Home Neuronal Signaling Histamine Receptor antagonist Nizatidine For research use only.

Nizatidine

Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.

Nizatidine Chemical Structure

Nizatidine Chemical Structure

CAS No. 76963-41-2

Purity & Quality Control

Nizatidine Related Products

Signaling Pathway

Histamine Receptor Signaling Pathways

Histamine Receptor Signaling Pathway

Biological Activity

Description Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.
Targets
Histamine H2 receptor [1] AChE [2]
0.9 nM 6.7 μM
In vitro
In vitro Nizatidine, a selective histamine H2-receptor antagonist, is a potent inhibitor of gastric acid secretion, with IC50 of 0.9 nM. [1] Nizatidine also reversibly inhibits acetylcholinesterase (AChE), with IC50 of 6.7 μM, and the inhibition is noncompetitive, with a Ki value of 7.4 μM. [2]
In Vivo
In vivo Nizatidine exhibits maximal inhibition of gastric acid in rats within the first hour of drug administration, with EC50 of 1.383 μmol/kg. [1] Nizatidine (0.3-3 mg/kg, i.v.) significantly increases the motor index of gastrointestinal (GI) motility in a dose-dependent manner. Nizatidine inhibits gastric acid secretion with ED50 and ED90 of 0.18 and 3.22 mg/kg in dogs, and 2.94 and 19.6 mg/kg in rats, respectively. [2]
Animal Research Animal Models Rat
Dosages 0.5-10 μmol/kg
Administration s.c
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01409395 Completed
Healthy
University of California San Francisco|National Institute of General Medical Sciences (NIGMS)
 September 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 331.46 Formula

C12H21N5O2S2
CAS No. 76963-41-2 SDF Download Nizatidine SDF
Smiles CNC(=C[N+](=O)[O-])NCCSCC1=CSC(=N1)CN(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 66 mg/mL ( (199.11 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 66 mg/mL

Ethanol : 12 mg/mL


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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