Dihydroergotamine (mesylate)
Based on 6 publication(s) in Google Scholar
Dihydroergotamine mesylate is a BBB-permeable ergot alkaloid that can be used for the research of migraines.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.94%
- CAS 番号: 6190-39-2
- 分子式: C34H41N5O8S
- 分子量:679.78
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Dihydroergotamine mesylate
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生物活性
Dihydroergotamine (10 μM, 72 h) reduces cell survival in A549 and NCI-H226 cells[4].
Dihydroergotamine (48 h) inhibits cell survival in Hep3B, PLC/PRF/5, Huh7 and HepG2 cells with IC50s of 49.91 μM, 42.0 μM, 25.42 μM and 20.23 μM respectively[5].
Dihydroergotamine (10 μM, 72 h) induces mitochondrial morphologic alterations and dysfunction, increases
ROS generation, induces apoptosis, and disturbs ATP production. in A549 cells[4].
Dihydroergotamine (40 μM, 48 h) inhibits STAT3 activation (down-regulates p-STAT3, while increasing p-ERK and has no effect on p-AKT), and enhances the protein stability of Mcl-1 (increases total p-Mcl-1 (Thr163) and Mcl-1) in HepG2 and Huh7 cells[5].
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:HepG2 cell xenografted mice[5]
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Dosage:44 mg/kg plus 30 mg/kg of Sorafenib
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Administration:oral gavage, a total of 31 days of treatment, a gavage every day for 5 days in a row, followed by 2 days of rest.
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Result:Reduced the average tumor weight and tumor volumes in the combined therapy group compared with either compound alone or control group.
Reduced Ki67 positive cells, reduced expression of Mcl-1, p-Mcl-1 and p-ERK.
化学情報
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CAS 番号 6190-39-2
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性状 Solid
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分子量 679.78
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分子式 C34H41N5O8S
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Color White to off-white
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SMILES
O[C@@]([C@@](CCC1)([H])N1C2=O)(O[C@](NC([C@@H](CN(C)[C@]3([H])C4)C[C@]3([H])C5=C6C4=CNC6=CC=C5)=O)(C)C7=O)N7[C@H]2CC8=CC=CC=C8.CS(=O)(O)=O
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別名
メシル酸ジヒドロエルゴタミン
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)
Publications (6)
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Journal Impact Factor
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Most Recent
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Science
2025 Feb 21;387(6736):892-900. PMID: 39977508 -
Nat Commun
2024 Sep 3;15(1):7654. PMID: 39227578
Dihydroergotamine mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 3;15(1):7654. [Abstract]
THLE3, Hep3B and HepG2 cells were treated with DMSO or DHE (20, 40, 60 μM) as indicated concentration for 48 h under hypoxia, followed by crystal violet staining assay.
Dihydroergotamine mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 3;15(1):7654. [Abstract]
His-PADI4 proteins were incubated with DMSO or DHE (10, 60 μM) under the indicated temperature before western blotting analysis.
Dihydroergotamine mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 3;15(1):7654. [Abstract]
Cell lysates of Hep3B-Flag-PADI4 cells were incubated with DMSO, 50 μM DHE, or 50 μM BBCA at 37 °C for 20 min before western blotting analysis. The samples were derived from the same experiment, but different gels for pan-Cit, another for Flag, Actin were processed in parallel.
Dihydroergotamine mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 3;15(1):7654. [Abstract]
Pull-down of His-PADI4 by GST-HIF-1α in the presence of DMSO or DHE as indicated concentration. g An in vitro citrullination assay of GST-HIF-1α was performed in the presence of DMSO or DHE as indicated concentration. The samples were derived from the same experiment, but different gels for R698Cit, His, another for GST were processed in parallel.
Dihydroergotamine mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 3;15(1):7654. [Abstract]
Total mRNA in Hep3B cells treated with DMSO or 20 μM, or 40 μM DHE under hypoxic conditions for 24 h were subjected to RNA-sequencing, followed by GO biological processes analysis.
Dihydroergotamine mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 3;15(1):7654. [Abstract]
Total mRNA in Hep3B cells treated with DMSO or 20 μM, or 40 μM DHE under hypoxic conditions for 24 h were subjected to RNA-sequencing, followed by GSEA analysis.
