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Cat. No.: HY-W018475

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Rizatriptan

(Synonyms: MK 462 free base)

Rizatriptan (MK 462 free base) is an orally active 5-HT_1B/5-HT_1D receptor agonist, with BBB permeability. Rizatriptan exerts significant anti-migraine effects by constricting intracranial and extracranial blood vessels and inhibiting neuropeptide release. Rizatriptan exhibits species- and tissue-specific metabolic characteristics; for example, it undergoes oxidative deamination mainly by MAO-A in the liver of brown rats, so co-administration with MAO-A inhibitors is prohibited. Rizatriptan may also exacerbate nitroglycerin-induced cutaneous allodynia, prolong the duration of central sensitization, and increase anxiety-like behavior and active drug-seeking behavior in mice. Rizatriptan has been widely used in studies related to migraine and medication-overuse headache.

For research use only. We do not sell to patients.

CAS No.: 144034-80-0
Formula: C₁₅H₁₉N₅
Molecular Weight:269.34

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

Rizatriptan Chemical Structure

CAS No.: 144034-80-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
- Clinical Trial
Chemical Information
Purity & Documentation
References
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Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

5-HT_1D Receptor

5-HT_1B Receptor

All 5-HT Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	8.4 nM Compound: Rizatriptan	Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor. Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor.	[PMID: 9357514]
CHO	IC₅₀	11 nM Compound: Rizatriptan	Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement. Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.	[PMID: 9357514]
CHO	IC₅₀	41 nM Compound: Rizatriptan	Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement. Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.	[PMID: 9357514]
Oocyte	IC₅₀	2.9 μM Compound: 18	Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes	[PMID: 18182301]
Vero C1008	IC₅₀	>2.0 × 10⁵M Compound: COVC-1751177664	Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging	10.6019/CHEMBL4651402

In Vivo

Rizatriptan (0.02 mg/kg; oral; voluntary free-choice access; during NTG stimulation phase until day 14) exacerbates Nitroglycerin (NTG)-induced cutaneous allodynia, prolongs central sensitization, increases anxiety-like behavior, and drives active medication-seeking behavior in female C57BL/6J mice, with the prelimbic cortex and spinal trigeminal nucleus caudalis acting as key hub brain regions^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6J (female, 8-10 weeks old, 20-30 g, SPF grade, NTG-induced medication overuse headache model)^[1]
Dosage:

0.02 mg/kg
Administration:

oral; voluntary free-choice access; during NTG stimulation phase until day 14
Result:

Exacerbated NTG-induced cutaneous allodynia, with hind paw mechanical pain thresholds significantly lower than control groups during modeling phase and returning to baseline only by day 40.
Showed a stable, fluctuating upward preference for rizatriptan solution, with consumption ratio to total liquid consistently above 0.5 and significantly higher on days 4, 6, 8, 10, 12, and 14.
Exhibited more rapid decrease in head and hind paw mechanical pain thresholds and slower recovery after SNP stimulation on day 40.
Had significantly lower time in open arms/total time, lower proportion of open arm entries, higher time in closed arms/total time, and higher proportion of closed arm entries.
Had significantly shorter residence time in central zone, shorter freezing time in central zone, shorter activity distance in central zone, and fewer entries into central zone.
Showed significantly increased c-Fos positive cell counts in 25 brain regions.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 144034-80-0
Molecular Weight 269.34
Formula C₁₅H₁₉N₅
SMILES

CN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3
Synonyms

MK 462 free base
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ma Z, et al. Induction of more severe central sensitization in a medication overuse headache model mice through active ingestion of rizatriptan. J Headache Pain. 2025;26(1):123. Published 2025 May 20. [Content Brief]

[2]. Ucar G. Interaction of Rizatriptan with Rat Liver Monoamine Oxidases[J]. Hacettepe University Journal of the Faculty of Pharmacy, 2004 (1): 25-36.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
- Clinical Trial
Chemical Information
Purity & Documentation
References

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Rizatriptan

All 5-HT Receptor Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Rizatriptan Related Classifications

HY-W018475 Related Classifications