| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Pipecuronium bromide targets nicotinic acetylcholine receptors (nAChRs) at the neuromuscular junction. It acts as a competitive antagonist, binding to the receptor with an apparent Kd of 3.06 µM. By blocking the binding of acetylcholine, it prevents depolarization of the motor endplate, leading to muscle relaxation. This non-depolarizing mechanism is the basis for its use as a muscle relaxant during surgery.
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| ln Vitro |
Pipecuronium is highly affinized for sgammadex. Relative blocking can be achieved with fewer molecules than rocuronium because pipecuronium is roughly six to seven times more powerful than that drug [1].
In vitro, Pipecuronium bromide binds to nicotinic acetylcholine receptors (nAChRs) with an apparent Kd of 3.06 µM. Its activity is characterized by its ability to competitively antagonize the effects of acetylcholine at the neuromuscular junction. This results in muscle relaxation, which is the basis for its pharmacological use. It is a bisquaternary ammonium compound. |
| ln Vivo |
The onset of action of pipecuronium varies between 2 and 6.3 minutes, depending on the dosage and background anesthesia. Its mean ED95 is 0.045 mg/kg (0.035-0.059 mg/kg). Even at doses of 3× ED95, pipecuronium has no cardiovascular side effects, does not release histamine, and does not seem to cause allergic reactions [2]. It was demonstrated that carboxymethylated γ-cyclodextrin could completely and successfully reverse the effects of pipecuronium-induced neuromuscular blockade in experiments conducted on isolated rat diaphragms [3].
In vivo, Pipecuronium bromide is a potent, long-acting, non-depolarizing neuromuscular blocking agent. It is used as a muscle relaxant during general anesthesia, particularly for patients undergoing coronary artery bypass graft surgery. Its long duration of action makes it suitable for prolonged surgical procedures. It is administered intravenously. |
| Enzyme Assay |
In vitro receptor binding assays for Pipecuronium bromide involve measuring its affinity for nicotinic acetylcholine receptors (nAChRs). Radioligand binding studies using ¹²⁵I-α-bungarotoxin are performed on membranes from tissues or cells expressing the receptor. The compound is incubated with increasing concentrations, and its Kd of 3.06 µM is determined. Functional assays measure its ability to antagonize acetylcholine-induced muscle contraction in isolated tissue preparations.
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| Cell Assay |
For in vitro cell-based assays, cells expressing nAChRs are cultured and treated with Pipecuronium bromide. Its antagonism is confirmed by its ability to block acetylcholine-induced calcium flux or ion flux. Its effects on cell viability are measured using standard assays. However, its primary use is in physiological preparations, such as the isolated phrenic nerve-hemidiaphragm preparation, to measure muscle twitch inhibition.
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| Animal Protocol |
In vivo animal studies with Pipecuronium bromide are conducted to assess its neuromuscular blocking activity. Animals are anesthetized, and the compound is administered intravenously. Muscle relaxation is measured by monitoring the twitch response of a muscle (e.g., the tibialis anterior) following nerve stimulation. Its duration of action and potency are compared to other neuromuscular blocking agents.
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| ADME/Pharmacokinetics |
Pipecuronium bromide (CAS: 52212-02-9) has a molecular weight of 762.70 g/mol and a molecular formula of C35H62Br2N4O4. It is also known as Arduan. It is a white to off-white solid and is soluble in water and saline. It is typically stored as a powder at room temperature. It is a steroidal neuromuscular blocking agent and a bisquaternary ammonium compound.
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| Toxicity/Toxicokinetics |
Pipecuronium bromide is an approved drug for use as a muscle relaxant during anesthesia. Its side effects are related to its mechanism of action and can include prolonged muscle relaxation, hypotension, and histamine release. It is contraindicated in patients with myasthenia gravis and other neuromuscular disorders. It has an established safety profile when used appropriately in a clinical setting.
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| References |
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| Additional Infomation |
Pipercuronium bromide is a steroidal ester. It is a piperazine-androstane derivative, belonging to the class of non-depolarizing neuromuscular blocking agents. It is used as a muscle relaxant in anesthesia and surgery.
Pipecuronium bromide is a potent, long-acting, non-depolarizing steroidal neuromuscular blocking agent. It is used as a muscle relaxant during general anesthesia, particularly in patients undergoing coronary artery bypass graft surgery. It binds to nicotinic acetylcholine receptors. It is an approved drug in many countries for this indication. |
| Molecular Formula |
C35H62N4O4+2.2[BR-]
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| Molecular Weight |
762.699180000001
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| Exact Mass |
760.314
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| CAS # |
52212-02-9
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| Related CAS # |
68399-58-6 (Parent)
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| PubChem CID |
65332
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.329
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| Melting Point |
262-264ºC
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
45
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| Complexity |
1060
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| Defined Atom Stereocenter Count |
10
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| SMILES |
CC(=O)O[C@H]1C[C@@H]2CC[C@@H]3[C@@H]([C@]2(C[C@@H]1N4CC[N+](CC4)(C)C)C)CC[C@]5([C@H]3C[C@@H]([C@@H]5OC(=O)C)N6CC[N+](CC6)(C)C)C.[Br-].[Br-]
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| InChi Key |
TXWBOBJCRVVBJF-YTGGZNJNSA-L
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| InChi Code |
InChI=1S/C35H62N4O4.2BrH/c1-24(40)42-32-21-26-9-10-27-28(35(26,4)23-31(32)37-15-19-39(7,8)20-16-37)11-12-34(3)29(27)22-30(33(34)43-25(2)41)36-13-17-38(5,6)18-14-36;;/h26-33H,9-23H2,1-8H3;2*1H/q+2;;/p-2/t26-,27+,28-,29-,30-,31-,32-,33-,34-,35-;;/m0../s1
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| Chemical Name |
[(2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)-17-acetyloxy-2,16-bis(4,4-dimethylpiperazin-4-ium-1-yl)-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl] acetate;dibromide
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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 : ~150 mg/mL (~196.67 mM)
H2O : ~100 mg/mL (~131.11 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3111 mL | 6.5557 mL | 13.1113 mL | |
| 5 mM | 0.2622 mL | 1.3111 mL | 2.6223 mL | |
| 10 mM | 0.1311 mL | 0.6556 mL | 1.3111 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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