Almotriptan
Based on 1 Customer Validation
Almotriptan (PNU180638 free base) is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan can be used in research related to migraine.
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- Purity: 99.18%
- CAS No.: 154323-57-6
- 화학식: C17H25N3O2S
- 분자량:335.46
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
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5-HT1B Receptor |
5-HT1D Receptor |
Almotriptan acts as a full agonist to induce potent concentration-dependent contractions in canine isolated saphenous veins, with an EC50 of 394 nM, via 5-HT1B/1D receptors[2].
Almotriptan induces vasoconstriction in human isolated meningeal, superficial temporal, and basilar arteries, with EC50 values of 0.7 μM (superficial temporal) and 3.7 μM (basilar), and greater potency than Sumatriptan (HY-B0121B) in meningeal arteries[2].
Almotriptan is metabolized by multiple human liver microsomal enzymes, including MAO-A, FMO, aldehyde dehydrogenase, CYP2D6, and CYP3A4, and only weakly inhibits CYP2D6 with no significant inhibition of MAO-A or MAO-B[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Almotriptan (0-1 mg/kg; intravenous injection; single dose; maximum 0.3 mg/kg; intravenous injection; single dose; 30 μg/min; intracoronary infusion; 1 h) increases carotid vascular resistance in beagle dogs, and exhibits better carotid-femoral artery selectivity than Sumatriptan. At the tested doses, this agent has favorable cardiovascular safety, with no cardiac inhibitory effect or QTc interval change[2].
Almotriptan (10 mg/kg; subcutaneous injection; single dose) inhibits trigeminal ganglion-induced meningeal vascular extravasation in anesthetized guinea pigs, and at a subcutaneous dose of 10 mg/kg, it causes no hypothermia or bronchospasm in conscious guinea pigs[2].
Almotriptan (oral administration; single dose) does not alter cardiovascular parameters or diuretic effects in normotensive Wistar rats at the tested oral doses[2].
Almotriptan (1-3 mg/kg; subcutaneous injection; single administration) exerts no cardiovascular effects at the dose of 1 mg/kg s.c. in conscious cynomolgus monkeys, while the 3 mg/kg s.c. dose only induces mild, transient effects without electrocardiogram changes[2].
Almotriptan (up to 300 mg/kg; p.o.; single administration) shows no central nervous system-related behavioral or motor function effects in mice at oral doses up to 300 mg/kg[2].
Almotriptan slightly alleviates apomorphine (HY-12723)-induced vomiting responses in dogs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 154323-57-6
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Appearance Solid
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분자량 335.46
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화학식 C17H25N3O2S
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Color White to off-white
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SMILES
O=S(CC1=CC2=C(NC=C2CCN(C)C)C=C1)(N3CCCC3)=O
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Synonyms
PNU180638 free base
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
DMSO : 100 mg/mL (298.10 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (7.45 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 (7.45 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
순도&문서
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Data Sheet (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9810 mL | 14.9049 mL | 29.8098 mL | 74.5245 mL |
| 5 mM | 0.5962 mL | 2.9810 mL | 5.9620 mL | 14.9049 mL | |
| 10 mM | 0.2981 mL | 1.4905 mL | 2.9810 mL | 7.4525 mL | |
| 15 mM | 0.1987 mL | 0.9937 mL | 1.9873 mL | 4.9683 mL | |
| 20 mM | 0.1490 mL | 0.7452 mL | 1.4905 mL | 3.7262 mL | |
| 25 mM | 0.1192 mL | 0.5962 mL | 1.1924 mL | 2.9810 mL | |
| 30 mM | 0.0994 mL | 0.4968 mL | 0.9937 mL | 2.4842 mL | |
| 40 mM | 0.0745 mL | 0.3726 mL | 0.7452 mL | 1.8631 mL | |
| 50 mM | 0.0596 mL | 0.2981 mL | 0.5962 mL | 1.4905 mL | |
| 60 mM | 0.0497 mL | 0.2484 mL | 0.4968 mL | 1.2421 mL | |
| 80 mM | 0.0373 mL | 0.1863 mL | 0.3726 mL | 0.9316 mL | |
| 100 mM | 0.0298 mL | 0.1490 mL | 0.2981 mL | 0.7452 mL |
Almotriptan Related Classifications
HY-B0383A Related Classifications
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