Pinacidil
Based on 4 publication(s) in Google Scholar
Pinacidil (P-1134) is a potent activator of ATP-sensitive potassium channel. Pinacidil is an antihypertensive agent hyperpolarizes vascular smooth muscle by opening K+ channels. Pinacidil enhances K+-efflux in smooth muscle. Pinacidil has vasorelaxant properties. Pinacidil is able to inhibit spontaneous tone and of reducing agonist induced contractions. Pinacidil can be studied in research area such as cardiovascular diseases.
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- Pureza: 99.88%
- No. CAS: 60560-33-0
- Fòrmula: C13H19N5
- Peso molecular:245.32
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Pinacidil
More
Actividad biológica
potassium channel[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Beta-TC6 | IC50 |
>100 μM
Compound: Pinacidil
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In vitro ability to inhibit glucose stimulated insulin release in beta-TC6 cells from rat islets
In vitro ability to inhibit glucose stimulated insulin release in beta-TC6 cells from rat islets
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[PMID: 15163199] |
| C6 | EC50 |
60.8 μM
Compound: Pinacidil
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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 |
21.6 μM
Compound: Pinacidil
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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] |
| Sf21 | IC50 |
221.6 μM
Compound: Pinacidil
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Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| Sf21 | IC50 |
348.1 μM
Compound: Pinacidil
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Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| TE-671 | EC50 |
3.54 μM
Compound: Pinacidil
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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] |
| U-373MG ATCC | IC50 |
>100 μM
Compound: R/S-pinacidil
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Growth inhibition of human U373 cells after 72 hrs by MTT assay
Growth inhibition of human U373 cells after 72 hrs by MTT assay
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[PMID: 22809560] |
| VSMC | EC50 |
0.62 μM
Compound: 2
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Myorelaxant effect in KCl-induced precontracted rat aorta ring VSMC
Myorelaxant effect in KCl-induced precontracted rat aorta ring VSMC
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[PMID: 21428460] |
Pinacidil (0-2 mM, 48 h) induces DNA fragmentation in a dose-dependent manner and is prominent at 1 mM in HepG2 cells[2].
Pinacidil (1-2 mM, 36 h) induces loss of phospholipid asymmetry, resulting in appearance of phosphatidylserine on the outer layer of the plasma membrane detected by annexin-V binding in HepG2 cells[2].
Pinacidil (1 mM, 0-48 h) induces apoptosis in a time-related manner without involvement of KATP channels in HepG2 cells[2].
Pinacidil (1 mM) induces a rapid and sustained increase in [K+] and [Ca2+] in HepG2 cells[2].
Pinacidil (1 mM, 0-60 min) induces Ca2+ influx through activation of the reverse mode of Na+/Ca2+ exchanger which is achieved by increased [Na+]i attributed to activation of NKCC[2].
Pinacidil (1-100 μM and 0.3-30 μM, 30 min) produces a concentration-dependent inhibition of responses to noradrenaline in rat aorta and portal vein[3].
Pinacidil (1-100 μM) produces a concentration-dependent inhibition of responses to KCl (10-80 mmol/L) in rat aorta[3].
Pinacidil (0.3-30 μM) produces an inhibition of responses to KCl (5-80 mmol/L) and the –log IC50 against KCl (20 mmol/L) contraction was 6.2[3].
Pinacidil (0.1-100 μM) is capable of producing almost total relaxation of tissue, and remains unaffected in the presence of Apamin (HY-P0256) (0.1 μM) in guinea-pig trachea[3].
Pinacidil (0.3-10 μM, 4.5-7 min) abolishes spontaneous multispike complexes and mechanical activity, and results in a concentration-dependent hyperpolarization in rat portal vein[3].
Pinacidil (0.3-30 μM, 10-35 min) produces a greater and longer lasting increase in 86Rb exchange in the aorta than in the portal vein[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pinacidil (10-100 μg, i.t., one single dose) produces dose-dependent and significant antinociception in diabetic mice and a dose of 100 μg results no significant antinociception in non-diabetic mice (ED50 = 18.5), whereas ED50 for diabetic mice is 95.6[4].
Pinacidil (30 μg, i.c.v., one single dose) is not affected by the pretreatment of β-Funaltrexamine (HY-101318) (20 and 40 mg/kg, s.c.) on the antinociception in diabetic mice[4].
Pinacidil (30 μg, i.t., one single dose) has a dose-dependently reduction of antinociceptive effect with β-Funaltrexamine (20 and 40 mg/kg, s.c.), and is antagonized by the pretreatment with 7-Benzylidenenaltrexon (HY-169867) (0.3 mg/kg), Naltriben (0.3 mg/kg) (HY-133717), or nor-Binaltorphimine (20 mg/kg, s.c.) (HY-117040) in diabetic mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 60560-33-0
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Appearance Solid
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Peso molecular 245.32
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Fòrmula C13H19N5
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Color White to off-white
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SMILES
CC(C(C)(C)C)N/C(NC1=CC=NC=C1)=N\C#N
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Synonyms
P-1134
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Bone Res
mTORC1 induces plasma membrane depolarization and promotes preosteoblast senescence by regulating the sodium channel Scn1a. [Abstract]2022 Mar 8;10(1):25. PMID: 35256591 -
Dev Cell
KCNJ8/ABCC9-containing K-ATP channel modulates brain vascular smooth muscle development and neurovascular coupling. [Abstract]2022 Jun 6;57(11):1383-1399.e7. PMID: 35588738 -
Sci Rep
Repositioning pinacidil and its anticonvulsant and anxiolytic properties in murine models. [Abstract]2024 Sep 30;14(1):22695. PMID: 39349563 -
Solvente y solubilidad
DMSO : 100 mg/mL (407.63 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)
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: ≥ 2.5 mg/mL (10.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (10.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 4.0763 mL | 20.3815 mL | 40.7631 mL | 101.9077 mL |
| 5 mM | 0.8153 mL | 4.0763 mL | 8.1526 mL | 20.3815 mL | |
| 10 mM | 0.4076 mL | 2.0382 mL | 4.0763 mL | 10.1908 mL | |
| 15 mM | 0.2718 mL | 1.3588 mL | 2.7175 mL | 6.7938 mL | |
| 20 mM | 0.2038 mL | 1.0191 mL | 2.0382 mL | 5.0954 mL | |
| 25 mM | 0.1631 mL | 0.8153 mL | 1.6305 mL | 4.0763 mL | |
| 30 mM | 0.1359 mL | 0.6794 mL | 1.3588 mL | 3.3969 mL | |
| 40 mM | 0.1019 mL | 0.5095 mL | 1.0191 mL | 2.5477 mL | |
| 50 mM | 0.0815 mL | 0.4076 mL | 0.8153 mL | 2.0382 mL | |
| 60 mM | 0.0679 mL | 0.3397 mL | 0.6794 mL | 1.6985 mL | |
| 80 mM | 0.0510 mL | 0.2548 mL | 0.5095 mL | 1.2738 mL | |
| 100 mM | 0.0408 mL | 0.2038 mL | 0.4076 mL | 1.0191 mL |
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