Name: Rizatriptan Benzoate
Brand: Selleck Chemicals
SKU: S1607
Rating: 5 (1 reviews)

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Quality Control

Batch: Purity: 99.98%

99.98

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	391.47	Formula	C₂₂H₂₅N₅O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	145202-66-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	MK-462 Benzoate			Smiles	CN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3.C1=CC=C(C=C1)C(=O)O

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (199.24 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 78 mg/mL

Ethanol : Insoluble

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.
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.
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.
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	5-HT1
In vivo	Rizatriptan Benzoate blocks neurogenic vasodilation via an action on 5-HT(1D) receptors located on perivascular trigeminal nerves to inhibit CGRP release in anaesthetized guinea-pigs. This compound evokes a transient reduction in dural blood vessel diameter which recovered to baseline values within 10 min in anaesthetized guinea-pigs. It significantly inhibits dural plasma protein extravasation produced by high intensity electrical stimulation of the trigeminal ganglion. This chemical significantly reduces electrically stimulated dural vasodilation in anaesthetised rats. It significantly reduced SP mRNA levels in the midbrains of normal and model group rats, indicating that this compound can downregulate SP gene expression in the rat midbrain. It significantly reduces midbrain PENK mRNA expression, decreasing the levels of midbrain met-enkephalin and leu-enkephalin, and thereby weakening the analgesic effects of the endogenous pain modulatory system in rat model of migraine. This chemical leads to the number of Fos-like immunoreactive neurons decreased in the spinal trigeminal nucleus caudal partand raphe magnus nucleus, increased the number of Fos-like immunoreactive neurons in the periaqueductal gray and remained unchanged in the ventromedial hypothalamic nucleus and mediodorsal thalamus nucleus in conscious rats. It markedly reduces the number of head-flicks in the rats. This compound also significantly reduces the duration of grooming behavior by nearly 2-fold when compared with that without treatment.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11487512/ [2] https://pubmed.ncbi.nlm.nih.gov/9203569/ [3] https://pubmed.ncbi.nlm.nih.gov/25767488/ [4] https://pubmed.ncbi.nlm.nih.gov/20934408/ [5] https://pubmed.ncbi.nlm.nih.gov/20971093/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00300924	Completed	Migraine	Diamond Headache Clinic\|Merck Sharp & Dohme LLC	March 2006	Phase 3

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Rizatriptan Benzoate 5-HT Receptor agonist

Chemical Structure

Molecular Weight: 391.47