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[CAS NO. 817194-38-0] GSK180736A
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-18990 |
| Brand: | MCE |
| CAS: | 817194-38-0 |
Overview
| MDL | MFCD30533616 |
|---|---|
| Molecular Weight | 365.36 |
| Molecular Formula | C19H16FN5O2 |
| SMILES | CC(N1)=C(C(NC2=CC=C(NN=C3)C3=C2)=O)C(C4=CC=C(F)C=C4)NC1=O |
4 Publications Citing Use of MCE
Summary
GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC 50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC 50 of 0.77 μM.
IC50 & Target
|
ROCK1 100 nM (IC 50 ) |
GRK2 770 nM (IC 50 ) |
In Vitro
GSK180736A is a compound structurally similar to paroxetine that is developed as a ROCK inhibitor, is shown to be an even more potent and selective inhibitor of GRK2 with an IC 50 of 0.77 μM and more than 100-fold selectivity over other GRKs. ROCK1 is a potential therapeutic target in the treatment of cardiovascular diseases such as hypertension. GSK180736A is a weak inhibitor of PKA with an IC 50 of 30 μM, but highly potent against ROCK1 (IC 50 =100 nM) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 30 mg/mL ( 82.11 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7370 mL | 13.6851 mL | 27.3703 mL |
| 5 mM | 0.5474 mL | 2.7370 mL | 5.4741 mL |
| 10 mM | 0.2737 mL | 1.3685 mL | 2.7370 mL |
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