Zolmitriptan
Based on 1 Customer Validation
Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist that can cross the blood-brain barrier, with Kis 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.
- Purity: 99.95%
- CAS No.: 139264-17-8
- Formula: C16H21N3O2
- Molecular Weight:287.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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5-HT1B Receptor |
5-HT1D Receptor |
5-HT1F Receptor |
5-HT1B Receptor 5.01 nM (Ki) |
5-HT1D Receptor 0.63 nM (Ki) |
5-HT1F Receptor 63.09 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
15.7 nM
Compound: 2 (Zolmitriptan)
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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
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[PMID: 9871581] |
Zolmitriptan (311C90) exhibits higher affinity to 5-HT than sumatriptan (pKA=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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Anaesthetized guinea-pigs[1]
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Dosage:0, 3, 10, 30 μg/kg
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Administration:I.v.
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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.
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Animal Model:Adult male CFW mice weighing approximately 25 g[3]
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Dosage:1, 3, 5.6, 10, 30, 56 mg/kg
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Administration:Administered i.p. in a volume of 1 mL/100 g body weight
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Result:Significantly decreased the frequency of attack bites.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 139264-17-8
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Appearance Solid
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Molecular Weight 287.36
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Formula C16H21N3O2
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Color White to off-white
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SMILES
O=C1OC[C@H](CC2=CC3=C(NC=C3CCN(C)C)C=C2)N1
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Synonyms
BW-311C90; 311C90
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (275 KB)
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SDS (584 KB)
- English - EN (584 KB)
- Français - FR (584 KB)
- Deutsch - DE (584 KB)
- Norwegian - NO (584 KB)
- Español - ES (584 KB)
- Swedish - SV (584 KB)
- Italian - IT (584 KB)
- Korean - KR (584 KB)
- Portuguese - PT (584 KB)
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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]
[3]. MacLennan SJ, et al. Cranial vascular effects of zolmitriptan, a centrally active 5-HT1B/1D receptor partial agonist for the acute treatment of migraine. Eur J Pharmacol. 1998 Nov 20;361(2-3):191-7. [Content Brief]
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.
| 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 |
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