1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel TRP Channel
  3. Hyperforin

Hyperforin  (Synonyms: 贯叶金丝桃素)

目录号: HY-116330
产品使用指南

Hyperforin 是瞬时受体典型 6 (TRPC6) 通道激活剂。Hyperforin 通过激活 Ca2+ 传导非选择性典型 TRPC6 通道来调节 Ca2+ 水平,并通过 Dlat-AMPK 信号轴触发脂肪组织产热,以抑制肥胖。Hyperforin 还表现出多种药理活性,包括抗抑郁、抗肿瘤、抗痴呆、抗糖尿病等。Hyperforin 调节 γδ T 细胞分泌 IL-17α,改善 Imiquimod (HY-B0180) 诱导的银屑病样小鼠皮肤炎症。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 Hyperforin dicyclohexylammonium salt 通常具有更好的水溶性和稳定性。

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Hyperforin Chemical Structure

Hyperforin Chemical Structure

CAS No. : 11079-53-1

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Hyperforin 的其他形式现货产品:

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target

TRPC6[1]

细胞效力
(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]
体外研究
(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].

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.
体内研究
(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].

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.
分子量

536.78

Formula

C35H52O4

CAS 号
中文名称

贯叶金丝桃素

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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.

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Hyperforin
目录号:
HY-116330
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