| Size | Price | Stock | Qty |
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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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| 1g |
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Purity: ≥98%
VU0357121 (VU-0357121, VU 0357121) is a positive allosteric modulator (PAM) of mGlu5 (metabotropic glutamate receptor 4) with antiparkinsonian-like effects. In inhibits mGlu5 with an EC50 of 33 nM, and exhibits little activity against other mGlu receptor subtypes.
| ln Vitro |
The fact that VU 0357121 can increase mGlu5's glutamate sensitivity is probably because of an interaction at a receptor site that is different from the MPEP binding site. VU 0357121 lacks mGlu5 NAM activity because it does not bind at the MPEP allosteric site of mGlu5. While the F585I/rmGlu5 mutation does not change the response to VU 0357121, the A809V/rmGlu5 mutation hindered VU 0357121's ability to shift the glutamate concentration response curve. In the Ca2+ mobilization assay, VU 0357121 exhibits less cooperation in the low-expressing HEK293A-mGlu5 cell line[1].
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| ln Vivo |
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| Animal Protocol |
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| References |
| Molecular Formula |
C17H17F2NO2
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| Molecular Weight |
305.32
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| Exact Mass |
305.122
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| CAS # |
433967-28-3
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| Related CAS # |
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| PubChem CID |
2296132
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
338.7±42.0 °C at 760 mmHg
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| Flash Point |
158.7±27.9 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.564
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| LogP |
4.78
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
346
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AHCYOTLTLQTPSU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17F2NO2/c1-2-3-10-22-14-7-4-12(5-8-14)17(21)20-16-9-6-13(18)11-15(16)19/h4-9,11H,2-3,10H2,1H3,(H,20,21)
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| Chemical Name |
4-butoxy-N-(2,4-difluorophenyl)benzamide
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.19 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 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 (8.19 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 | 3.2753 mL | 16.3763 mL | 32.7525 mL | |
| 5 mM | 0.6551 mL | 3.2753 mL | 6.5505 mL | |
| 10 mM | 0.3275 mL | 1.6376 mL | 3.2753 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.
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