Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Pirmenol HCl (Cl-845) is a potent antiarrhythmic agent that inhibits muscarinic acetylcholine receptor-operated K+ current in the guinea pig heart. Pirmenol has an IC50 of 0.1 μM for inhibiting Carbachol-induced IK.ACh. Pirmenol has a favorable therapeutic index when compared to other class I agents and is active in a variety of experimental arrhythmic models with different etiologies. Pirmenol has a high degree of effectiveness regardless of the type of arrhythmia—atrial, ventricular, chemically, mechanically, electrically, or reentrant.
Targets |
IK.ACh ( IC50 = 40.1 μM )
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ln Vitro |
Pirmenol (1 μM) hydrochloride inhibits the IK.ACh triggered by carbachol or intracellular loading of GTPg S in in atrial cells[1].
Pirmenol (5 μM) hydrochloride prolongs the final repolarization of the action potentials and depresses the early portion of the plateau in ventricular myocytes[3]. Pirmenol (1 μM) hydrochloride extends the action potential duration at 90% repolarization in atrial muscles and Purkinje fibers[3]. |
ln Vivo |
Pirmenol (2.5 and 5 mg/kg, p.o.) hydrochloride is efficient in treating arrhythmias in dogs with ligated coronary arteries who are conscious[4].
Pirmenol (rats) hydrochloride demonstrates LD50s of 359.9 mg/kg (p.o), 23.6 mg/kg (i.v.)[2]. Pirmenol (mice) hydrochloride demonstrates LD50s of 215.5 mg/kg (p.o), 20.8 mg/kg (i.v.)[2]. |
Animal Protocol |
Conscious, coronary artery ligated dogs
Oral administration (p.o.) 2.5 and 5 mg/kg |
References |
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Molecular Formula |
C₂₂H₃₁CLN₂O
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Molecular Weight |
374.95
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Exact Mass |
374.21
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Elemental Analysis |
C, 70.47; H, 8.33; Cl, 9.45; N, 7.47; O, 4.27
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CAS # |
61477-94-9
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Related CAS # |
Pirmenol; 68252-19-7
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Appearance |
Solid powder
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SMILES |
C[C@@H]1CCC[C@@H](N1CCCC(C2=CC=CC=C2)(C3=CC=CC=N3)O)C.Cl
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InChi Key |
HFIHPVIVQSWZBV-ROSXHPEZSA-N
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InChi Code |
InChI=1S/C22H30N2O.ClH/c1-18-10-8-11-19(2)24(18)17-9-15-22(25,20-12-4-3-5-13-20)21-14-6-7-16-23-21;/h3-7,12-14,16,18-19,25H,8-11,15,17H2,1-2H3;1H/t18-,19+,22?;
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Chemical Name |
4-[(2S,6R)-2,6-dimethylpiperidin-1-yl]-1-phenyl-1-pyridin-2-ylbutan-1-ol;hydrochloride
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Synonyms |
Cl-845; Cl 845Cl845; (±)-Pirmenol hydrochloride
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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 (e.g. under nitrogen), 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) |
H2O: ~100 mg/mL (~266.7 mM)
DMSO: ~66.7 mg/mL (~177.8 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.55 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 20.8 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: ≥ 2.08 mg/mL (5.55 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 20.8 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: ≥ 2.08 mg/mL (5.55 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 | 2.6670 mL | 13.3351 mL | 26.6702 mL | |
5 mM | 0.5334 mL | 2.6670 mL | 5.3340 mL | |
10 mM | 0.2667 mL | 1.3335 mL | 2.6670 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.