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Lidocaine Histamine Receptor agonist

Cat.No.S1357

Lidocaine (Alphacaine) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.
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Quality Control

Batch: S135701 DMSO]47 mg/mL]false]Ethanol]47 mg/mL]false]Water]9 mg/mL]false Purity: 99.97%
99.97

Solubility

In vitro
Batch:

DMSO : 47 mg/mL (200.56 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 47 mg/mL

Water : 9 mg/mL

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

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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.)

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%
% Tween 80
% ddH2O
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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.

Chemical Information, Storage & Stability

Molecular Weight 234.34 Formula

C14H22N2O

Storage (From the date of receipt)
CAS No. 137-58-6 Download SDF Storage of Stock Solutions

Synonyms Alphacaine SMILES CCN(CC)CC(=O)NC1=C(C=CC=C1C)C

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
Histamine H1 receptor
>32 μM
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-01-23)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07361549 NOT_YET_RECRUITING
Refractory Migraine; Headache
Daniel A Tonetti, MD
2026-03 PHASE2
NCT07793552 NOT_YET_RECRUITING
Vulvar Cancers; Vulva Neoplasm; Vulvar Dysplasia
Tufts Medical Center
2026-11
NCT07709390 RECRUITING
Emergency Coughing
Ohio State University
2023-05-31 EARLY_PHASE1
NCT07631364 NOT_YET_RECRUITING
Neisseria Gonorrhoeae (Ng) Infections
Assistance Publique - Hôpitaux de Paris
2026-09 PHASE3
NCT07794878 RECRUITING
Nasolabial Folds
AbbVie
2026-08-19 PHASE3
NCT07778043 NOT_YET_RECRUITING
Myofacial Pain; Pelvic Pain
Women and Infants Hospital of Rhode Island
2026-08-17 PHASE4

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