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Caulophylline (N-Methylcytisine) AChR antagonist

Name: Caulophylline (N-Methylcytisine)
Brand: Selleck Chemicals
SKU: S3298
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S3298

Caulophylline (N-Methylcytisine, Caulophyllin, NMC) is a tricyclic quinolizidine alkaloid with anti-inflammatory activities. It binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. This compound significantly reduces myeloperoxidase (MPO) activity and blocks the activation of NF-κB by inhibiting IκB and IKK phosphorylation.

Chemical Structure

Molecular Weight: 204.27

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S329801 DMSO]100 mg/mL]false]]]false]]]false Purity: 99.85%

99.85

Related Targets	Adrenergic Receptor 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel GluR MAO Beta Amyloid NMDAR P2 Receptor Trk receptor Serotonin Transporter Notch Cannabinoid Receptor P-gp CaMK Opioid Receptor BACE Sigma Receptor FAAH Neurokinin Receptor OX Receptor CGRP Receptor BChE Adenosine Deaminase CCK receptor MT Receptor
Related Products	PNU-120596 Benzethonium Chloride Arecoline HBr Otilonium Bromide Lycorine Hyoscyamine (-)-Huperzine A (HupA) Nitenpyram Cytisine Chelidonine

Chemical Information, Storage & Stability

Molecular Weight	204.27	Formula	C₁₂H₁₆N₂O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	486-86-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Caulophyllin, NMC			Smiles	CN1CC2CC(C1)C3=CC=CC(=O)N3C2

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (489.54 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	MPO ^[2] IκB ^[2] IKK ^[2] NF-κB ^[2] nAChR ^[1] (Cell-free assay) 50 nM(Kd)
References	https://pubmed.ncbi.nlm.nih.gov/3689962/ https://pubmed.ncbi.nlm.nih.gov/29495327/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06302790	Recruiting	Mollii Suit\|Cerebral Palsy	Kırıkkale University\|Gazi University	March 1 2024	Not Applicable
NCT05689476	Recruiting	Work of Breathing\|Lung Transplantation\|Neurally Adjusted Ventilatory Assist\|Ventilator-Induced Lung Injury	University of Padova	December 27 2022	Not Applicable
NCT04457765	Withdrawn	Rhinoplasty	Boston Medical Center	April 2021	Early Phase 1
NCT04979013	Completed	Smoking\|Smoking Cessation\|Tobacco Use	RAI Services Company	May 30 2019	Not Applicable
NCT02012699	Recruiting	Pancreatic Cancer\|Thyroid Cancer\|Lung Cancer\|Esophageal Cancer\|Thymus Cancer\|Colon Cancer\|Rectal Cancer\|Gastrointestinal Stromal Tumors\|Anal Cancer\|Bile Duct Cancer\|Duodenal Cancer\|Gallbladder Cancer\|Gastric Cancer\|Liver Cancer\|Small Intestine Cancer\|Peritoneal Surface Malignancies\|Familial Adenomatous Polyposis\|Lynch Syndrome\|Bladder Cancer\|Kidney Cancer\|Penile Cancer\|Prostate Cancer\|Testicular Cancer\|Ureter Cancer\|Urethral Cancer\|Hypopharyngeal Cancer\|Laryngeal Cancer\|Lip Cancer\|Oral Cavity Cancer\|Nasopharyngeal Cancer\|Oropharyngeal Cancer\|Paranasal Sinus Cancer\|Nasal Cavity Cancer\|Salivary Gland Cancer\|Skin Cancer\|Central Nervous System Tumor\|Central Nervous System Cancer\|Mesothelioma\|Breast Cancer\|Leukemia\|Melanoma\|Sarcoma\|Unknown Primary Tumor\|Multiple Myeloma\|Ovarian Cancer\|Endometrial Cancer\|Vaginal Cancer\|Neuroendocrine Tumors\|Plasma Cell Dyscrasia\|Healthy Control	University of Nebraska	November 1 2013	--

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