Dihydroergotamine mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 3;15(1):7654. [Abstract]
Parental Hep3B cells were injected subcutaneously into the flanks of BALB/c nude mice (n = 6 per group). After 12 days, the mice were treated with DMSO or DHE (25 mg/kg or 75 mg/kg) by i.g every 2 days. Tumour volume was determined starting on Day 14 and photographs show xenografts at the end of the experiment.
Dihydroergotamine mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 3;15(1):7654. [Abstract]
Parental Hep3B cells were injected subcutaneously into the flanks of BALB/c nude mice (n = 6 per group). After 12 days, the mice were treated with DMSO or DHE (25 mg/kg or 75 mg/kg) by i.g every 2 days. Tumour weight was measured.
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Free Radic Biol Med
Targeted delivery of nebivolol via lactoferrin-modified liposomes inhibits NEK7-mediated pyroptosis to ameliorate inflammatory bowel disease. [Abstract]2026 Aug 16:252:493-508. PMID: 42061481 -
Biofactors
GRHL2/SENP1/VDR Signaling Axis: A Key Regulator of SUMOylation and Calcitriol Resistance in SHPT. [Abstract]2026 Mar-Apr;52(2):e70086. PMID: 41760369 -
Biomed Pharmacother
Identification of nsp16 inhibitors of SARS -CoV-2, SARS -CoV-1 and MERS-CoV from FDA-approved drugs using in silico and in vitro methods. [Abstract]2025 Aug:189:118246. PMID: 40543162 -
Elife
2020 Dec 7:9:e61405. PMID: 33284104
溶剤 & 溶解度
DMSO : 50 mg/mL (73.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: 50% PEG400 50% Saline
Solubility: 25 mg/mL (36.78 mM); Clear solution; Need ultrasonic
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.68 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 (3.68 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, 1 year; -20°C, 6 months (sealed storage, away from moisture and 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.
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参考文献
[1]. Colman, I., et al., Parenteral dihydroergotamine for acute migraine headache: a systematic review of the literature. Ann Emerg Med, 2005. 45(4): p. 393-401. [Content Brief]
[2]. Saper, J.R., et al., DHE in the pharmacotherapy of migraine: potential for a larger role. Headache, 2006. 46 Suppl 4: p. S212-20. [Content Brief]
[3]. Schaerlinger, B., et al., Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy. Br J Pharmacol, 2003. 140(2): p. 277-84. [Content Brief]
[4]. Chang SH, et al. Dihydroergotamine Tartrate Induces Lung Cancer Cell Death through Apoptosis and Mitophagy. Chemotherapy. 2016;61(6):304-12. [Content Brief]
[5]. He M, et al. Dihydroergotamine mesylate enhances the anti-tumor effect of sorafenib in liver cancer cells. Biochem Pharmacol. 2023 May;211:115538. [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, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4711 mL | 7.3553 mL | 14.7106 mL | 36.7766 mL |
| 5 mM | 0.2942 mL | 1.4711 mL | 2.9421 mL | 7.3553 mL | |
| 10 mM | 0.1471 mL | 0.7355 mL | 1.4711 mL | 3.6777 mL | |
| 15 mM | 0.0981 mL | 0.4904 mL | 0.9807 mL | 2.4518 mL | |
| 20 mM | 0.0736 mL | 0.3678 mL | 0.7355 mL | 1.8388 mL | |
| 25 mM | 0.0588 mL | 0.2942 mL | 0.5884 mL | 1.4711 mL | |
| 30 mM | 0.0490 mL | 0.2452 mL | 0.4904 mL | 1.2259 mL | |
| 40 mM | 0.0368 mL | 0.1839 mL | 0.3678 mL | 0.9194 mL | |
| 50 mM | 0.0294 mL | 0.1471 mL | 0.2942 mL | 0.7355 mL | |
| 60 mM | 0.0245 mL | 0.1226 mL | 0.2452 mL | 0.6129 mL |
Dihydroergotamine mesylate 関連分類
HY-B0670A 関連分類
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