| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
In SAN and HPC cells, VU0810464 (0, 0.1, 0.3, 1, 3, 10, 30 μM) generated concentration-dependent current response curves. Furthermore, compared to the control SAN unit, VU0810464 had nine times the potency to activate Kir3 channels in neurons[2].
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|---|---|
| ln Vivo |
Male C57BL/6J mice treated with VU0810464 (ip; 30 mg/kg, 10 mg/kg, 30 mg/kg; 30 min pretreatment) showed a dose-dependent decrease in the SIH response. VU0810464 (10 mg/kg) decreased the SIH response in wild-type mice but showed no impact in Kcnj3−/− animals, suggesting that it may work through Kir3 channel activation [2]. Compared to ML297 (Kp,uu = 0.32) VU0810464 (ip; 30 mg/kg; 15, 30, 45, or 60 minutes postinjection) demonstrated good brain distribution (Kp,uu = 0.83). According to PK tests, VU0810464 is rapidly eliminated, having a 20-minute half-life in the brain and plasma [2].
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| Animal Protocol |
Animal/Disease Models: Male C57BL/6J mice, Kcnj3−/− female and male C57BL/6J mice
Doses: 10mg/kg; 30mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Reduce stress-induced hyperthermia (SIH), This is a physiological test of anxiolytic efficacy in wild-type mice but has no effect on Kcnj3 (Girk1) −/− mice. |
| References |
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| Molecular Formula |
C18H21CLFN3O
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|---|---|
| Molecular Weight |
349.830246686935
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| Exact Mass |
349.135
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| CAS # |
2126040-21-7
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| PubChem CID |
146014436
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| Appearance |
White to off-white solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
433
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C=CC(=C1)CC(NC1=CC(C)=NN1C1CCCCC1)=O)F
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| InChi Key |
HNJJARDABGKWSO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H21ClFN3O/c1-12-9-17(23(22-12)14-5-3-2-4-6-14)21-18(24)11-13-7-8-16(20)15(19)10-13/h7-10,14H,2-6,11H2,1H3,(H,21,24)
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| Chemical Name |
2-(3-chloro-4-fluorophenyl)-N-(2-cyclohexyl-5-methylpyrazol-3-yl)acetamide
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| Synonyms |
VU 0810464; VU-0810464
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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 : ≥ 250 mg/mL (~714.63 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8585 mL | 14.2927 mL | 28.5853 mL | |
| 5 mM | 0.5717 mL | 2.8585 mL | 5.7171 mL | |
| 10 mM | 0.2859 mL | 1.4293 mL | 2.8585 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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