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Tegaserod Maleate

Name: Tegaserod Maleate
Brand: Selleck Chemicals
SKU: S5401
Rating: 5 (2 reviews)

Synonyms: HTF-919

Catalog No.S5401 Purity: 99.89%

Tegaserod Maleate(HTF-919) is a hydrogen maleate salt form of tegaserod, which is a 5-HT4 receptor partial agonist and binds with high affinity to 5-HT4 receptors. It has limited affinity for 5-HT1 receptors and no appreciable affinity for other 5-HT receptors, muscarinic, adrenergic, dopaminergic or opiate receptors.

Tegaserod Maleate Chemical Structure

CAS: 189188-57-6

Selleck's Tegaserod Maleate has been cited by 2 publications

Purity & Quality Control

Batch: S540101 DMSO] 83 mg/mL] false] Ethanol] 8 mg/mL] false] Water] Insoluble] false Purity: 99.89%

99.89

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Biological Activity

Description

Targets

5-HT4 receptor ^[1]

In vitro
In vitro	In guinea-pig and rat colon, luminal application of tegaserod activates 5-HT4 receptors on intrinsic primary sensory neurons that release calcitonin gene-related peptide which in turn activates cholinergic interneurons stimulating the peristaltic reflex. In isolated segments of guinea-pig colon, intralumnal tegaserod increased the velocity of propulsion of artificial faecal pellets through the stimulation of the same receptor. In rat distal colon, intraluminal tegaserod stimulated 5-HT4 4 receptors on colonocytes to secrete chloride and water through an adenylyl cyclase-dependent pathway^[1].

In Vivo
In vivo	In a study in dogs tegaserod 0.1 or 0.3 mg/kg i.v. increased the motility of the antrum, duodenum and jejunum in both fasting and fed conditions. In a model of delayed gastric emptying, the same doses of tegaserod restored normal gastric transit time. Tegaserod 0.3 mg/kg in rats was able to increase gastric and small bowel motility while in a model of postoperative ileus it was able to restore gastric motility. In humans, pharmacokinetic analysis reveals that tegaserod is rapidly absorbed following oral administration. Absolute bioavailability is 11 ± 3% and is decreased by 50% under fed conditions. The time to reach peak plasma concentration ranges from 1-1.3 h. In the bloodstream, tegaserod is predominantly bound by α1-glycoprotein and does not cross the blood-brain barrier to any significant extent. The terminal elimination half time is 11 ± 5 h. Age and gender do not influence the pharmacokinetics of tegaserod and tegaserod has the potential for good tolerability^[1].

References

[1] Corsetti M, et al. Expert Opin Pharmacother. 2002, 3(8):1211-8.

Chemical lnformation & Solubility

Molecular Weight	417.46	Formula	C₁₆H₂₃N₅O.C₄H₄O₄
CAS No.	189188-57-6	SDF	--
Smiles	CCCCCN=C(N)NN=CC1=CNC2=C1C=C(C=C2)OC.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 83 mg/mL ( (198.82 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble

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In vivo
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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.

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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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