Formaat : 5mg
Synonyms: (S)-(-)-Blebbistatin
| Description | (-)-Blebbistatin ((S)-(-)-Blebbistatin) is an S enantiomer of blebbistatin. It is a potent and selective myosin II inhibitor with IC50 ranging from 0.5 to 5 μM. |
| Targets & IC50 | non muscle myosin II ATPase (cell-free assays):2 μM, Non-muscle myosin II ATPases:0.5 μM-5 μM, Smooth muscle myosin:80 μM |
| In vitro | METHODS: Mouse hepatic stellate cell HSCs were treated with (-)-Blebbistatin (12.5-50 µM) for 2 h and cell morphology was observed using microscopy. RESULTS: When treated with (-)-Blebbistatin for 2 h, the cells became smaller, acquired more dendritic morphology, and had fewer stress fibers and lamellipods. [1] METHODS: Porcine TM cells were treated with (-)-Blebbistatin (25-100 µM) for 2 h. The expression levels of target proteins were detected using Western Blot. RESULTS: There was no difference in MLC phosphorylation status between control and drug-treated samples. [2] |
| In vivo | Blebbistatin completely relaxes both KCl- and carbachol-induced rat detrusor and endothelin-1-induced human bladder contraction in a dose-dependent manner. Pre-incubation with 10 μM blebbistatin attenuates carbachol responsiveness by 65% while blocking electrical field stimulation-induced bladder contraction reaching 50% inhibition at 32 Hz[4]. |
| Synonyms | (S)-(-)-Blebbistatin |
| Kinase Assay | Inhibition of Cox Activity: Inhibition of Cox-1 activity is measured by monitoring oxygen consumption during the conversion of arachidonic acid to PGs using a Clark-type O2-electrode. The reaction mixture contains ～0.2 units Cox-1 in 100 μL of microsome fraction derived from ram seminal vesicles as a crude source of Cox-1 (specific activity 0.2–1 units/mg protein) or 0.23 units of recombinant human Cox-2 (specific activity 43 units/mg protein). For calculation, the rate of O2 consumption is compared with a DMSO control (100% activity). Piroxicam, a nonsteroidal anti-inflammatory drug, is used as positive inhibitory substance for Cox-1 activity with an IC50 of 0.35 ± 0.05 μM (n = 2). Alternatively, nimesulide, a Cox-2 specific inhibitor, inhibits Cox-2 activity by 52 ± 5.7% (n = 2) at a concentration of 50 μM. |
| Cell Research | Freshly isolated HSCs are replated on 96-well plate. At day 3, medium is replaced by serum-free medium and cells are starved overnight, treated with or without blebbistatin (25 μM) for 2 h followed by stimulation with platelet-derived growth factor-BB (20 ng/mL). After an overnight incubation, the WST-1 cell proliferation assay are performed[3]. |
| Molecular Weight | 292.33 |
| Formula | C18H16N2O2 |
| Cas No. | 856925-71-8 |
| Smiles | Cc1ccc2N=C3N(CC[C@@]3(O)C(=O)c2c1)c1ccccc1 |
| Relative Density. | 1.31 g/cm3 (Predicted) |
| Storage | Store at low temperature,Keep away from moisture,Keep away from direct sunlight,Store under nitrogen,The compound is unstable in solution. Please use soon, Powder: -20°C for 3 years Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 105 mg/mL (359.18 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.93 mg/mL (10.02 mM), Suspension. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
| Size | Quantity | Unit Price | Amount | Operation |
|---|
