| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
|
||
| Other Sizes |
| Targets |
Nicotinic acetylcholine receptors at autonomic ganglia (ganglionic blocker).
|
|---|---|
| ln Vitro |
In vitro, Pempidine acts as a ganglionic blocking agent by antagonizing nicotinic acetylcholine receptors at autonomic ganglia. Quantitative in vitro activity data (e.g., IC50 values) is not detailed in publicly available sources.
|
| ln Vivo |
In vivo, Pempidine is an orally bioactive ganglionic blocking agent used in patients with hypertension. It reduces blood pressure by blocking sympathetic ganglionic transmission. Detailed dose-response and pharmacokinetic data are limited in publicly available literature.
|
| Enzyme Assay |
No specific cell-free nicotinic receptor binding assay protocol is detailed for Pempidine. For ganglionic blockers, typical cell-free assays include radioligand binding studies using [3H]epibatidine or [125I]α-bungarotoxin and membrane preparations from tissues expressing nicotinic receptors.
|
| Cell Assay |
Cellular nicotinic receptor antagonism is assessed in cells expressing nicotinic receptors (e.g., ganglionic neurons or heterologous expression systems). Cells are treated with Pempidine and stimulated with nicotine or acetylcholine; inhibition of the response (e.g., ion flux, membrane depolarization) is measured.
|
| Animal Protocol |
In vivo efficacy is evaluated in animal models of hypertension or in clinical use. Pempidine is administered orally. Endpoints include blood pressure, heart rate, and sympathetic nerve activity.
|
| ADME/Pharmacokinetics |
Molecular weight: 155.28 g/mol; molecular formula: C10H21N. CAS No.: 79-55-0. Appearance: clear colorless to light yellow liquid. Boiling point: 187-188°C. Storage: typical for amines (protected from light, inert atmosphere).
|
| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a ganglionic blocker, potential side effects include orthostatic hypotension, dry mouth, blurred vision, constipation, and urinary retention due to autonomic blockade.
|
| References |
|
| Additional Infomation |
1,2,2,6,6-Pentamethylpiperidine is a type of piperidine compound. It is a nicotine receptor antagonist, most commonly used in laboratory settings. It was once used as a ganglion blocker to treat hypertension, but has since been superseded by more specific drugs.
Pempidine is a research-grade compound and was historically used as an antihypertensive agent. It is not commonly used in modern clinical practice due to the availability of safer antihypertensive drugs. No FDA approval in the US for current use has been reported. Its mechanism involves ganglionic nicotinic receptor blockade. |
| Molecular Formula |
C10H21N
|
|---|---|
| Molecular Weight |
155.28044
|
| Exact Mass |
155.167
|
| CAS # |
79-55-0
|
| Related CAS # |
546-48-5 (tartrate); 79-55-0; 6152-95-0 (HCl);
|
| PubChem CID |
6603
|
| Appearance |
Colorless to off-white liquid（Density：0.858 g/cm3 ）
|
| Density |
0.858 g/mL at 25 °C(lit.)
|
| Boiling Point |
187-188 °C(lit.)
|
| Melting Point |
137-141ºC
|
| Flash Point |
122 °F
|
| Index of Refraction |
n20/D 1.460(lit.)
|
| LogP |
2.597
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
11
|
| Complexity |
131
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N1(C(C)(C)CCCC1(C)C)C
|
| InChi Key |
XULIXFLCVXWHRF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C10H21N/c1-9(2)7-6-8-10(3,4)11(9)5/h6-8H2,1-5H3
|
| Chemical Name |
1,2,2,6,6-pentamethylpiperidine
|
| 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 : ≥ 2.1 mg/mL (~13.52 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (16.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (16.10 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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 3: ≥ 2.5 mg/mL (16.10 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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.4400 mL | 32.1999 mL | 64.3998 mL | |
| 5 mM | 1.2880 mL | 6.4400 mL | 12.8800 mL | |
| 10 mM | 0.6440 mL | 3.2200 mL | 6.4400 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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