Pinacidil (Synonyms: P-1134)

Name: Pinacidil
Brand: MedChemExpress
SKU: HY-14290
Rating: 5.0 (4 reviews)

Cat. No.: HY-14290 Purity: 99.89%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

Pinacidil Chemical Structure

CAS No. : 60560-33-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Pinacidil:

Pinacidil monohydrate In-stock
Pinacidil (Standard) Get quote

4 Publications Citing Use of MCE Pinacidil

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

potassium channel^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
C6	EC₅₀	60.8 μM Compound: Pinacidil	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	[PMID: 19101153]
COS-7	EC₅₀	21.6 μM Compound: Pinacidil	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	[PMID: 19101153]
TE-671	EC₅₀	3.54 μM Compound: Pinacidil	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	[PMID: 19101153]
U-373MG ATCC	IC₅₀	> 100 μM Compound: R/S-pinacidil	Growth inhibition of human U373 cells after 72 hrs by MTT assay Growth inhibition of human U373 cells after 72 hrs by MTT assay	[PMID: 22809560]

In Vitro

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 K_ATP 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.

In Vivo

Pinacidil (3-30 μg, i.c.v., one single dose) increases tail-flick latency dose-dependently in non- diabetic (ED₅₀ = 16.1) and diabetic mice (ED₅₀ = 22.3)^[4].
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.

Molecular Weight

245.32

Formula

C₁₃H₁₉N₅

CAS No.

60560-33-0

Appearance

Solid

Color

White to off-white

SMILES

CC(C(C)(C)C)N/C(NC1=CC=NC=C1)=N\C#N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.0763 mL	20.3815 mL	40.7631 mL
5 mM	0.8153 mL	4.0763 mL	8.1526 mL
10 mM	0.4076 mL	2.0382 mL	4.0763 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (10.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.89%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (247 KB) LCMS (104 KB)

Handling Instructions (2659 KB)

References

[1]. Hamilton TC, et al., Cromakalim, nicorandil and pinacidil: novel drugs which open potassium channels in smooth muscle. Gen Pharmacol. 1989;20(1):1-9. [Content Brief]

[2]. Jung-Ae Kim, et al., Activation of Na+, K+, Cl−-Cotransport Mediates Intracellular Ca2+ Increase and Apoptosis Induced by Pinacidil in HepG2 Human Hepatoblastoma Cells, Biochemical and Biophysical Research Communications, Volume 281, Issue 2, 2001, Pages 511-519, ISSN 0006-291X,

[3]. Weston, A.H., et al., In Vitro Studies on the Mode of Action of Pinacidil. Drugs 36 (Suppl 7), 10–28 (1988).

[4]. Ko Zushida, et al ., Effect of diabetes on pinacidil-induced antinociception in mice, European Journal of Pharmacology, Volume 453, Issues 2–3, 2002, Pages 209-215, ISSN 0014-2999.

Complete Stock Solution Preparation Table

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

Pinacidil Related Classifications

Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pinacidil60560-33-0P-1134P1134P 1134Potassium ChannelKcsApotassium channelantihypertensivereperfusioncardiac compliancecardioprotectivevasorelaxantcardiovascularInhibitorinhibitorinhibit

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Pinacidil (Synonyms: P-1134)

Customer Review

Other Forms of Pinacidil:

Pinacidil Related Antibodies

4 Publications Citing Use of MCE Pinacidil

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Pinacidil Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Pinacidil Related Classifications

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