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MedKoo Cat#: 318673 | Name: Rizatriptan Benzoate
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Description:

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

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
Rizatriptan Benzoate
CAS#145202-66-0

Theoretical Analysis

MedKoo Cat#: 318673

Name: Rizatriptan Benzoate

CAS#: 145202-66-0

Chemical Formula: C22H25N5O2

Exact Mass: 0.0000

Molecular Weight: 391.47

Elemental Analysis: C, 67.50; H, 6.44; N, 17.89; O, 8.17

Price and Availability

Size Price Availability Quantity
50mg USD 350.00
100mg USD 650.00
250mg USD 1,150.00
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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
View handling instruction
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/
Solvent mg/mL mM
Solubility
DMSO 50.0 127.72
Water 100.0 255.45
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

Recalculate based on batch purity %
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.
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.