| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| Targets |
D1 Receptor D5 Receptor 5-HT2 Receptor 11 nM (Ki)
|
|---|---|
| ln Vitro |
When single-pulse stimulation is applied, SKF-83566 (0.1 μM–10 μM) increases peak evoked extracellular DA concentration ([DA]o) in a concentration-dependent manner. Peak increases of up to 65% are observed when 5 μM is applied. For this effect, SKF-83566 has an EC50 value of 1.3 μM[2]. The [3H]DA uptake is inhibited by SKF-83566, with an IC50 of 5.73 μM. Moreover, tests on [3H]DA uptake and [3H]CFT binding show that SKF-83566 inhibits [3H]CFT binding more successfully, with an IC50 of 0.51 μM [2]. Likewise, with an IC50 of 0.77 μM, SKF-83566 also prevented [3H]CFT binding in LLc-PK-rDAT cell membrane preparations [2].
|
| ln Vivo |
SKF 83566 (oral; 20 μg/mL; 7 days) did not change LTP (115%) in any way. SKF 83566 + nicotine + cocaine, 120%; nicotine + cocaine, 143%), however, significantly inhibited the increase of long-term synaptic potentiation (LTP) caused by nicotine pretreatment[1].
|
| Animal Protocol |
Animal/Disease Models: Male C57BL6/J mice (6- to 9-wk-old)[1]
Doses: 20 µg/mL (Together with nicotine for 7 d, followed by the injection of cocaine) Route of Administration: Oral administration; 7 days Experimental Results: Blocked nicotine and cocaine-induced facilitation of LTP. |
| References |
|
| Additional Infomation |
8-bromo-3-methyl-5-phenyl-1,2,4,5-tetrahydro-3-benzazepin-7-ol is a benzazepine.
|
| Molecular Formula |
C17H18BRNO
|
|---|---|
| Molecular Weight |
332.23
|
| Exact Mass |
367.034
|
| CAS # |
99295-33-7
|
| Related CAS # |
SKF-83566 hydrobromide;108179-91-5
|
| PubChem CID |
1243
|
| Appearance |
Off-white to light yellow solid powder
|
| Boiling Point |
447.5ºC at 760mmHg
|
| Flash Point |
224.4ºC
|
| LogP |
4.514
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
20
|
| Complexity |
318
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
XFTVOHWWEQGXLS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H18BrNO/c1-19-8-7-13-9-16(18)17(20)10-14(13)15(11-19)12-5-3-2-4-6-12/h2-6,9-10,15,20H,7-8,11H2,1H3
|
| Chemical Name |
8-bromo-3-methyl-5-phenyl-1,2,4,5-tetrahydro-3-benzazepin-7-ol
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 33.33 mg/mL (100.32 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.52 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 (7.52 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 (7.52 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 | 3.0100 mL | 15.0498 mL | 30.0996 mL | |
| 5 mM | 0.6020 mL | 3.0100 mL | 6.0199 mL | |
| 10 mM | 0.3010 mL | 1.5050 mL | 3.0100 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
