Home>>Signaling Pathways>> Membrane Transporter/Ion Channel>> TRP Channel>>Hydroxy-α-sanshool

Hydroxy-α-sanshool

Catalog No.GC36277

Hydroxy-α-sanshool is a transient receptor potential base 1 (TRPA1) and TRP vanilloid 1 (TRPV1) agonist with EC50 values of 69 and 1.1µM, respectively, commonly used in hyperlipidemia studies.

Products are for research use only. Not for human use. We do not sell to patients.

Hydroxy-α-sanshool Chemical Structure

Cas No.: 83883-10-7

Size Price Stock Qty
10mM (in 1mL DMSO)
$248.00
In stock
5mg
$225.00
In stock
10mg
$360.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com


Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Description of Hydroxy-α-sanshool

Hydroxy-α-sanshool is a transient receptor potential base 1 (TRPA1) and TRP vanilloid 1 (TRPV1) agonist with EC50 values of 69 and 1.1µM, respectively, commonly used in hyperlipidemia studies[1].

In HaCaT cells, Hydroxy-α-sanshool (10-40μM; 24h) effectively inhibited intracellular ROS production induced by C. acnes.10μM of Hydroxy-α-sanshool significantly reduced ROS levels in THP-1 cells[2]. Hydroxy-α-sanshool showed a significant protective effect on H2O2-stimulated PC12 cells without significant cytotoxicity against normal PC12 cells. Hydroxy-α-sanshool also reduced H2O2-induced apoptosis of PC12 cells by decreasing intracellular ROS and increasing mitochondrial membrane potential (MMP)[3].

Hydroxy-α-sanshool (0.5, 1.25, 2.5, 5mg/kg; po) reduces blood glucose in the T2DM mouse model by regulating glycogen metabolism through a mechanism involving the regulation of the PI3K/Akt/GSK3β/GS signaling pathway[4]. In the insulin resistance model, the Hydroxy-α-sanshool (8mg/kg) intervention lowered serum total cholesterol and LDL cholesterol and significantly reduced triacylglycerol[5].

References:
[1]. Riera C E, Menozzi‐Smarrito C, Affolter M, et al. Compounds from Sichuan and Melegueta peppers activate, covalently and non‐covalently, TRPA1 and TRPV1 channels[J]. British journal of pharmacology, 2009, 157(8): 1398-1409.
[2]. Zhou X, Su Y, Wang H, et al. Hydroxy-α-sanshool has anti-inflammatory and antioxidant effects and affects the NF-κB/STAT3 pathway via TRPV1 in acne[J]. Journal of Functional Foods, 2023, 110: 105823.
[3]. Li R L, Zhang Q, Liu J, et al. Hydroxy‐α‐sanshool Possesses Protective Potentials on H2O2‐Stimulated PC12 Cells by Suppression of Oxidative Stress‐Induced Apoptosis through Regulation of PI3K/Akt Signal Pathway[J]. Oxidative Medicine and Cellular Longevity, 2020, 2020(1): 3481758.
[4]. Zhang Q, Li R L, Wang L Y, et al. Hydroxy-α-sanshool isolated from Zanthoxylum bungeanum Maxim. has antidiabetic effects on high-fat-fed and streptozotocin-treated mice via increasing glycogen synthesis by regulation of PI3K/Akt/GSK-3β/GS signaling[J]. Frontiers in Pharmacology, 2022, 13: 1089558.
[5]. Xu F, Zhu Y, Lu M, et al. Effects of hydroxy-alpha-sanshool on intestinal metabolism in insulin-resistant mice[J]. Foods, 2022, 11(14): 2040.

Protocol of Hydroxy-α-sanshool

Cell experiment [1]:

Cell lines

PC12 cells

Preparation Method

PC12 cells were pretreated with different concentrations of Hydroxy-α-sanshool (15, 30, and 60μM) for 2 hours and then incubated with 90μM H2O2 for another 4 hours. The control group was administered with the same amount of 1640 medium and then stimulated with H2O2. Hydroxy-α-sanshool was solubilized with DMSO and subsequently diluted in culture medium with the final concentration of DMSO less than 0.1% (v/v).

