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P-1075

Name: P-1075
Brand: TargetMol
SKU: T16420
Price: 55 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16420Cas No. 60559-98-0

P-1075 is a potent sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6) activator (EC50 = 45 nM). P-1075 opens opens mitoKATP channels and may be cardioprotective.

P-1075

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Purity: 99.85%

Catalog No. T16420Cas No. 60559-98-0

P-1075 is a potent sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6) activator (EC50 = 45 nM). P-1075 opens opens mitoKATP channels and may be cardioprotective.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$55	In Stock	In Stock
5 mg	$128	In Stock	In Stock
10 mg	$213	In Stock	In Stock
25 mg	$388	In Stock	In Stock
50 mg	$589	In Stock	In Stock
100 mg	$787	In Stock	In Stock
200 mg	$1,070	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$97	In Stock	In Stock

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

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.

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Purity:99.85%

Appearance:Solid

Color:White

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COA LCMS

Product Introduction

P-1075 AI Summary

P-1075 exhibits diverse bioactivities, including ionization constants with pKa1 at 2.61 and pKa2 at 12.18. It shows potent bioactivity in various assays: it induces a 15% increase in [86Rb+] efflux from rat portal vein at a concentration with a pEC15 of 7.4, inhibits spontaneous activity with an IC50 of 1.995 nM, and has binding affinities with a Ki of 27.0 nM in canine cardiac membranes and a Hill coefficient of 1.17. It requires an EC50 of 60.0 nM to delay contracture onset in ischemic rat hearts and shows inhibition of methoxamine-induced contractions in rat aorta with an IC50 of 4.4 nM. Additionally, it modulates K-ATP channels, with EC50 values of 44.67 nM and 85.11 nM in guinea pig and landrace pig bladder assays, respectively, and shows vasorelaxant activity in rat aorta (IC50 250.0 nM), though it is weakly active against rat mitochondrial ATP hydrolase (IC50 > 100,000 nM). P-1075 displays hypotensive effects, effective at doses as low as 0.1 mg/kg, but is toxic at higher doses (LD50 14 mg/kg). It also exhibits antibacterial and antiviral properties, showing various inhibition percentages against pathogens and high IC50 values (>20,000 nM) for SARS-CoV-2 antiviral activity. Lastly, it has a complex impact on cell viability, enhancing growth in some cell lines while suppressing it in others..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	P-1075 is a potent sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6) activator (EC50 = 45 nM). P-1075 opens opens mitoKATP channels and may be cardioprotective.
Targets&IC50	SUR2-KIR6:45 nM(EC50)

Chemical Properties

Molecular Weight	231.3
Formula	C₁₂H₁₇N₅
Cas No.	60559-98-0
Smiles	CCC(C)(C)N\C(NC#N)=N\c1cccnc1
Relative Density.	1.07 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (1080.85 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (21.62 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	4.3234 mL	21.6169 mL	43.2339 mL	216.1695 mL
5 mM	0.8647 mL	4.3234 mL	8.6468 mL	43.2339 mL
10 mM	0.4323 mL	2.1617 mL	4.3234 mL	21.6169 mL
20 mM	0.2162 mL	1.0808 mL	2.1617 mL	10.8085 mL
50 mM	0.0865 mL	0.4323 mL	0.8647 mL	4.3234 mL
100 mM	0.0432 mL	0.2162 mL	0.4323 mL	2.1617 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