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Rocuronium Bromide AChR inhibitor

Cat.No.S1397

Rocuronium Bromide (ORG 9426) is a competitive AchR antagonist, used in modern anaesthesia.
Rocuronium Bromide AChR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 609.68

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 609.68 Formula

C32H53N2O4.Br

Storage (From the date of receipt)
CAS No. 119302-91-9 Download SDF Storage of Stock Solutions

Synonyms ORG 9426 Smiles CC(=O)OC1C(CC2C1(CCC3C2CCC4C3(CC(C(C4)O)N5CCOCC5)C)C)[N+]6(CCCC6)CC=C.[Br-]

Solubility

In vitro
Batch:

DMSO : 122 mg/mL (200.1 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 122 mg/mL

Ethanol : 122 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Mechanism of Action

Targets/IC50/Ki
AChR [1]
In vitro
Rocuronium bromide (RB), an aminosteroid type neuromuscular blocking agent, acts by reducing or inhibiting the depolarising effect of acetylcholine on the terminal disc of the muscle cell. [1] Rocuronium interacts with human liver microsomal cytochromes P450 (CYP) by binding to the substrate site. Rocuronium has caused inhibition of both reactions by 20 and 15%, respectively. [2]
In vivo
Rocuronium is an ideal muscle relaxant with a rapid onset, intermediate duration of action, nondepolarizing properties and lack of cardiovascular side effects. Rocuronium produces a dose-dependent duration of neuromuscular blockade in isoflurane anesthetized horses. [3] Rocuronium bromide, is a relatively low potency, intermediate-acting agent with a rapid onset time of 98 seconds in dogs. [4] Rocuronium is an effective nondepolarizing muscle relaxant in the cat under the clinical conditions of this study. Rocuronium has a rapid onset, a short duration of action. [5] Rocuronium (0.6 mg/kg) results in a significant increase in heart rate one min after IV administration in the dog. Rocuronium (0.3 mg/kg and 0.6 mg/kg) produce a reliable neuromuscular block of 23–32 min duration, respectively. [6] Rocuronium bromide paralyzes the internal laryngeal muscles keeping the vocal cords in an intermediate position (paramedial) 60 seconds after being administered in cats. [7]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/12711837/
  • [5] https://pubmed.ncbi.nlm.nih.gov/16764586/
  • [6] https://pubmed.ncbi.nlm.nih.gov/16426875/
  • [7] https://pubmed.ncbi.nlm.nih.gov/23480130/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05619848 Completed
Spinal Stenosis Lumbar
Zheng Guo|Second Hospital of Shanxi Medical University
October 25 2022 Early Phase 1
NCT00675792 Completed
Anesthesia
Merck Sharp & Dohme LLC
May 2008 Phase 3

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