Reaction Conditions

15, 30, 60μM; 2h

Applications

Hydroxy-α-sanshool showed a significant protective effect on H2O2-stimulated PC12 cells without significant cytotoxicity against normal PC12 cells. Hydroxy-α-sanshool also reduced H2O2-induced apoptosis of PC12 cells by decreasing intracellular ROS and increasing mitochondrial membrane potential (MMP).
Animal experiment [2]:

Animal models

Type 2 diabetic mouse model (T2DM)

Preparation Method

Male C57BL/6J mice were prepared as a model of T2DM. The mice were randomly divided into five groups, including HFD/STZ (HFD feeding plus STZ treatment), HFD/STZ+Metformin (Met 150mg/kg), HFD/STZ+Hydroxy-α-sanshool -L (HAS 1.25mg/kg), HFD/STZ+HAS-M (Hydroxy-α-sanshool 2.5mg/kg), and HFD/STZ+Hydroxy-α-sanshool-H (Hydroxy-α-sanshool 5mg/kg). Subsequently, Hydroxy-α-sanshool was dissolved in 0.5% CMC-Na, and mice in the NC+Hydroxy-α-sanshool (5mg/kg) and HFD/STZ+Hydroxy-α-sanshool (1.25, 2.5, 5mg/kg) groups were administered Hydroxy-α-sanshool orally at doses of 5mg/kg, 1.25mg/kg, 2.5mg/kg, or 5mg/kg for 4 weeks, respectively. The positive control treatment used in this study was Met, which was administered daily by gavage at 150mg/kg. The mice in the NC and HFD/STZ groups received vehicle solvent. During the experiment, changes in blood glucose, body weight, feed intake, and water intake were recorded.

Dosage form

0.5, 1.25, 2.5, 5mg/kg; po; 4 weeks

Applications

Hydroxy-α-sanshool reduces blood glucose in the T2DM mouse model by regulating glycogen metabolism through a mechanism involving the regulation of the PI3K/Akt/GSK3β/GS signaling pathway.

References:
[1]. Li R L, Zhang Q, Liu J, et al. Hydroxy‐α‐sanshool Possesses Protective Potentials on H2O2‐Stimulated PC12 Cells by Suppression of Oxidative Stress‐Induced Apoptosis through Regulation of PI3K/Akt Signal Pathway[J]. Oxidative Medicine and Cellular Longevity, 2020, 2020(1): 3481758.
[2].Zhang Q, Li R L, Wang L Y, et al. Hydroxy-α-sanshool isolated from Zanthoxylum bungeanum Maxim. has antidiabetic effects on high-fat-fed and streptozotocin-treated mice via increasing glycogen synthesis by regulation of PI3K/Akt/GSK-3β/GS signaling[J]. Frontiers in Pharmacology, 2022, 13: 1089558.

Chemical Properties of Hydroxy-α-sanshool

Cas No. 83883-10-7 SDF
Canonical SMILES C/C=C/C=C/C=C\CC/C=C/C(NCC(C)(O)C)=O
Formula C16H25NO2 M.Wt 263.38
Solubility DMSO : 100 mg/mL (379.68 mM; Need ultrasonic) Storage Store at -20°C,protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Hydroxy-α-sanshool

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.7968 mL 18.984 mL 37.968 mL
5 mM 0.7594 mL 3.7968 mL 7.5936 mL
10 mM 0.3797 mL 1.8984 mL 3.7968 mL
  • Molarity Calculator

  • Dilution Calculator

  • Molecular Weight Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution) of Hydroxy-α-sanshool

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

Quality Control & SDS

View current batch:

Reviews

Review for Hydroxy-α-sanshool

Average Rating: 5 ★★★★★ (Based on Reviews and 13 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for Hydroxy-α-sanshool

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.