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BLU0588

Name: BLU0588
Brand: TargetMol
SKU: T60169
Price: 1890 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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Purity: 99.85%

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	USA Warehouse	Global Warehouse
1 mg	$195	In Stock	In Stock
5 mg	$448	In Stock	In Stock
10 mg	$658	In Stock	In Stock
25 mg	$987	-	In Stock
50 mg	$1,380	-	In Stock
100 mg	$1,890	-	In Stock
500 mg	Inquiry	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$497	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:99.85%

ee:100%

Appearance:Solid

Color:Yellow

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COA HNMR LCMS CSFC

Product Introduction

Bioactivity

Description	BLU0588 is a selective PRKACA inhibitor. BLU0588 inhibits PRKACA catalytic activity with a half-maximal inhibitory concentration (IC50) of 1 nM.
Targets&IC50	RKACA (PHOS cellsphorylation of VASP Ser157 in Huh7 cells):25.0 nM, PRKACA:4 nM (Kd), PRKACA: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].

Chemical Properties

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

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 85.8 mg/mL (202.59 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3612 mL	11.8061 mL	23.6122 mL	118.0610 mL
5 mM	0.4722 mL	2.3612 mL	4.7224 mL	23.6122 mL
10 mM	0.2361 mL	1.1806 mL	2.3612 mL	11.8061 mL
20 mM	0.1181 mL	0.5903 mL	1.1806 mL	5.9030 mL
50 mM	0.0472 mL	0.2361 mL	0.4722 mL	2.3612 mL
100 mM	0.0236 mL	0.1181 mL	0.2361 mL	1.1806 mL

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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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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