Dihydroergotamine mesylate

Name: Dihydroergotamine mesylate
Brand: MedChemExpress
SKU: HY-B0670A
Rating: 5.0 (5 reviews)

Cat. No.: HY-B0670A Purity: 99.94%: Data Sheet
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Dihydroergotamine mesylate is a BBB-permeable ergot alkaloid that can be used for the research of migraines.

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

CAS No. : 6190-39-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Dihydroergotamine mesylate:

Dihydroergotamine-d₃ Get quote
Dihydroergotamine Get quote
Dihydroergotamine mesylate (Standard) Get quote

5 Publications Citing Use of MCE Dihydroergotamine mesylate

Cell Imaging/Staining

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: 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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Biological Activity
Purity & Documentation
References
Customer Review

Description

Dihydroergotamine mesylate is a BBB-permeable ergot alkaloid that can be used for the research of migraines^[1]^[2]^[3].

In Vitro

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.

In Vivo

Dihydroergotamine mesylate (oral gavage, 44 mg/kg) combined with Sorafenib (HY-10201) (oral gavage, 30 mg/kg) inhibits tumor growth of liver cancer in HepG2 xenografted mice^[5].

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

Animal Model:	HepG2 cell xenografted mice^[5]
Dosage:	44 mg/kg plus 30 mg/kg of Sorafenib
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.
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.

Molecular Weight

679.78

Formula

C₃₄H₄₁N₅O₈S

CAS No.

6190-39-2

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.4711 mL	7.3553 mL	14.7106 mL
5 mM	0.2942 mL	1.4711 mL	2.9421 mL
10 mM	0.1471 mL	0.7355 mL	1.4711 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, 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.

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: 50% PEG400 50% Saline
Solubility: 25 mg/mL (36.78 mM); Clear solution; Need ultrasonic
Protocol 2

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.
Protocol 3

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.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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).

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)

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: 99.94%

Select Batch:

Data Sheet (277 KB) SDS (453 KB)

COA (258 KB) HNMR (293 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[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

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