| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Pinacidil (P 1134; P-1134; Pinacidil; S-1230; S 1230; P1134; S1230) is an orally bioavailable and guanidine-based antihypertensive drug acting as a potassium channel activator.
| References |
|
|---|---|
| Additional Infomation |
1-cyano-2-(3,3-dimethylbutan-2-yl)-3-pyridin-4-ylguanidine is a member of pyridines.
Pinacidil is a cyanoguanidine drug that acts by opening ATP-sensitive potassium channels, leading to peripheral vasodilatation of arterioles and decreasing peripheral vascular resistance. The above processes result in reduced blood pressure. This drug has been discontinued by the FDA. A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed) |
| Molecular Formula |
C13H19N5
|
|---|---|
| Molecular Weight |
245.33
|
| Exact Mass |
245.164
|
| CAS # |
60560-33-0
|
| Related CAS # |
Pinacidil monohydrate;85371-64-8
|
| PubChem CID |
4826
|
| Appearance |
White to off-white solid powder
|
| Density |
1.1402 (rough estimate)
|
| Boiling Point |
378.29°C (rough estimate)
|
| Melting Point |
110-114℃
|
| Index of Refraction |
1.6500 (estimate)
|
| LogP |
2.818
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
18
|
| Complexity |
327
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
IVVNZDGDKPTYHK-UHFFFAOYSA-N
|
| 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)
|
| Chemical Name |
(Z)-2-cyano-1-(3,3-dimethylbutan-2-yl)-3-(pyridin-4-yl)guanidine
|
| Synonyms |
P 1134 P-1134 PinacidilS-1230 S 1230P1134 S1230
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~407.63 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
