P-1075
Based on 1 publication(s) in Google Scholar
P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.
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- Pureté : 99.94%
- CAS No.: 60559-98-0
- Formule: C12H17N5
- Masse moléculaire:231.30
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) P-1075
More
Activité biologique
Description
IC50 & Target
EC50: 45 nM (SUR2-KIR6)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| C6 | EC50 |
60.5 μM
Compound: P1075
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Channel opening activity at SUR1/Kir6.2 potassium ATP channel in mouse beta-TC6 cells assessed as isometric force by FLIPR
Channel opening activity at SUR1/Kir6.2 potassium ATP channel in mouse beta-TC6 cells assessed as isometric force by FLIPR
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[PMID: 19101153] |
| COS-7 | EC50 |
0.62 μM
Compound: P1075
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Channel opening activity at SUR2A/Kir6.2 potassium ATP channel in african green monkey COS7 cells assessed as isometric force by FLIPR
Channel opening activity at SUR2A/Kir6.2 potassium ATP channel in african green monkey COS7 cells assessed as isometric force by FLIPR
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[PMID: 19101153] |
| TE-671 | EC50 |
0.23 μM
Compound: P1075
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Channel opening activity at SUR2B/Kir6.2 potassium ATP channel in human TE671 cells assessed as isometric force by FLIPR
Channel opening activity at SUR2B/Kir6.2 potassium ATP channel in human TE671 cells assessed as isometric force by FLIPR
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[PMID: 19101153] |
In Vitro
P1075 (3 nM) induces monophasic inhibition curves by competition-binding experiments, in the presence of MgATP[1].
P1075 (100 µM; 10 min) leads to rabbit cardiomyocytes to produce ROS in a KATP-dependent fashion[2].
P1075 (150 nM) reduces infarct size in isolated rabbit hearts compared to control animals (10.6% of the area at risk vs. 31.5%, P < 0.05)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:COS-7 cells
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Concentration:3-15 nM
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Incubation Time:
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Result:Showed IC50 value of 15 nM and Hill coefficient of 1.0.
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Cell Line:Adult rabbit cardiomyocytes
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Concentration:100 µM
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Incubation Time:10 min
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Result:Led to a 44% increase in ROS generation (P<0.001 vs. untreated cells).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats subjected to 30 minutes of ischemia and 2 hours of reperfusion[3]
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Dosage:1μg/kg
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Administration:Intravenous injection; 1μg/kg; once
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Result:Reduced infarct size (41.8%) compared to the vehicle.
Chemical Information
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CAS No. 60559-98-0
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Appearance Solid
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Masse moléculaire 231.30
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Formule C12H17N5
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Color White to off-white
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SMILES
CCC(N/C(NC#N)=N/C1=CC=CN=C1)(C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (432.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (8.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (8.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Schwanstecher M, et al. Potassium channel openers require ATP to bind to and act through sulfonylurea receptors. EMBO J. 1998 Oct 1;17(19):5529-35. [Content Brief]
[2]. Oldenburg O, et al. P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts. J Mol Cell Cardiol. 2003 Sep;35(9):1035-42. [Content Brief]
[3]. Gross ER, et al. GSK3beta inhibition and K(ATP) channel opening mediate acute opioid-induced cardioprotection at reperfusion. Basic Res Cardiol. 2007 Jul;102(4):341-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.3234 mL | 21.6169 mL | 43.2339 mL | 108.0847 mL |
| 5 mM | 0.8647 mL | 4.3234 mL | 8.6468 mL | 21.6169 mL | |
| 10 mM | 0.4323 mL | 2.1617 mL | 4.3234 mL | 10.8085 mL | |
| 15 mM | 0.2882 mL | 1.4411 mL | 2.8823 mL | 7.2056 mL | |
| 20 mM | 0.2162 mL | 1.0808 mL | 2.1617 mL | 5.4042 mL | |
| 25 mM | 0.1729 mL | 0.8647 mL | 1.7294 mL | 4.3234 mL | |
| 30 mM | 0.1441 mL | 0.7206 mL | 1.4411 mL | 3.6028 mL | |
| 40 mM | 0.1081 mL | 0.5404 mL | 1.0808 mL | 2.7021 mL | |
| 50 mM | 0.0865 mL | 0.4323 mL | 0.8647 mL | 2.1617 mL | |
| 60 mM | 0.0721 mL | 0.3603 mL | 0.7206 mL | 1.8014 mL | |
| 80 mM | 0.0540 mL | 0.2702 mL | 0.5404 mL | 1.3511 mL | |
| 100 mM | 0.0432 mL | 0.2162 mL | 0.4323 mL | 1.0808 mL |
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