| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
GRK5[1]
GRK5 (G protein-coupled receptor kinase 5). GRK5-IN-2 is a potent, selective inhibitor of GRK5. It inhibits GRK5 activity with an IC50 of 49.7 μM in a luminescent ADP detection assay. By inhibiting GRK5, the compound modulates GPCR signaling, which is involved in various physiological processes including cardiovascular regulation and metabolism. |
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| ln Vitro |
GRK5-IN-2 is a potent GRK5 inhibitor with an IC50 of 49.7 μM in a biochemical assay. It regulates the expression and/or release of insulin. By blocking GRK5 activity, it modulates GPCR signaling pathways. This makes it a useful tool for studying the role of GRK5 in various diseases, including metabolic disorders and cancer.
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| ln Vivo |
In vivo, GRK5-IN-2 is used to study the role of GRK5 in metabolic diseases, as it regulates insulin expression and release. By inhibiting GRK5, the compound can modulate GPCR signaling pathways that are involved in insulin secretion and glucose homeostasis. This makes it a potential tool for investigating the pathophysiology of diabetes and other metabolic disorders.
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| Enzyme Assay |
In vitro activity of GRK5-IN-2 is typically determined using enzyme activity assays. Recombinant GRK5 enzyme is incubated with its substrate in the presence of varying concentrations of the inhibitor. The inhibition of kinase activity is then measured using a luminescent ADP detection assay, which quantifies the amount of ADP produced during the kinase reaction. This allows for the determination of the compound's IC50 (49.7 μM).
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| Cell Assay |
Cellular assays for GRK5 inhibition involve treating cells with GRK5-IN-2 and measuring downstream effects of GRK5 blockade. For example, the compound's effect on insulin expression or release could be assessed in relevant cell lines, such as pancreatic beta cells. This would confirm that the compound can effectively inhibit GRK5 in a cellular context and modulate its physiological functions.
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| Animal Protocol |
In vivo studies with GRK5-IN-2 would be performed in animal models of metabolic disease. The compound could be administered to assess its effects on insulin levels, glucose tolerance, and other metabolic parameters. Its ability to regulate insulin expression and release makes it a candidate for studying the role of GRK5 in diabetes and related disorders.
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| ADME/Pharmacokinetics |
GRK5-IN-2 is a small molecule with the molecular formula C19H18F2N4O3S. Its pharmacokinetic properties, such as oral bioavailability and half-life, are key factors for its utility in in vivo studies. As a research compound, it is designed to be a potent and selective inhibitor of GRK5, which is the primary determinant of its pharmacodynamic profile.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for GRK5-IN-2. As a kinase inhibitor, its safety profile would be an important consideration. Potential off-target effects could lead to toxicity, and standard preclinical safety studies would be needed to evaluate its safety margin. Its selectivity for GRK5 would be expected to minimize off-target toxicity.
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| References | |
| Additional Infomation |
GRK5-IN-2 (CAS#: 1642839-27-7) is a potent and selective inhibitor of G protein-coupled receptor kinase 5 (GRK5). It has an IC50 of 49.7 μM. The compound regulates insulin expression and release and is used for metabolic disease research. It is a research tool and is not approved for clinical use.
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| Molecular Formula |
C20H20N4O4
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|---|---|
| Molecular Weight |
380.397204399109
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| Exact Mass |
380.148
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| CAS # |
1642839-27-7
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| PubChem CID |
71729633
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| Appearance |
Light yellow to brown solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
499
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C=CC=C1C1=NC2C=NC(=CC=2N1C)NC1C=C(C(=C(C=1)OC)OC)OC
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| InChi Key |
CRUXKUKVTMZKSO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H20N4O4/c1-24-14-10-18(21-11-13(14)23-20(24)15-6-5-7-28-15)22-12-8-16(25-2)19(27-4)17(9-12)26-3/h5-11H,1-4H3,(H,21,22)
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| Chemical Name |
2-(furan-2-yl)-1-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[4,5-c]pyridin-6-amine
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| 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) |
DMSO: 62.5 mg/mL (164.30 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6288 mL | 13.1441 mL | 26.2881 mL | |
| 5 mM | 0.5258 mL | 2.6288 mL | 5.2576 mL | |
| 10 mM | 0.2629 mL | 1.3144 mL | 2.6288 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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