VU 0155041 sodium saltCAS# 1259372-69-4 |
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Quality Control & MSDS
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| Cas No. | 1259372-69-4 | SDF | Download SDF |
| PubChem ID | 56972207 | Appearance | Powder |
| Formula | C14H14Cl2NNaO3 | M.Wt | 338.16 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 25 mM in water | ||
| Chemical Name | sodium;(1R,2S)-2-[(3,5-dichlorophenyl)carbamoyl]cyclohexane-1-carboxylate | ||
| SMILES | C1CCC(C(C1)C(=O)NC2=CC(=CC(=C2)Cl)Cl)C(=O)[O-].[Na+] | ||
| Standard InChIKey | ZFDOLOCYGVTGDQ-ZVWHLABXSA-M | ||
| Standard InChI | InChI=1S/C14H15Cl2NO3.Na/c15-8-5-9(16)7-10(6-8)17-13(18)11-3-1-2-4-12(11)14(19)20;/h5-7,11-12H,1-4H2,(H,17,18)(H,19,20);/q;+1/p-1/t11-,12+;/m0./s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent, positive allosteric modulator/allosteric agonist at mGlu4 receptors (EC50 = 798 and 693 nM at human and rat mGlu4 receptors respectively). Active in in vivo models of Parkinson's disease following i.c.v. administration. Sodium salt of VU 0155041. |
VU 0155041 sodium salt Dilution Calculator
VU 0155041 sodium salt Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.9572 mL | 14.7859 mL | 29.5718 mL | 59.1436 mL | 73.9295 mL |
| 5 mM | 0.5914 mL | 2.9572 mL | 5.9144 mL | 11.8287 mL | 14.7859 mL |
| 10 mM | 0.2957 mL | 1.4786 mL | 2.9572 mL | 5.9144 mL | 7.393 mL |
| 50 mM | 0.0591 mL | 0.2957 mL | 0.5914 mL | 1.1829 mL | 1.4786 mL |
| 100 mM | 0.0296 mL | 0.1479 mL | 0.2957 mL | 0.5914 mL | 0.7393 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.[Pubmed:18664603]
Mol Pharmacol. 2008 Nov;74(5):1345-58.
Parkinson's disease (PD) is caused by the death of dopamine neurons in the basal ganglia and results in motor symptoms such as tremor and bradykinesia. Activation of metabotropic glutamate receptor 4 (mGluR4) has been shown to modulate neurotransmission in the basal ganglia and results in antiparkinsonian effects in rodent PD models. N-Phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide (PHCCC) is a positive allosteric modulator (PAM) of mGluR4 that has been used to further validate the role of mGluR4 in PD, but the compound suffers from a lack of selectivity, relatively low potency, and poor solubility. Via high-throughput screening, we discovered more than 400 novel PAMs of mGluR4. Compounds derived from a novel chemical scaffold were characterized in vitro at both rat and human mGluR4 using two distinct assays of mGluR4 function. The lead compound was approximately 8-fold more potent than PHCCC, enhanced the potency of glutamate at mGluR4 by 8-fold, and did not show any significant potentiator or antagonist activity at other mGluR subtypes. Resolution of the regioisomers of the lead revealed that the cis regioisomer, (+/-)-cis-2-(3,5-dichlorphenylcarbamoyl)cyclohexanecarboxylic acid (VU0155041), contained the majority of the mGluR4 PAM activity and also exhibited partial agonist activity at mGluR4 at a site that was distinct from the glutamate binding site, suggesting that this compound is a mixed allosteric agonist/PAM of mGluR4. VU0155041 was soluble in an aqueous vehicle, and intracerebroventricular administration of 31 to 316 nmol of VU0155041 dose-dependently decreased haloperidol-induced catalepsy and reserpine-induced akinesia in rats. These exciting results provide continued support for mGluR4 as a therapeutic target in PD.
