Cat. No.: HY-B0670

Copy Link Print Information

Dihydroergotamine

Name: Dihydroergotamine
Brand: MedChemExpress
SKU: HY-B0670
Availability: PreOrder

(Synonyms: DFN-19)

6 Cited Publications

고객리뷰

Based on 6 publication(s) in Google Scholar

Dihydroergotamine (DFN-19) is a blood-brain barrier-permeable semi-synthetic ergot alkaloid, acting as a full agonist of 5-HT1B/1D receptors (K_i values of 0.3 nM and 2.5 nM, respectively; functional IC₅₀ values of 2 nM and 2.2 nM, respectively). Dihydroergotamine inhibits Forskolin (HY-15371)-stimulated cAMP accumulation, possesses α-adrenergic receptor antagonistic activity and weak dopaminergic agonistic activity. It mediates intracranial cerebrovascular contraction, inhibits the release of neuropeptides such as CGRP/substance P, and suppresses neurogenic inflammation by activating 5-HT1B/1D receptors in the trigeminovascular system. Dihydroergotamine binds to the catalytic site of Trypanosoma cruzi trypanothione reductase and exhibits trypanocidal activity in vitro. Dihydroergotamine can be used in studies related to migraine and trypanosome infections.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 511-12-6
화학식: C₃₃H₃₇N₅O₅
분자량:583.68

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (294 KB)

Dihydroergotamine Chemical Structure

CAS No.: 511-12-6

사이즈

가격

재고

수량

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (6)
Protocol (1)
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]^[2]^[3]

α adrenergic receptor

human 5-HT_1B Receptor

0.3 nM (Ki)

human 5-HT_1D Receptor

2.5 nM (Ki)

All Adrenergic Receptor Isoforms :

All 5-HT Receptor Isoforms :

All Dopamine Receptor Isoforms :

All Parasite Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	12.6 μM Compound: dihydroergotamine	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	2.8 μM Compound: dihydroergotamine	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	49.9 μM Compound: dihydroergotamine	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]

In Vitro

Dihydroergotamine binds with high affinity to human 5-HT1B receptors in butyrate-treated HEK293 cells (K_i = 0.3 nM), human 5-HT1B receptors in mIFNβ-induced L929sA cells (K_i = 0.5 nM), and human 5-HT1D receptors in butyrate-treated C6 glioma cells (K_i = 0.7 nM)^[1].
Dihydroergotamine (20 min) fully inhibits Forskolin (HY-15371)-stimulated cAMP accumulation in L929sA and HEK 293 cells expressing human 5-HT₁B receptors, with IC₅₀ values of 0.4 nM and 2.0 nM, respectively^[1].
Dihydroergotamine (20 min) completely inhibits Forskolin-stimulated cyclic AMP accumulation in mIFNβ-induced L929sA cells expressing human 5-HT₁B receptors, with an IC₅₀ of 0.4 nM^[1].
Dihydroergotamine (20 min) completely inhibits Forskolin (IC₅₀ = 2.2 nM)- and isoproterenol-stimulated cyclic AMP accumulation in C6 glioma cells expressing the human 5-HT₁D receptor^[1].
Dihydroergotamine (0.01-1 μM; 24 h) mesylate protects Neuro-2a neuronal cells against oxygen-glucose deprivation-induced injury, with a significant increase in cell viability observed^[3].
Dihydroergotamine binds to the catalytic site of Trypanosoma cruzi trypanothione reductase, with a docking score of -9.536 kcal/mol^[4].
Dihydroergotamine (6.25-100 μg/mL; 24 h) exhibits an LC₅₀ of 28.1 μM against the trypomastigote form of Trypanosoma cruzi strain NINOA and an LC₅₀ of 57 μM against strain INC-5 in vitro, showing superior trypanocidal activity compared with reference trypanocidal drugs^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Cell Viability Assay^[3]

View Protocol

Cell Line:

Neuro-2a neuron cell line
Concentration:

0.01 μM, 0.1 μM, 1 μM
Incubation Time:

24 h
Result:

Exerted no significant effect on the viability of untreated Neuro-2a cells.
Significantly increased Neuro-2a cell viability compared to the OGD-only group at 0.1 μM and 1 μM following OGD-induced injury.

