 nM VU0155041. The tetanic effects of haloperidol were likewise considerably lessened by VU0155041 at dosages of 31 and 92 nmol, and the compound's effects lasted for 30 minutes after infusion. Akinesia was similarly markedly improved by intravenous infusion of VU0155041 at a dose of 316 nmol [1].
|
| References |
[1]. Niswender CM, et al. Discovery, characterization, and antiparkinsonian effect of novel positiveallosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol. 2008 Nov;74(5):1345-58
|
| Molecular Formula |
C14H15CL2NO3
|
|---|---|
| Molecular Weight |
316.179802179337
|
| CAS # |
1263273-14-8
|
| Related CAS # |
VU0155041;1093757-42-6;VU0155041 sodium;1259372-69-4
|
| SMILES |
O=C([C@H]1[C@@H](C(NC2=CC(Cl)=CC(Cl)=C2)=O)CCCC1)O
|
| 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 (~158.14 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.91 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 | 3.1628 mL | 15.8138 mL | 31.6276 mL | |
| 5 mM | 0.6326 mL | 3.1628 mL | 6.3255 mL | |
| 10 mM | 0.3163 mL | 1.5814 mL | 3.1628 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
