| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
Pinacidil targets ATP-sensitive potassium channels (KATP channels). It acts as a potent activator of these channels, opening them and allowing potassium ions to flow out of cells. This leads to hyperpolarization of vascular smooth muscle cells, relaxation of smooth muscle, and peripheral vasodilation. It decreases peripheral vascular resistance, resulting in reduced blood pressure.
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| ln Vitro |
Pinacidil demonstrates potent potassium channel opening activity in vitro. It enhances K+-efflux in smooth muscle cells. Its activity is assessed by electrophysiological recordings (patch-clamp) in cells expressing KATP channels or by measuring membrane potential changes using fluorescent voltage-sensitive dyes. It relaxes smooth muscles in vitro. Its IC50 for KATP channel activation is in the micromolar range.
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| ln Vivo |
Pinacidil is an antihypertensive agent that has been used in the management of hypertension and angina pectoris. It acts by opening K+ channels, leading to peripheral arteriolar vasodilation and decreased peripheral vascular resistance. It significantly improves cardiac function after reperfusion and has direct cardioprotective effects. Its in vivo efficacy has been established through clinical use.
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| Enzyme Assay |
KATP channel activity assays are performed using patch-clamp electrophysiology in cells expressing KATP channels (e.g., HEK-293 cells transfected with Kir6.2 and SUR2A). Pinacidil is applied at varying concentrations, and K+ currents are recorded. Activation of KATP channels is measured as an increase in outward K+ current. EC50 values for channel activation are determined by non-linear regression analysis. Each concentration is tested in multiple cells. Rb+ efflux assays are also used to measure channel activity.
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| Cell Assay |
Cellular KATP channel activation is evaluated in vascular smooth muscle cells or cell lines expressing KATP channels. Cells are cultured in appropriate media and treated with Pinacidil at various concentrations (0.1-100 µM). Membrane potential is measured using fluorescent voltage-sensitive dyes (e.g., DiBAC4(3)). K+ efflux is measured using Rb+ or Tl+ flux assays. Cell viability is assessed using MTT or LDH assays. Each experiment includes known KATP channel openers (e.g., diazoxide, cromakalim) as positive controls.
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| Animal Protocol |
In vivo studies are conducted in animal models of hypertension. Pinacidil is administered orally or intravenously at doses determined by preclinical studies. Blood pressure is measured by telemetry or tail-cuff methods. Heart rate and cardiac function are assessed. For cardioprotection studies, animal models of ischemia-reperfusion injury are used. Sample sizes typically range from 6-10 animals per group. Clinical studies have been conducted for hypertension and angina.
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| ADME/Pharmacokinetics |
Pinacidil has a molecular weight of 245.32 g/mol and a molecular formula of C13H19N5. IUPAC name: 1-cyano-2-(3,3-dimethylbutan-2-yl)-3-pyridin-4-ylguanidine. Synonyms: (R,S)-Pinacidil, P-1134, Pindac, S-1230. Solubility: soluble in DMSO. Storage: typically at room temperature. As an antihypertensive agent, it is orally administered.
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| Toxicity/Toxicokinetics |
Pinacidil is generally well-tolerated at therapeutic doses. Common adverse effects may include headache, flushing, palpitations, and edema due to vasodilation. It is contraindicated in patients with certain cardiovascular conditions. Standard toxicology studies have demonstrated an acceptable safety profile for its approved uses. It has been used clinically for hypertension and angina.
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| References |
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| Additional Infomation |
1-Cyano-2-(3,3-dimethylbutyl-2-yl)-3-pyridin-4-ylguanidine belongs to the pyridine class of compounds. Pinafenidil is a cyanoguanidine drug whose mechanism of action is through the opening of ATP-sensitive potassium channels, leading to vasodilation of peripheral arterioles and reducing peripheral vascular resistance. This process lowers blood pressure. This drug has been discontinued by the U.S. Food and Drug Administration (FDA). A guanidine drug that directly dilates peripheral arterioles by opening potassium channels, thereby lowering blood pressure and peripheral vascular resistance, and causing fluid retention. (Martindale Pharmacopeia, 31st Edition)
Pinacidil is also known as P-1134, Pindac, and S-1230. It is a guanidine derivative with vasodilatory properties. It acts as a potent activator of ATP-sensitive potassium channels. It is an antihypertensive agent used in the management of hypertension and angina pectoris. Regulatory approvals exist in some countries. |
| Molecular Formula |
C13H19N5
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|---|---|
| Molecular Weight |
245.33
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| Exact Mass |
245.164
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| CAS # |
60560-33-0
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| Related CAS # |
Pinacidil monohydrate;85371-64-8
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| PubChem CID |
4826
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| Appearance |
White to off-white solid powder
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| Density |
1.1402 (rough estimate)
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| Boiling Point |
378.29°C (rough estimate)
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| Melting Point |
110-114℃
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| Index of Refraction |
1.6500 (estimate)
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| LogP |
2.818
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
18
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| Complexity |
327
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C(C)(C)C)N=C(NC#N)NC1=CC=NC=C1.O
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| InChi Key |
IVVNZDGDKPTYHK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H19N5/c1-10(13(2,3)4)17-12(16-9-14)18-11-5-7-15-8-6-11/h5-8,10H,1-4H3,(H2,15,16,17,18)
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| Chemical Name |
(Z)-2-cyano-1-(3,3-dimethylbutan-2-yl)-3-(pyridin-4-yl)guanidine
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| Synonyms |
P 1134 P-1134 PinacidilS-1230 S 1230P1134 S1230
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~407.63 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.19 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0761 mL | 20.3807 mL | 40.7614 mL | |
| 5 mM | 0.8152 mL | 4.0761 mL | 8.1523 mL | |
| 10 mM | 0.4076 mL | 2.0381 mL | 4.0761 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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