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GSK180736A
🥰Excellent
Catalog No. T3513Cas No. 817194-38-0
Alias GSK180736
GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).
GSK180736A
🥰Excellent
Purity: 98.44%
Catalog No. T3513Alias GSK180736Cas No. 817194-38-0
GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $35 | In Stock | |
| 2 mg | $48 | In Stock | |
| 5 mg | $67 | In Stock | |
| 10 mg | $90 | In Stock | |
| 25 mg | $173 | In Stock | |
| 50 mg | $323 | In Stock | |
| 100 mg | $598 | In Stock | |
| 500 mg | $1,290 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $59 | In Stock |
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Purity:98.44%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM). |
| Targets&IC50 | GRK2:0.77 μM, ROCK1:100 nM |
| In vitro | GSK180736A exhibits a 770 nM IC50 value against GRK2 and 300-fold less potency against GRK5[2]. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM)[3]. |
| Cell Research | Cardiac myocytes are isolated from LV free wall and septum of C57/Bl6 mice. Cells are treated with isoproterenol (0.5 μM) for 2 min for the recording of contraction, with pretreatment of either PBS as vehicle or paroxetine (10 μM), 215022 (0.1, 0.5, 1, 10 μM), 215023 (0.1, 0.5, 1, 10 μM), 224064 (0.1, 0.5, 1, 10 μM), and GSK180736A ( 0.5, 1 μM), for 10 min[1]. |
| Alias | GSK180736 |
| Molecular Weight | 365.36 |
| Formula | C19H16FN5O2 |
| Cas No. | 817194-38-0 |
| Smiles | CC1=C(C(NC(=O)N1)c1ccc(F)cc1)C(=O)Nc1ccc2[nH]ncc2c1 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 60 mg/mL (164.22 mM), Sonication is recommended.  Ethanol: 3 mg/mL (8.21 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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Sci Citations
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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