| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
ATP-sensitive potassium (KATP) channels, composed of Kir6.x and SUR subunits. Pinacidil activates these channels by binding to the SUR subunit, increasing open probability. This leads to K+ efflux, hyperpolarization, closure of voltage-gated Ca2+ channels, and vasodilation. It shows tissue selectivity with Ki values of 104 nM in guinea pig bladder and 251 nM in heart, indicating higher affinity for smooth muscle isoforms.
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| ln Vitro |
Pinacidil monohydrate is a potassium channel activator [1]. Pinacidil hydrate is an antihypertensive medication classified as a "potassium channel opener" [2]. Pinacidil hydrate activates ATP-regulated potassium channels in the Guinea pig bladder and heart at Ki values of 104 and 251 nM, respectively [3].
In vitro, Pinacidil activates KATP channels in patch-clamp studies, inducing a time-independent outward current in cardiac and smooth muscle cells. It relaxes pre-contracted arterial rings (e.g., porcine coronary, human internal mammary) with EC50 values in the range of 0.1–1 µM. The relaxation is reversed by KATP channel blockers like glibenclamide. It also inhibits spontaneous contractions in urinary bladder strips. |
| ln Vivo |
In vivo, Pinacidil lowers blood pressure by reducing peripheral vascular resistance. In spontaneously hypertensive rats, oral or intravenous administration produces dose-dependent hypotension lasting several hours. It enhances K+ efflux and hyperpolarizes smooth muscle, resulting in vasodilation of resistance vessels. It is effective in all grades of hypertension and is often combined with a diuretic or beta-blocker to counteract reflex tachycardia.
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| Enzyme Assay |
Cell-free assays use inside-out or outside-out membrane patches from cells expressing KATP channels (e.g., HEK-293 co-expressing Kir6.2 and SUR2B). Pinacidil is applied to the bath, and single-channel currents are recorded under voltage-clamp. Open probability is calculated. Alternatively, rubidium (86Rb+) efflux assays using membrane vesicles or loaded cells measure channel activity. EC50 for activation is determined from concentration-response curves.
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| Cell Assay |
Vascular smooth muscle cells (e.g., from rat aorta) are cultured and loaded with a fluorescent membrane potential dye. Cells are pre-contracted with phenylephrine or KCl, then exposed to increasing concentrations of Pinacidil. The change in fluorescence (hyperpolarization) is measured. Relaxation of isolated arterial rings in organ baths is also used: rings are mounted on force transducers, pre-contracted, and cumulative concentration-relaxation curves are generated. The pD2 (-log EC50) is calculated.
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| Animal Protocol |
In vivo, Pinacidil is typically administered orally (1–5 mg/kg) or intravenously (0.1–0.5 mg/kg) to spontaneously hypertensive rats or dogs. Blood pressure is monitored via indwelling catheters or telemetry. Heart rate is measured simultaneously. The duration of action and peak effect are recorded. In combination studies, co-administration with hydrochlorothiazide or propranolol is performed to assess additive effects. Pharmacokinetic sampling from blood is done to correlate plasma levels with efficacy.
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| ADME/Pharmacokinetics |
Molecular formula C13H21N5O·H2O, MW 263.34. White powder, mp 164-165°C. Solubility: DMSO 97 mg/mL, ethanol 47 mg/mL. Storage: powder at -20°C for up to 3 years. Purity >98%. For oral administration, prepare suspension in 0.5% methylcellulose. For IV, dissolve in saline with pH adjustment. LogP ~1.9, moderate plasma protein binding (~60%).
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| Toxicity/Toxicokinetics |
Well-tolerated in preclinical and clinical studies. Common side effects: headache, flushing, edema (due to vasodilation). Tachycardia may occur due to reflex sympathetic activation. No significant hepatotoxicity or nephrotoxicity reported. In clinical trials, adverse effects were mild and transient. Contraindicated in patients with hypersensitivity. Safety in pregnancy not established.
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| References |
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| Additional Infomation |
Pinacidil is an organic molecular entity. It is a guanidine compound that opens potassium channels and directly dilates peripheral arterioles. It lowers blood pressure and peripheral resistance and causes fluid retention. (Martindale Pharmacopoeia, 31st edition) See also: Pinacidil (note moved here).
Pinacidil was developed as an antihypertensive agent but is not currently marketed in many countries due to availability of newer drugs. It remains a research tool for studying KATP channel physiology. It has been used in experimental models of asthma, overactive bladder, and ischemia-reperfusion injury. Its mechanism has provided insights into the role of KATP channels in vascular tone. No recent clinical trials are ongoing. |
| Molecular Formula |
C13H19N5.H2O
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|---|---|
| Molecular Weight |
263.33874
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| Exact Mass |
263.174
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| CAS # |
85371-64-8
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| Related CAS # |
Pinacidil;60560-33-0
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| PubChem CID |
55329
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| Appearance |
White to off-white solid powder
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| Boiling Point |
356.7ºC at 760 mmHg
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| Melting Point |
164-165ºC
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| Flash Point |
169.5ºC
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| LogP |
2.945
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
19
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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 |
AFJCNBBHEVLGCZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H19N5.H2O/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);1H2
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| Chemical Name |
1-cyano-2-(3,3-dimethylbutan-2-yl)-3-pyridin-4-ylguanidine;hydrate
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~379.74 mM)
Ethanol : ~50 mg/mL (~189.87 mM) H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.49 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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 (9.49 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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 (9.49 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 1.83 mg/mL (6.95 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 18.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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 5: ≥ 1.83 mg/mL (6.95 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 18.3 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. Solubility in Formulation 6: ≥ 1.83 mg/mL (6.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 18.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7974 mL | 18.9869 mL | 37.9737 mL | |
| 5 mM | 0.7595 mL | 3.7974 mL | 7.5947 mL | |
| 10 mM | 0.3797 mL | 1.8987 mL | 3.7974 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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