(+)-Kavain

Name: (+)-Kavain
Brand: MedChemExpress
SKU: HY-B1671
Rating: 4.5 (1 reviews)

Cat. No.: HY-B1671 Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions

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(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na⁺ and Ca²⁺ channels. (+)-Kavain is shown to bind at the α4β2δ GABA_A receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.

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

(+)-Kavain Chemical Structure

CAS No. : 500-64-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of (+)-Kavain:

(+)-Kavain (Standard) Get quote

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View All Sodium Channel Isoform Specific Products:

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Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na⁺ and Ca²⁺ channels^[1]. (+)-Kavain is shown to bind at the α4β2δ GABA_A receptor and potentiate GABA efficacy^[2]. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied^[4].

IC₅₀ & Target

Na⁺, Ca²⁺ channel^[1].
α4β2δ GABA_A receptor^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	32 μg/mL Compound: (+)-Kavain	Inhibition of TNF-alpha-induced NF-kappaB expressed in human A549 cells treated 1 hr after TNFalpha challenge measured after 6 hrs by luciferase reporter gene assay Inhibition of TNF-alpha-induced NF-kappaB expressed in human A549 cells treated 1 hr after TNFalpha challenge measured after 6 hrs by luciferase reporter gene assay	[PMID: 19716299]

In Vitro

(+)-Kavain (10-300 μM) enhances GABA-elicited responses in a concentration-dependent manner. The modulatory effect of Kavain is moderate, with only 170±23% of enhancement measured at 300 μM^[2]. (+)-Kavain inhibits TNF-α secretion in cells via suppression of LITAF^[4].

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

Molecular Weight

230.26

Formula

C₁₄H₁₄O₃

CAS No.

500-64-1

Appearance

Solid

Color

White to off-white

SMILES

O=C1C=C(OC)C[C@H](/C=C/C2=CC=CC=C2)O1

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (217.15 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	4.3429 mL	21.7146 mL	43.4292 mL
5 mM	0.8686 mL	4.3429 mL	8.6858 mL
10 mM	0.4343 mL	2.1715 mL	4.3429 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 (sealed storage, away from moisture and 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: ≥ 2.08 mg/mL (9.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (9.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (9.03 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 (sealed storage, away from moisture and 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: 99.98%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (247 KB) HNMR (205 KB) LCMS (119 KB)

Handling Instructions (2659 KB)

References

[1]. Bradić I, et al. [Hirschsprung's disease -- therapy and results]. Acta Chir Iugosl. 1975;22(2):183-95. [Content Brief]

[2]. Chua HC, et al. Kavain, the Major Constituent of the Anxiolytic Kava Extract, Potentiates GABAA Receptors: Functional Characteristics and Molecular Mechanism. PLoS One. 2016 Jun 22;11(6):e0157700. [Content Brief]

[3]. G. Boonen, et al. In vivo Effects of the Kavapyrones (+)-Dihydromethysticin and (±)-Kavain on Dopamine, 3,4-Dihydroxyphenylacetic Acid, Serotonin and 5-Hydroxyindoleacetic Acid Levels in Striatal and Cortical Brain Regions. Planta Medica 64 (1998) 507-510.

[4]. Tang X, et al. Kavain Inhibition of LPS-Induced TNF-α via ERK/LITAF. Toxicol Res (Camb). 2016 Jan 1;5(1):188-196. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	4.3429 mL	21.7146 mL	43.4292 mL	108.5729 mL
	5 mM	0.8686 mL	4.3429 mL	8.6858 mL	21.7146 mL
	10 mM	0.4343 mL	2.1715 mL	4.3429 mL	10.8573 mL
	15 mM	0.2895 mL	1.4476 mL	2.8953 mL	7.2382 mL
	20 mM	0.2171 mL	1.0857 mL	2.1715 mL	5.4286 mL
	25 mM	0.1737 mL	0.8686 mL	1.7372 mL	4.3429 mL
	30 mM	0.1448 mL	0.7238 mL	1.4476 mL	3.6191 mL
	40 mM	0.1086 mL	0.5429 mL	1.0857 mL	2.7143 mL
	50 mM	0.0869 mL	0.4343 mL	0.8686 mL	2.1715 mL
	60 mM	0.0724 mL	0.3619 mL	0.7238 mL	1.8095 mL
	80 mM	0.0543 mL	0.2714 mL	0.5429 mL	1.3572 mL
	100 mM	0.0434 mL	0.2171 mL	0.4343 mL	1.0857 mL

(+)-Kavain Related Classifications

Neurological Disease Metabolic Disease

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:

(+)-Kavain500-64-1GABA ReceptorSodium ChannelCalcium ChannelGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorNa channelsNa+ channelsCa2+ channelsCa channelsInhibitorinhibitorinhibit

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(+)-Kavain

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Complete Stock Solution Preparation Table

(+)-Kavain Related Classifications

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