| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.
| Targets |
mGlu7 Receptor ( EC50 = 0.65 μM ); mGlu8 Receptor ( EC50 = 2.6 μM )
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|---|---|
| ln Vitro |
VU6005649 is a mGlu7/8 receptor agonist that penetrates the central nervous system. Its EC50 values for the mGlu7 and mGlu8 receptors are 0.65 μM and 2.6 μM, respectively. The terminal Kp of VU6005649 is 2.43, and its total brain levels are approximately 9× higher than the mGlu7 positive allosteric modulator (PAM) in vitro EC50[1].
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| ln Vivo |
VU6005649 (compound 9f) does not show any efficacy in this assay when dosed at 30 mg/kg IP in 10% Tween 80/H2O (0.75 mg/kg. s.c. amphetamine). In wild-type mice, VU6005649 exhibits small but noteworthy pro-cognitive effects on associative learning. It also provides the first instance of a mGlu7/8 positive allosteric modulator's (PAM) effectiveness in this model[1].
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| Animal Protocol |
VU6005649 (compound 9f) is formulated in 10% polysorbate 80 and administered intraperitoneally (3 times per time point) to 20-week-old female C57/Bl6 mice for tissue distribution studies. Animals are put to death and beheaded at 0.25, 0.5, 1, 3, and 6 hours after the dose. Blood is drawn by cardiac puncture, and the brains are extracted, thoroughly cleaned in cold phosphate-buffered saline, and then frozen on dry ice right away[1].
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| References |
| Molecular Formula |
C₁₆H₁₂F₅N₃O
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|---|---|
| Molecular Weight |
357.278000831604
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| Exact Mass |
357.09
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| Elemental Analysis |
C, 53.79; H, 3.39; F, 26.59; N, 11.76; O, 4.48
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| CAS # |
2137047-43-7
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| Appearance |
Solid powder
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| SMILES |
CC1=NC2=C(C(=NN2C(=C1)C(F)(F)F)C)C3=C(C(=C(C=C3)OC)F)F
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| InChi Key |
NYBZCKAQIIPSDS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12F5N3O/c1-7-6-11(16(19,20)21)24-15(22-7)12(8(2)23-24)9-4-5-10(25-3)14(18)13(9)17/h4-6H,1-3H3
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| Chemical Name |
3-(2,3-difluoro-4-methoxyphenyl)-2,5-dimethyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine
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| Synonyms |
VU6005649; VU-6005649; VU 6005649
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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: ~50 mg/mL (~140.0 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.00 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 (7.00 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 | 2.7989 mL | 13.9946 mL | 27.9893 mL | |
| 5 mM | 0.5598 mL | 2.7989 mL | 5.5979 mL | |
| 10 mM | 0.2799 mL | 1.3995 mL | 2.7989 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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