| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
ROCK1 (Rho-associated protein kinase 1) and GRK2 (G protein-coupled receptor kinase 2). GSK270822A is a selective ROCK1 inhibitor and a GRK2 inhibitor. GRK2 has been implicated in the progression of heart failure.
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|---|---|
| ln Vitro |
GSK270822A inhibits ROCK1 with an IC50 of 8-9 nM. It also inhibits RSK1 (IC50 = 1100 nM) and p70S6K (IC50 = 1550 nM). As a GRK2 inhibitor, it has potential applications in heart failure and Parkinson's disease research.
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| ln Vivo |
Specific in vivo activity data for GSK270822A are not detailed in the available literature. As a ROCK1 and GRK2 inhibitor, it could have effects on cardiovascular function and other physiological processes. GRK2 inhibitors have been implicated in the progression of heart failure and may be useful as chemical probes.
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| Enzyme Assay |
In vitro kinase inhibition assays for GSK270822A involve measuring the activity of ROCK1, GRK2, or other kinases in the presence of varying concentrations of the compound. The enzyme is incubated with ATP and a substrate peptide, and the phosphorylation of the substrate is quantified. The IC50 is determined from the dose-response curve.
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| Cell Assay |
In vitro cell-based assays for GSK270822A assess its effects on ROCK1- or GRK2-dependent signaling in cells. Cells are treated with GSK270822A, and the phosphorylation of downstream targets is measured by Western blotting or ELISA. The compound's effects on cell morphology, migration, or other functional endpoints can also be evaluated.
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| Animal Protocol |
Specific in vivo animal model protocols for GSK270822A are not described in the available literature. To evaluate its in vivo activity, GSK270822A could be administered to animal models of heart failure or other diseases where ROCK1 or GRK2 plays a role.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GSK270822A are not reported in the available literature. As a small molecule inhibitor, its absorption, distribution, metabolism, and excretion properties would need to be characterized for in vivo use. The compound is available as a hydrochloride salt.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GSK270822A are not available. As a research compound, its safety profile has not been comprehensively characterized. Toxicity studies would be required to determine its safety margin and potential off-target effects.
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| References | |
| Additional Infomation |
GSK270822A is a research tool for studying ROCK1 and GRK2 function. GRK2 has been implicated in the progression of heart failure, and the compound may be useful as a chemical probe for therapeutic applications ranging from heart failure to Parkinson's disease. It is not an approved therapeutic agent.
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| Molecular Formula |
C24H20N4O2
|
|---|---|
| Molecular Weight |
396.44
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| Exact Mass |
396.158
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| CAS # |
864082-23-5
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| PubChem CID |
11269477
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
3.2
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
30
|
| Complexity |
720
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=C(C(CC(=O)N1)C2=CC3=CC=CC=C3C=C2)C(=O)NC4=CC5=C(C=C4)NN=C5
|
| InChi Key |
ODLNBFNBEPOFNC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H20N4O2/c1-14-23(24(30)27-19-8-9-21-18(11-19)13-25-28-21)20(12-22(29)26-14)17-7-6-15-4-2-3-5-16(15)10-17/h2-11,13,20H,12H2,1H3,(H,25,28)(H,26,29)(H,27,30)
|
| Chemical Name |
N-(1H-indazol-5-yl)-6-methyl-4-naphthalen-2-yl-2-oxo-3,4-dihydro-1H-pyridine-5-carboxamide
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5224 mL | 12.6122 mL | 25.2245 mL | |
| 5 mM | 0.5045 mL | 2.5224 mL | 5.0449 mL | |
| 10 mM | 0.2522 mL | 1.2612 mL | 2.5224 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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