In Vivo

Dihydroergotamine (617 mg/kg; lower unspecified doses) induces 50% embryonic mortality in rats, while lower doses cause structural congenital malformations^[2].
Dihydroergotamine (10 mg/kg/day; i.p.; daily; 14 days) improves survival, neurological function, and reduces brain injury in MCAO mice by inhibiting pro-inflammatory cytokine production and promoting microglial/macrophage polarization toward the neuroprotective M2 phenotype^[3].
Dihydroergotamine (100 mg/kg; single dose) mesylate reduces blood parasite survival to 62.44% at 8 hours post-administration in a short-term murine model of acute Chagas disease, with less efficacy than benznidazole^[4].

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

Animal Model:

C57BL/6J (male, 2-month-old, 22-25 g, middle cerebral artery occlusion induced via intraluminal filament method)^[3]
Dosage:

10 mg/kg/day
Administration:

i.p.; daily; 14 days
Result:

Improved 14-day survival rates in MCAO mice.
Reduced contact time and removal time in the adhesive removal test.
Improved motor function scores in the beam walking test compared to untreated MCAO mice.
Reduced cerebral infarct volume from ~50% to ~30% of contralateral hemisphere volume 3 days after MCAO.
Reduced brain tissue loss from ~16% to ~7% of contralateral hemisphere volume 14 days after MCAO.
Decreased ischemic hemisphere levels of IL-1β from ~0.005 pg/μg to ~0.003 pg/μg.
Decreased ischemic hemisphere levels of TNF-α from ~0.015 pg/μg to ~0.008 pg/μg.
Reduced the ratio of TNF-α/NeuN and IL-1β/NeuN positive neurons.
Decreased the relative level of M1 microglial/macrophage marker CD16 from ~3 to ~1.
Increased the relative level of M2 marker CD206 from ~0.7 to ~2.3 compared to untreated MCAO mice.

Animal Model:

CD1 mice (female, 30-40 g, inoculated intraperitoneally with 1×10⁵ Trypanosoma cruzi NINOA strain trypomastigotes/mL)^[4]
Dosage:

100 mg/kg
Administration:

single dose
Result:

Reduced blood parasite survival to 62.44% at 8 hours post-treatment.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 511-12-6
분자량 583.68
화학식 C₃₃H₃₇N₅O₅
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
Synonyms

DFN-19
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (6)

All Cell Imaging/StainingWBIPBio/Physico-chemical AssayIn Vivo Efficacy Study

Sort by:

Journal Impact Factor

Science

Neuronal FAM171A2 mediates α-synuclein fibril uptake and drives Parkinson's disease. [Abstract]

2025 Feb 21;387(6736):892-900. PMID: 39977508
Nat Commun

Citrullination modulation stabilizes HIF-1α to promote tumour progression. [Abstract]

2024 Sep 3;15(1):7654. PMID: 39227578

Dihydroergotamine 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 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 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 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 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 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 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 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.
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

Cohesin mutations are synthetic lethal with stimulation of WNT signaling. [Abstract]

2020 Dec 7:9:e61405. PMID: 33284104

Protocol

All Signal Pathway Related

Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (294 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lesage AS, et al. Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. British journal of pharmacology. 1998 Apr;123(8):1655-65. [Content Brief]

[2]. Shafqat R, et al. Updated Evaluation of IV Dihydroergotamine (DHE) for Refractory Migraine: Patient Selection and Special Considerations. Journal of pain research. 2020;13:859-864.

[3]. Zheng Y, et al. Dihydroergotamine protects against ischemic stroke by modulating microglial/macrophage polarization and inhibiting inflammation in mice. Neurological research. 2024 Apr;46(4):367-377.

[4]. Gómez-Escobedo R, et al. Molecular Docking-Based Virtual Screening of FDA-Approved Drugs Using Trypanothione Reductase Identified New Trypanocidal Agents. Molecules (Basel, Switzerland). 2024 Aug 10;29(16):3796.

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Dihydroergotamine

6 Cited Publications

100 mg 견적 받기

Subscribe to the

MedChemExpress

Newsletter

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

Dihydroergotamine

Publications Citing Use of MedChemExpress (MCE) Dihydroergotamine

All Adrenergic Receptor Isoforms

All 5-HT Receptor Isoforms

All Dopamine Receptor Isoforms

All Parasite Isoforms