| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Retinal ganglion cells' synaptic input is regulated by mGluR8 [1]. Depending on the strength of light stimulation, AZ 12216052 (10 μM) increases the peak excitatory currents of switching currents in switch ganglion cells [1]. In human neuroblastoma SH-SY5Y cells, AZ 12216052 (0.01-1 μM; 24-48 hours) partially decreased Dox-induced damage and shown effects on cell differentiation [2]. In UN-SH-SY5Y cells, AZ 12216052 promotes proliferation and reduces the toxicity caused by doxorubicin (Dox) and staurosporine (St) [2]. The glutamate activity of human mGluR8b receptors expressed in GHEK cells is enhanced by AZ12216052 (10 μM) [3].
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| ln Vivo |
Mice's anxiety levels are lowered by AZ 12216052 (10 mg/kg; intraperitoneal injection; two hours prior to testing) without altering their speed [3]. In mice lacking mGluR8, AZ12216052 (10 mg/kg; i.p.; single dose) shows lingering anxiolytic effects that might be related to mGluR4 because mGluR4 PAM (positive allosteric modulator) VU 0155041 similarly lowers the levels of anxiety in mice with wild-type [4].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: UN- and RA-SH-SY5Y Cell Tested Concentrations: 0.01-1 μM Incubation Duration: 48 hrs (hours) Experimental Results: Cell viability increased at 0.1 μM and protected undifferentiated neuroblastoma cells against Destructive effects of Iri or Cis. |
| Animal Protocol |
Animal/Disease Models: WT and apolipoprotein E-deficient (Apoe−/−) mice (C57BL/6J, 2 months old) in the elevated zero maze [3]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; intraperitoneal (ip) injection. Single dose, 2 hrs (hrs (hours)) before testing Experimental Results: diminished anxiety measures in the elevated zero maze without affecting mice's speed. Reduce sound startle response. |
| References |
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| Molecular Formula |
C17H26BNO2SI
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|---|---|
| Molecular Weight |
315.290345668793
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| Exact Mass |
391.061
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| CAS # |
1290628-31-7
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| PubChem CID |
73755190
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| Appearance |
White to off-white solid powder
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| LogP |
5.907
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
23
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| Complexity |
349
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QKUYZJOTWYRWNF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H22BrNOS/c1-3-14(2)16-6-10-18(11-7-16)21-19(22)13-23-12-15-4-8-17(20)9-5-15/h4-11,14H,3,12-13H2,1-2H3,(H,21,22)
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| Chemical Name |
2-[(4-bromophenyl)methylsulfanyl]-N-(4-butan-2-ylphenyl)acetamide
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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 (~254.87 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.37 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.37 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 | 3.1717 mL | 15.8584 mL | 31.7168 mL | |
| 5 mM | 0.6343 mL | 3.1717 mL | 6.3434 mL | |
| 10 mM | 0.3172 mL | 1.5858 mL | 3.1717 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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