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VUF 10166 5-HT Receptor antagonist

Name: VUF 10166
Brand: Selleck Chemicals
SKU: S2865
Rating: 5 (1 reviews)

Cat.No.S2865

VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with K_i of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower.

Chemical Structure

Molecular Weight: 262.74

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Quality Control

Batch: S286501 Ethanol]61 mg/mL]false]DMSO]21 mg/mL]false]Water]Insoluble]false Purity: 99.77%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.77

Related Targets	Adrenergic Receptor AChR COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other 5-HT Receptor Inhibitors	WAY-100635 Maleate Serotonin (5-HT) HCl Puerarin BRL-15572 Dihydrochloride SB269970 HCl Ketanserin RS-127445 Nuciferine Flopropione BRL-54443

Chemical Information, Storage & Stability

Molecular Weight	262.74	Formula	C₁₃H₁₅ClN₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	155584-74-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN1CCN(CC1)C2=NC3=CC=CC=C3N=C2Cl

Solubility

In vitro
Batch:

Ethanol : 61 mg/mL

DMSO : 21 mg/mL (79.92 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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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+ %

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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	5-HT3A 0.04 nM(Ki) 5-HT3AB 22 nM(Ki)
In vitro	VUF10166 shows low activity to 5-HT₃AB receptor with K_i of 22 nM. VUF10166 may be used to can distinguish between 5-HT₃A and 5-HT₃AB receptors. VUF10166 has no activity to 7 nACh receptor. VUF10166 also acts as a partial agonist at 5-HT3A receptors with EC50 of 5.2 , which shows that VUF10166 is unlikely to bind in the receptor pore.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22306960/

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