Zolmitriptan (Synonyms: BW-311C90; 311C90)

Cat. No.: HY-B0229: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist with K_is of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine.

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

Zolmitriptan Chemical Structure

CAS No. : 139264-17-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 41	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 41	In-stock	Estimated Time of Arrival: December 31
Solid
50 mg	USD 38	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
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5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

5-HT_1B Receptor

5.01 nM (Ki)

5-HT_1D Receptor

0.63 nM (Ki)

5-HT_1F Receptor

63.09 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	15.7 nM Compound: 2 (Zolmitriptan)	Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines	[PMID: 9871581]

In Vitro

Zolmitriptan (311C90) exhibits higher affinity to 5-HT than sumatriptan (pK_A=6.63±0.04 and 6.16±0.03, respectively). 311C90 displays high affinity at human recombinant 5-HT1D and 5-HT1B receptors in transfected CHO-K1 cell membranes (pIC₅₀ values=9.16±0.12 and 8.32±0.09, respectively) ^[1].

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

In Vivo

"Zolmitriptan (311C90; 3-30 μg/kg, i.v.) causes a dose-dependent inhibition of [¹²⁵I]-albumin extravasation within the ipsilateral dura mater. Zolmitriptan also produces dose-dependent falls in cranial vascular conductance (32.3% at 30 μg/kg)^[1].Zolmitriptan is an anti-migraine agent with action at 5-HT1B/D receptors. Zolmitriptan is an effective and behaviorally specific anti-aggressive agent in situations that engender moderate and alcohol-heightened levels of aggression. Zolmitriptan (1-30 mg/kg, i.p.) exerts behaviorally specific anti-aggressive effects in mice^[3]."

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

Animal Model:	Anaesthetized guinea-pigs^[1]
Dosage:	0, 3, 10, 30 μg/kg
Administration:	I.v.
Result:	In vehicle-treated animals, unilateral electrical stimulation of the trigeminal ganglion increased extravasation of [125I]-albumin into the dura on the side ipsilateral to stimulation producing a stimulated/unstimulated ratio of 1.57. Zolmitriptan decreased this ratio in a dose-dependent fashion. Zolmitriptan produced concomitant, dose-related falls in ear conductance.

Animal Model:	Adult male CFW mice weighing approximately 25 g^[3]
Dosage:	1, 3, 5.6, 10, 30, 56 mg/kg
Administration:	Administered i.p. in a volume of 1 mL/100 g body weight
Result:	Significantly decreased the frequency of attack bites.

Molecular Weight

287.36

Formula

C₁₆H₂₁N₃O₂

CAS No.

139264-17-8

Appearance

Solid

Color

White to off-white

SMILES

O=C1OC[C@H](CC2=CC3=C(NC=C3CCN(C)C)C=C2)N1

Structure Classification

Initial Source

Endogenous metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (348.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4800 mL	17.3998 mL	34.7996 mL
5 mM	0.6960 mL	3.4800 mL	6.9599 mL
10 mM	0.3480 mL	1.7400 mL	3.4800 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (8.70 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (274 KB) SDS (644 KB)

COA (247 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. G R Martin, et al. Receptor specificity and trigemino-vascular inhibitory actions of a novel 5-HT1B/1D receptor partial agonist, 311C90 (zolmitriptan). Br J Pharmacol. 1997 May;121(2):157-64. [Content Brief]

[2]. Katherine C Murray, et al. Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors. J Neurophysiol. 2011 Aug;106(2):925-43. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4800 mL	17.3998 mL	34.7996 mL	86.9989 mL
	5 mM	0.6960 mL	3.4800 mL	6.9599 mL	17.3998 mL
	10 mM	0.3480 mL	1.7400 mL	3.4800 mL	8.6999 mL
	15 mM	0.2320 mL	1.1600 mL	2.3200 mL	5.7999 mL
	20 mM	0.1740 mL	0.8700 mL	1.7400 mL	4.3499 mL
	25 mM	0.1392 mL	0.6960 mL	1.3920 mL	3.4800 mL
	30 mM	0.1160 mL	0.5800 mL	1.1600 mL	2.9000 mL
	40 mM	0.0870 mL	0.4350 mL	0.8700 mL	2.1750 mL
	50 mM	0.0696 mL	0.3480 mL	0.6960 mL	1.7400 mL
	60 mM	0.0580 mL	0.2900 mL	0.5800 mL	1.4500 mL
	80 mM	0.0435 mL	0.2175 mL	0.4350 mL	1.0875 mL
	100 mM	0.0348 mL	0.1740 mL	0.3480 mL	0.8700 mL

Zolmitriptan Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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