Hydroxy-α-sanshool

Name: Hydroxy-α-sanshool
Brand: MedChemExpress
SKU: HY-N6825
Rating: 5.0 (3 reviews)

Cat. No.: HY-N6825 Purity: 99.13%: Data Sheet
SDS

COA
Handling Instructions
FAQs
Technical Support

Hydroxy-α-sanshool is a transient receptor potential ankyrin 1 (TRPA1) and TRP vanilloid 1 (TRPV1) agonist with EC₅₀s of 69 and 1.1 μM, respectively. Hydroxy-α-sanshool can be used for pain research.

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

Hydroxy-α-sanshool Chemical Structure

CAS No. : 83883-10-7

Size	Stock	Quantity
Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid or liquid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Hydroxy-α-sanshool:

Hydroxy-α-sanshool (Standard) Get quote

3 Publications Citing Use of MCE Hydroxy-α-sanshool

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•Related Screening Libraries:

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View All TRP Channel Isoform Specific Products:

View All Isoforms

TRPC TRPM TRPV TRPA TRPML

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

EC50: 69 µM (TRPA1), 1.1 µM (TRPV1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	59 nM Compound: 2	Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis	[PMID: 24175626]
CHO	IC₅₀	7400 nM Compound: 2	Displacement of [3H]-Win55212-2 from human CB1 receptor expressed in CHO cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis Displacement of [3H]-Win55212-2 from human CB1 receptor expressed in CHO cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis	[PMID: 24175626]

In Vitro

Hydroxy-α-sanshool (0-10 mM; 20 s) induces inward currents in cultured DRG neuron^[2].
Hydroxy-α-sanshool (1 mM; 0-1 min) increases intracellular Ca²⁺ in cultured DRG neuron^[2].

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

Cell Viability Assay^[2]

Cell Line:	Dorsal root ganglion (DRG) neurons
Concentration:	0-10 mM
Incubation Time:	20 s
Result:	Induced small but robust inward currents for DRG neuron with an EC₅₀ of 66.2 μM.

Cell Viability Assay^[2]

Cell Line:	Dorsal root ganglion (DRG) neurons
Concentration:	1 mM
Incubation Time:	0-1 min
Result:	Led to an intracellular Ca²⁺ increase in the majority of DRG neurons tested (98 of 100).

In Vivo

Hydroxy-α-sanshool (intradermal injection; 4 mg per mouse; once) shows paw-licking response in wild-type and TRPV1-deficient mice^[2].
Hydroxy-α-sanshool (1 mM) is markedly aversive to WT mice, but in TRPV1 KO mice, the aversion is almost entirely eliminated (P<0.001)^[1].

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

Animal Model:	Wild-type and TRPV1-deficient mice^[2]
Dosage:	4 mg per mouse
Administration:	Intradermal injection; 4 mg per mouse; once
Result:	Reduced paw-licking response in TRPV1-deficient mice (160 times, P < 0.05). Showed paw-licking response in wild-type mice (mean 284.8 times) in 20 min.

Molecular Weight

263.38

Formula

C₁₆H₂₅NO₂

CAS No.

83883-10-7

Appearance

Viscous Liquid

SMILES

C/C=C/C=C/C=C\CC/C=C/C(NCC(C)(O)C)=O

Structure Classification

Initial Source

Endogenous metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (379.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.7968 mL	18.9840 mL	37.9680 mL
5 mM	0.7594 mL	3.7968 mL	7.5936 mL
10 mM	0.3797 mL	1.8984 mL	3.7968 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (9.49 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (9.49 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.57%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (241 KB) LCMS (91 KB)

Handling Instructions (2659 KB)

References

[1]. Koo JY, et al. Compounds from Sichuan and Melegueta peppers activate, covalently and non-covalently, TRPA1 and TRPV1 channels. Br J Pharmacol. 2009 Aug;157(8):1398-409. [Content Brief]

[2]. Koo JY, et al. Hydroxy-alpha-sanshool activates TRPV1 and TRPA1 in sensory neurons. Eur J Neurosci. 2007 Sep;26(5):1139-47. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.7968 mL	18.9840 mL	37.9680 mL	94.9199 mL
	5 mM	0.7594 mL	3.7968 mL	7.5936 mL	18.9840 mL
	10 mM	0.3797 mL	1.8984 mL	3.7968 mL	9.4920 mL
	15 mM	0.2531 mL	1.2656 mL	2.5312 mL	6.3280 mL
	20 mM	0.1898 mL	0.9492 mL	1.8984 mL	4.7460 mL
	25 mM	0.1519 mL	0.7594 mL	1.5187 mL	3.7968 mL
	30 mM	0.1266 mL	0.6328 mL	1.2656 mL	3.1640 mL
	40 mM	0.0949 mL	0.4746 mL	0.9492 mL	2.3730 mL
	50 mM	0.0759 mL	0.3797 mL	0.7594 mL	1.8984 mL
	60 mM	0.0633 mL	0.3164 mL	0.6328 mL	1.5820 mL
	80 mM	0.0475 mL	0.2373 mL	0.4746 mL	1.1865 mL
	100 mM	0.0380 mL	0.1898 mL	0.3797 mL	0.9492 mL