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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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UV0155041 is a potent, positive allosteric modulator/allosteric agonist at mGlu4 receptors (EC50 = 798 and 693 nM at human and rat mGlu4 receptors respectively).
Targets |
Human mGlu4 ( EC50 = 798 nM ); Rat mGlu4 ( EC50 = 693 nM )
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ln Vitro |
VU0155041 (10 μM) has no effect on NMDA receptor currents in striatal medium spiny neurons[1].
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ln Vivo |
VU0155041 (31 nmol, 93 nmol; i.c.v.) reverses catalepsy brought on by the dopamine D2 receptor antagonist haloperidol (1.5 mg/kg, i.p.) in rats[1].
VU0155041 (93 nnmol, 316 nmol; i.c.v.) reversibly akinesia in rats induced by serpine (HY-N0480)[1].
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Animal Protocol |
Third ventricle cannulated (TVC) Male Sprague-Dawley rats (225-255 g)
31 nmol, 93 nmol (10 μL) Intracerebroventrical injection, after the Haloperidol (1.5 mg/kg) treatment 2 hours |
References |
Molecular Formula |
C14H15CL2NO3
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Molecular Weight |
316.178
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Exact Mass |
315.04
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Elemental Analysis |
C, 53.18; H, 4.78; Cl, 22.42; N, 4.43; O, 15.18
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CAS # |
1093757-42-6
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Related CAS # |
(1R,2S)-VU0155041; 1263273-14-8; VU0155041 sodium; 1259372-69-4
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Appearance |
Solid powder
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SMILES |
C1CC[C@H]([C@H](C1)C(=O)NC2=CC(=CC(=C2)Cl)Cl)C(=O)O
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InChi Key |
VSMUYYFJVFSVCA-NWDGAFQWSA-N
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InChi Code |
InChI=1S/C14H15Cl2NO3/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)/t11-,12+/m0/s1
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Chemical Name |
(1R,2S)-2-[(3,5-dichlorophenyl)carbamoyl]cyclohexane-1-carboxylic acid
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Synonyms |
UV0155041; UV-0155041; UV 0155041
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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: ~100 mg/mL (~316.3 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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. View More
Solubility in Formulation 3: ≥ 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. |
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.
The cis regioisomer (VU0155041) of VU0003423 was more potent and efficacious than the trans regioisomer (VU0155040) in two assays of mGluR4 function. Mol Pharmacol . 2008 Nov;74(5):1345-58. td> |
VU0155041 had no effect on NMDA receptor-mediated currents in striatal medium spiny neurons. Mol Pharmacol . 2008 Nov;74(5):1345-58. td> |
VU0155041 reversed catalepsy induced by the dopamine D2 receptor antagonist haloperidol in rats. Mol Pharmacol . 2008 Nov;74(5):1345-58. td> |
U0155041 reversed reserpine-induced akinesia in rats. Mol Pharmacol . 2008 Nov;74(5):1345-58. td> |