1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. Rapacuronium bromide

Rapacuronium bromide (Synonyms: Org 9487)

Cat. No.: HY-16423 Purity: >98.0%
Handling Instructions

Rapacuronium bromide is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).

For research use only. We do not sell to patients.

Rapacuronium bromide Chemical Structure

Rapacuronium bromide Chemical Structure

CAS No. : 156137-99-4

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10 mM * 1 mL in DMSO USD 522 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
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10 mg USD 550 In-stock
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50 mg USD 1600 In-stock
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100 mg USD 2600 In-stock
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Description

Rapacuronium bromide is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).

IC50 & Target

Muscarinic receptor[1]

In Vitro

Rapacuronium binds to all muscarinic receptor subtypes at physiologically relevant concentrations and displays micromolar affinity and slight selectivity towards M2 receptor. Rapacuronium exhibits complex effects on the kinetics of ACh binding and subsequent receptor activation estimated from stimulation of [35S]GTPγS binding. Rapacuronium alone concentration dependently lowers [35S]GTPγS binding to membranes with a maximal effect of approximately 25% at odd-numbered subtypes and 15% at even-numbered subtypes, with EC50 ranging from 28 μM at M2 receptors to 76 μM at M3 receptors. While the EC50 values of Rapacuronium in inhibiting [35S]GTPγS binding at individual subtypes correlated with affinities measured in binding experiments with [3H]ACh (R2 = 0.76) they are lower (4- to 12-fold) at all subtypes. Measurements of ACh-stimulated [35S]GTPγS binding in the presence of 0.1, 1 and 10 μM Rapacuronium shows differential effects of Rapacuronium on receptor activation by an orthosteric agonist at individual receptor subtypes. At even-numbered subtypes 1 μM and 10 μM Rapacuronium significantly increases ACh EC50, with lowering of EMAX at 10 μM Rapacuronium. At this subtype 0.1 and 1 μM Rapacuronium causes a significant 2-fold decrease in ACh EC50 and approximately 60% and 35% increase in EMAX, respectively. Rapacuronium at 10 μM increases ACh EC50 by about 3-fold without a significant change in EMAX. Rapacuronium (0.1 - 10 μM) has no effect on ACh efficacy at the M1 and M5 subtypes but decreases the EC50 of ACh in stimulating [35S]GTPγS binding by 1.5- and 4-fold, respectively, at concentrations of 0.1 and 1 μM. However, this effect is not evident at 10 μM Rapacuronium[1].

In Vivo

Time course of the neuromuscular effects of Rapacuronium following the administration of the 2×ED90 doses to rats and guinea-pigs with ED90 of 5953±199 and 187±16 µg/kg in rat and guinea pig, respectively[2].

Molecular Weight

677.80

Formula

C₃₇H₆₁BrN₂O₄

CAS No.

156137-99-4

SMILES

C[[email protected]@]12[[email protected]](CC[[email protected]]3([H])[[email protected]]2([H])CC[[email protected]@]4(C)[[email protected]@]3([H])C[[email protected]]([N+]5(CC=C)CCCCC5)[[email protected]@H]4OC(CC)=O)([H])C[[email protected]](OC(C)=O)[[email protected]@H](N6CCCCC6)C1.[Br-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (184.42 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4754 mL 7.3768 mL 14.7536 mL
5 mM 0.2951 mL 1.4754 mL 2.9507 mL
10 mM 0.1475 mL 0.7377 mL 1.4754 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.07 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.07 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.07 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

For determination of [35S]GTPγS binding to G-proteins in membranes a final concentration of 200 pM (M1, M3 and M5 receptors) or 500 pM (M2 and M4 receptors) of [35S]GTPγS is used. Incubation medium is supplemented with 5 μM (M1, M3 and M5 receptors) or 50 μM (M2 and M4 receptors) GDP. Nonspecific binding is determined in the presence of 1 μM unlabeled GTPγS. When effects of Rapacuronium on ACh-stimulated [35S]GTPγS binding is measured Rapacuronium is added to membranes 60 min prior to ACh and [35S]GTPγS. Incubation with [35S]GTPγS is carried out for 20 min and free ligand is removed by filtration as described above. Filtration and washing with ice-cold water lasted for 9 s (wash-aspirate button time). After filtration filters are dried in vacuum for 1 h while heated at 80°C and then solid scintillator Meltilex A is melted on filters (105°C, 90 s) using a hot plate. After cooling the filters are counted using a Wallac Microbeta scintillation counter[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

RapacuroniumOrg 9487Org9487Org-9487mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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Product Name:
Rapacuronium bromide
Cat. No.:
HY-16423
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