Hyperforin

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Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca²⁺ levels by activating Ca²⁺-conducting non-selective canonical TRPC6 channels and triggers adipose tissue thermogenesis via the Dlat-AMPK signaling axis to suppress obesity. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Hyperforin dicyclohexylammonium salt) usually boasts enhanced water solubility and stability.

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

Hyperforin Chemical Structure

CAS No. : 11079-53-1

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Other Forms of Hyperforin:

Hyperforin dicyclohexylammonium salt Get quote

1 Publications Citing Use of MCE Hyperforin

•Transfus Med. 2023 Feb 6. [Abstract]

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•Related Small Molecules:

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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TRPC TRPM TRPV TRPA TRPML

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

TRPC6^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 40 μM Compound: 1	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 25871261]
HL-60	IC₅₀	> 40 μM Compound: 1	Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 25871261]
MCF7	IC₅₀	> 40 μM Compound: 1	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 25871261]
SMMC-7721	IC₅₀	> 40 μM Compound: 1	Cytotoxicity against human SMMC7721 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human SMMC7721 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 25871261]
SW480	IC₅₀	> 40 μM Compound: 1	Cytotoxicity against human SW480 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human SW480 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 25871261]

In Vitro

Hyperforin has a multi-directional mechanism of action. It blocks conductance of ligand-gated (GABA, NMDA, and AMPA receptors) and voltage-gated channels (Ca²⁺, K⁺, and Na⁺)^[2].
Hyperforin (0.1, 1, 10 μM; 2 h) reduces the expression and secretion of IL-17A in γδ T cell in vitro cultured murine splenic γδ T cells^[3].
Hyperforin (0.1, 1, 10 μM; 2 h) suppresses phosphorylation of MAPK and STAT3 pathways in TNF-α stimulated HaCaT cells^[3].
Hyperforin (IC₅₀=3.7 μmol/L) inhibits the microvascular tube formation and proliferation of HDMEC in a dose-dependent manner without toxic effects^[4].

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

Western Blot Analysis^[3]

Cell Line:	HaCaT cells
Concentration:	0.1, 1, 10 μM; with or without 10, 20 ng/mL TNF-α
Incubation Time:	2 hours
Result:	Reduced the expressions of p-p38, p-ERK, p-JNK, and p-STAT3, especially at the dosage of 10 μM.

In Vivo

Hyperforin (5 mg/kg; i.p.; once daily for 7 d) ameliorates Imiquimod (HY-B0180)-induced psoriatic skin lesion in mice, as well as inhibiting inflammatory cell infiltration and inflammatory cytokines release^[3].

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

Animal Model:	IMQ-induced psoriasis-like mice model^[3]
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; once daily for 7 days
Result:	Significantly ameliorated skin lesion throughout the treatment period, demonstrated by the reduced severity score of skin inflammation. Suppressed infiltration of CD3+ T cells and downregulated expression of Il1, Il6, Il23, Il17a, Il22, antimicrobial peptides (AMPs) in the skin lesion.

Molecular Weight

536.78

Formula

C₃₅H₅₂O₄

CAS No.

11079-53-1

SMILES

CC(C)C([C@@]12[C@@](C)([C@H](C[C@](C/C=C(C)/C)(C(C(C/C=C(C)/C)=C2O)=O)C1=O)C/C=C(C)/C)CC/C=C(C)/C)=O

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Heiser JH, et al. TRPC6 channel-mediated neurite outgrowth in PC12 cells and hippocampal neurons involves activation of RAS/MEK/ERK, PI3K, and CAMKIV signaling. J Neurochem. 2013 Nov;127(3):303-13. [Content Brief]

[2]. Pochwat B, et al. Hyperforin Potentiates Antidepressant-Like Activity of Lanicemine in Mice. Front Mol Neurosci. 2018 Dec 12;11:456. [Content Brief]

[3]. Zhang S, et al. Hyperforin Ameliorates Imiquimod-Induced Psoriasis-Like Murine Skin Inflammation by Modulating IL-17A-Producing γδ T Cells. Front Immunol. 2021 May 5;12:635076. [Content Brief]

[4]. Adam P, et al. Biosynthesis of hyperforin in Hypericum perforatum. J Med Chem. 2002 Oct 10;45(21):4786-93. [Content Brief]

[5]. Li XX, et al. Hyperforin: A natural lead compound with multiple pharmacological activities. Phytochemistry. 2023 Feb;206:113526. [Content Brief]

[6]. Suzhen Chen, et al. "The phytochemical hyperforin triggers thermogenesis in adipose tissue via a Dlat-AMPK signaling axis to curb obesity." Cell Metabolism 33.3 (2021): 565-580. [Content Brief]

Hyperforin Related Classifications

Neurological Disease Inflammation/Immunology

Molarity Calculator
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The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Hyperforin11079-53-1Calcium ChannelTRP ChannelCa2+ channelsCa channelsTransient receptor potential channelsInhibitorinhibitorinhibit

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