Hyperforin 

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^{[1][2][3][4][5][6]}.

TRPC6^[1]

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.

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.

536.78

C₃₅H₅₂O₄

11079-53-1

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

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

• [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]