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BLU0588
🥰Excellent
Catalog No. T60169Cas No. 2810747-78-3
BLU0588 is a selective PRKACA inhibitor. BLU0588 inhibits PRKACA catalytic activity with a half-maximal inhibitory concentration (IC50) of 1 nM.
BLU0588
🥰Excellent
Purity: 98.25%
Catalog No. T60169Cas No. 2810747-78-3
BLU0588 is a selective PRKACA inhibitor. BLU0588 inhibits PRKACA catalytic activity with a half-maximal inhibitory concentration (IC50) of 1 nM.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $195 | In Stock | |
| 5 mg | $448 | In Stock | |
| 10 mg | $658 | In Stock | |
| 25 mg | $987 | In Stock | |
| 50 mg | $1,380 | In Stock | |
| 100 mg | $1,890 | In Stock | |
| 500 mg | $3,780 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $497 | In Stock |
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Purity:98.25%
ee:100%
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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 | BLU0588 is a selective PRKACA inhibitor. BLU0588 inhibits PRKACA catalytic activity with a half-maximal inhibitory concentration (IC50) of 1 nM. |
| In vitro | RKACA cellular IC50 values were 25.0 nM with BLU0588, which were determined from inhibition of VASP Ser157 phosphorylation in forskolin-stimulated Huh7 cells[1]. |
| In vivo | For in vivo studies, mice were given either BLU0588 at 30 mg/kg and 75 mg/kg once daily (QD) and monitored for 24 hours. Plasma concentrations peaked within 2–4 hours of QD dosing. For BLU0588-treated mice, phosphorylated VASP was reduced to 19% and 4% of baseline phosphorylation levels with 30 mg/kg QD and 75 mg/kg QD, respectively, 4 hours after dosing; phosphorylated VASP levels fully recovered by 24 hours post administration of 30 mg/kg QD. When mice harboring FLC PDX tumors were treated with BLU0588 given orally at 30 mg/kg QD, by Day 34 tumor growth was inhibited by 48.5% (P = 0.003)[1]. |
| Molecular Weight | 423.51 |
| Formula | C26H25N5O |
| Cas No. | 2810747-78-3 |
| Smiles | O=C(N[C@@H]1C2=C(C=CC=C2)C[C@H]1N1CCCC1)C1=CC=C(C2=C3C=CNC3=NC=C2)N=C1 |
| Relative Density. | 1.35 g/cm3 at 20℃ (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (129.87 mM)  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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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.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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