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SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: 3 nM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $48 | In Stock | In Stock | |
| 10 mg | $81 | In Stock | In Stock | |
| 25 mg | $157 | In Stock | In Stock | |
| 50 mg | Preferential | In Stock | - | |
| 1 mL x 10 mM (in DMSO) | $53 | In Stock | In Stock |
| Description | SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: 3 nM). |
| Targets&IC50 | ROCK2:3 nM, ROCK1:56 nM |
| In vitro | SR-3677 has an IC50 of ~3 nM in enzyme and cell-based assays and has an off-target hit rate of 1.4% against 353 kinases, and inhibits only 3 out of 70 non-kinase enzymes and receptors. The IC50 value of SR-3677 for ROCK-I is 56 nM. |
| In vivo | SR-3677 increases ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation. Continuous exposure of 25 μM SR-3677 increases the outflow facility by 60% at 1 h perfusion, increasing to 70–80% for the 2–5 h time points. |
| Kinase Assay | 5 μL mixture of a 1 μM STK2 substrate and ATP (ROCK-I: 4 μM; ROCK-II: 20 μM) in STK-buffer is added to the wells. 20 nL of test compounds (SR-3677) is dispensed. The reaction is started by addition of 5 μL of 2.5 nM. ROCK-I or 0.5 nM ROCK-II in STK-buffer. After 4 h at RT, the reaction is stopped by the addition of 10 μL of 1x antibody and 62.5 nM Sa-XL in the detection buffer. |
| Molecular Weight | 408.45 |
| Formula | C22H24N4O4 |
| Cas No. | 1072959-67-1 |
| Smiles | CN(C)CCOc1cc(ccc1NC(=O)C1COc2ccccc2O1)-c1cn[nH]c1 |
| Relative Density. | 1.298 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (97.93 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.9 mM), Sonication is recommended. 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
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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.
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