Rizatriptan Benzoate | CAS#145202-66-0 | Sertonin 5-HT1B/1D Agonist

Rizatriptan Benzoate
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 318673

CAS#: 145202-66-0

Description: Rizatriptan benzoate is a selective serotonin 5-HTID receptor agonist derived from tryptamine. Rizatriptan benzoate is a 5-HT1 agonist triptan agent for the treatment of migraine headaches.

Chemical Structure

Rizatriptan Benzoate

CAS# 145202-66-0

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 318673
Name: Rizatriptan Benzoate
CAS#: 145202-66-0
Chemical Formula: C22H25N5O2
Exact Mass: 0.00
Molecular Weight: 391.470
Elemental Analysis: C, 67.50; H, 6.44; N, 17.89; O, 8.17

Price and Availability

Size	Price	Availability	Quantity
50mg	USD 350
100mg	USD 650
250mg	USD 1150
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Rizatriptan Benzoate; MK-462; MK-0462; 2-(5-((1H-1,2,4-TRIAZOL-1-YL)METHYL)-1H-INDOL-3-YL)-N,N-DIMETHYLETHANAMINE BENZOATE; MK 462; rizatriptan benzoate; Maxalt; MK 0462; MK 462;

IUPAC/Chemical Name: 2-(5-((1H-1,2,4-triazol-1-yl)methyl)-1H-indol-3-yl)-N,N-dimethylethan-1-amine benzoate

InChi Key: JPRXYLQNJJVCMZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H19N5.C7H6O2/c1-19(2)6-5-13-8-17-15-4-3-12(7-14(13)15)9-20-11-16-10-18-20;8-7(9)6-4-2-1-3-5-6/h3-4,7-8,10-11,17H,5-6,9H2,1-2H3;1-5H,(H,8,9)

SMILES Code: CN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3.C1=CC=C(C=C1)C(=O)O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO and water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO and water

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	Rizatriptan benzoate is an activator of SR-1B. Rizatriptan benzoate selectively binds to and activates serotonin (5-HT) 1B receptors and to 5-HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brain stem sensory nuclei. It is believed to alleviate migraines by narrowing blood vessels around the brain.
In vitro activity:	To be determined
In vivo activity:	mRNA and protein levels of calcitonin gene-related peptide and cholecystokinin in the periaqueductal gray of a rat migraine model were significantly reduced upon rizatriptan treatment. Reference: Neurosci Lett. 2015 Feb 5;587:29-34. https://pubmed.ncbi.nlm.nih.gov/25524408/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	50.0	127.72
	Water	100.0	255.45

Preparing Stock Solutions

The following data is based on the product molecular weight 391.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Yao G, Han X, Hao T, Huang Q, Yu T. Effects of rizatriptan on the expression of calcitonin gene-related peptide and cholecystokinin in the periaqueductal gray of a rat migraine model. Neurosci Lett. 2015 Feb 5;587:29-34. doi: 10.1016/j.neulet.2014.12.021. Epub 2014 Dec 15. PMID: 25524408. 2. Fard JK, Hamzeiy H, Sattari M, Eftekhari A, Ahmadian E, Eghbal MA. Triazole rizatriptan Induces Liver Toxicity through Lysosomal/Mitochondrial Dysfunction. Drug Res (Stuttg). 2016 Sep;66(9):470-478. doi: 10.1055/s-0042-110178. Epub 2016 Jul 11. PMID: 27399851.
In vitro protocol:	To be determined
In vivo protocol:	1. Yao G, Han X, Hao T, Huang Q, Yu T. Effects of rizatriptan on the expression of calcitonin gene-related peptide and cholecystokinin in the periaqueductal gray of a rat migraine model. Neurosci Lett. 2015 Feb 5;587:29-34. doi: 10.1016/j.neulet.2014.12.021. Epub 2014 Dec 15. PMID: 25524408. 2. Fard JK, Hamzeiy H, Sattari M, Eftekhari A, Ahmadian E, Eghbal MA. Triazole rizatriptan Induces Liver Toxicity through Lysosomal/Mitochondrial Dysfunction. Drug Res (Stuttg). 2016 Sep;66(9):470-478. doi: 10.1055/s-0042-110178. Epub 2016 Jul 11. PMID: 27399851.

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1: Bhagawati ST, Chonkar AD, Dengale SJ, Reddy M S, Bhat K. Bioavailability enhancement of rizatriptan benzoate by oral disintegrating strip: In vitro and in vivo evaluation. Curr Drug Deliv. 2015 Aug 27. [Epub ahead of print] PubMed PMID: 26310617.

2: Yao G, Man Y, Luo X, Yu T, Ji L. Rizatriptan benzoate influences the endogenous pain modulatory system in a rat model of migraine. Neural Regen Res. 2012 Jan 15;7(2):131-5. doi: 10.3969/j.issn.1673-5374.2012.02.009. PubMed PMID: 25767488; PubMed Central PMCID: PMC4354128.

3: Sundar BS, Suneetha A. Development and Validation of HPTLC Method for the
Estimation of Rizatriptan Benzoate in Bulk and Tablets. Indian J Pharm Sci. 2010
Nov;72(6):798-801. doi: 10.4103/0250-474X.84601. PubMed PMID: 21969758; PubMed
Central PMCID: PMC3178987.

4: Keny RV, Desouza C, Lourenco CF. Formulation and evaluation of rizatriptan benzoate mouth disintegrating tablets. Indian J Pharm Sci. 2010 Jan;72(1):79-85. doi: 10.4103/0250-474X.62253. PubMed PMID: 20582194; PubMed Central PMCID: PMC2883231.

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