| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥98%
Vecuronium (ORG NC 45) is a non-depolarizing neuromuscular blocking agent widely used as an adjunct to general anesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. . Vecuronium inhibits both forms of the muscle-type acetylcholine receptor with IC50 of 1-2 mM. Vecuronium combined with methylprednisolone shows additive effects on both receptor forms, which is best described by a two-site model, with each site independent. Vecuronium interferes with nicotinic processes in the carotid body and inhibits the chemoreceptor neural response to hypoxia. Vecuronium significantly attenuates the increase in CSNA (DeltaCSNA) in response to hypoxia in the carotid body.
| ln Vitro |
In adrenal medullary cells, vecuronium bromide (0-100 μM, 15 min) decreases [3H] norepinephrine (NE) uptake to 65% at 100 μM[1]. In a concentration-dependent manner, vecuronium bromide (0-15 μM, 72 hours) suppresses the proliferation and migration of cancer cells[2]. When combined with cisplatin, vecuronium bromide (0–15 μM, 72 hours) can dramatically lower cell viability[2].
|
|---|---|
| ln Vivo |
In Wister rats, vecuronium bromide (intravenous injection, 0–5 μM, every 30 min, 2 hours) suppresses the carotid body's neural response to acetylcholine (ACh) and attenuates the response of carotid sinus nerve activity (CSNA) to hypoxia in a dose-dependent manner[3].
|
| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: Lung cancer cell line (A549 ) Tested Concentrations: 0-15 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited cell proliferation at concentrations ranging from 5.0 μM to 15 μM. Cell Cytotoxicity Assay[2] Cell Types: Lung cancer cell line (A549) Tested Concentrations: 0-15 μM Incubation Duration: 72 hrs (hours) Experimental Results: Resulted in a decrease in cell viability from 10 μM to 15 Μm by combining with cisplatin. |
| Animal Protocol |
Animal/Disease Models: Wister rats weighing 250-350 g[3]
Doses: 0-5 μM Route of Administration: intravenous (iv) injection; every 30 min; 2 hrs (hours) Experimental Results: Dramatically diminished CSNA response to hypoxia at the concentration of 5 μM and decreased carotid sinus nerve response to ACh at 0.5 μM. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No information is available on the use of vecuronium during breastfeeding Because it is short acting, highly polar and poorly absorbed orally, it is not likely to reach the breastmilk in high concentration or to reach the bloodstream of the infant. When a combination of anesthetic agents is used for a procedure, follow the recommendations for the most problematic medication used during the procedure. General anesthesia for cesarean section using vecuronium as a component may delay the onset of lactation. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk A randomized study compared the effects of cesarean section using general anesthesia, spinal anesthesia, or epidural anesthesia, to normal vaginal delivery on serum prolactin and oxytocin as well as time to initiation of lactation. General anesthesia was performed using propofol 2 mg/kg and rocuronium 0.6 mg/kg for induction, followed by sevoflurane and rocuronium 0.15 mg/kg as needed. After delivery, patients in all groups received an infusion of oxytocin 30 international units in 1 L of saline, and 0.2 mg of methylergonovine if they were not hypertensive. Fentanyl 1 to 1.5 mcg/kg was administered after delivery to the general anesthesia group. Patients in the general anesthesia group (n = 21) had higher post-procedure prolactin levels and a longer mean time to lactation initiation (25 hours) than in the other groups (10.8 to 11.8 hours). Postpartum oxytocin levels in the nonmedicated vaginal delivery group were higher than in the general and spinal anesthesia groups. |
| References |
|
| Additional Infomation |
Vecuronium bromide is the organic bromide salt of a 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidinino- and 16beta-N-methylpiperidinium substituents. It has a role as a nicotinic antagonist, a neuromuscular agent and a muscle relaxant. It is a quaternary ammonium salt and an organic bromide salt. It contains a vecuronium. It is functionally related to a 5alpha-androstane.
Vecuronium Bromide is the bromide salt form of vecuronium, a synthetic steroid derivative of the naturally occurring alkaloids of curare with a muscle relaxant property. Vecuronium bromide competes with acetylcholine for the nicotinic receptors at the neuromuscular junction of skeletal muscles, thereby inhibiting the action of acetylcholine and blocking the neural transmission without depolarizing the postsynaptic membrane. This leads to skeletal muscle relaxation and paralysis. Monoquaternary homolog of PANCURONIUM. A non-depolarizing neuromuscular blocking agent with shorter duration of action than pancuronium. Its lack of significant cardiovascular effects and lack of dependence on good kidney function for elimination as well as its short duration of action and easy reversibility provide advantages over, or alternatives to, other established neuromuscular blocking agents. See also: Vecuronium (has active moiety). |
| Molecular Formula |
C34H57N2O4.BR
|
|
|---|---|---|
| Molecular Weight |
637.73
|
|
| Exact Mass |
636.35
|
|
| CAS # |
50700-72-6
|
|
| Related CAS # |
|
|
| PubChem CID |
39764
|
|
| Appearance |
White to off-white solid powder
|
|
| Melting Point |
227-229°C
|
|
| LogP |
2.866
|
|
| Hydrogen Bond Donor Count |
0
|
|
| Hydrogen Bond Acceptor Count |
6
|
|
| Rotatable Bond Count |
6
|
|
| Heavy Atom Count |
41
|
|
| Complexity |
958
|
|
| Defined Atom Stereocenter Count |
10
|
|
| SMILES |
CC(=O)O[C@H]1C[C@@H]2CC[C@@H]3[C@@H]([C@]2(C[C@@H]1N4CCCCC4)C)CC[C@]5([C@H]3C[C@@H]([C@@H]5OC(=O)C)[N+]6(CCCCC6)C)C.[Br-]
|
|
| InChi Key |
VEPSYABRBFXYIB-WSIGYWTFSA-M
|
|
| InChi Code |
InChI=1S/C34H57N2O4.BrH/c1-23(37)39-31-20-25-12-13-26-27(34(25,4)22-29(31)35-16-8-6-9-17-35)14-15-33(3)28(26)21-30(32(33)40-24(2)38)36(5)18-10-7-11-19-36;/h25-32H,6-22H2,1-5H3;1H/q+1;/p-1/t25-,26+,27-,28-,29-,30-,31-,32+,33-,34-;/m0./s1
|
|
| Chemical Name |
1-((2S,3S,5S,8R,9S,10S,13S,14S,16S,17S)-3,17-diacetoxy-10,13-dimethyl-2-(piperidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl)-1-methylpiperidin-1-ium bromide
|
|
| Synonyms |
ORG NC45; C 45; NC-45; NC45; ORG NC 45; ORG NC45; ORG-NC 45; ORG-NC-45; ORG-NC45; ORGNC 45; ORGNC45; Vecuronium bromide. Brand name Norcuron
|
|
| 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 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.26 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 (3.26 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 (3.26 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 | 1.5681 mL | 7.8403 mL | 15.6806 mL | |
| 5 mM | 0.3136 mL | 1.5681 mL | 3.1361 mL | |
| 10 mM | 0.1568 mL | 0.7840 mL | 1.5681 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA