Art. -Nr.: HY-N1965

Gaultherin

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Gaultherin is an orally active non-steroidal anti-inflammatory agent. Gaultherin selectively inhibits NF-κB, MAPK, COX-2 (IC₅₀ = 0.35 mg/mL), LOX (IC₅₀ = 0.56 mg/mL) and HYAL (IC₅₀ = 28.58 μg/mL) to exert anti-inflammatory, antipyretic and analgesic effects. Gaultherin exhibits modest direct antioxidant capacity, greater in cell-based models. Gaultherin does not affect COX-1 so that avoids the common gastrointestinal side effects of Aspirin (HY-14654).

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Reinheit: 99.44%
CAS. Nr.: 490-67-5
Formel: C₁₉H₂₆O₁₂
Molecular Weight:446.40

Speicherung:

4°C, protect from light

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

Gaultherin Chemical Structure

CAS. Nr.: 490-67-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[2]

COX-2

250 μg/mL (IC₅₀)

MMP-9

IL-1β

IL-8

NF-κB

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Alle COX Isoform-spezifische Produkte anzeigen :

Alle Monoamine Oxidase Isoform-spezifische Produkte anzeigen :

MAO-A
MAO-B

Alle MMP Isoform-spezifische Produkte anzeigen :

Alle Interleukin Related Isoform-spezifische Produkte anzeigen :

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Gaultherin acts only after it is transformed into methyl salicylate by intestinal bacteria and then the absorbed methyl salicylate is hydrolyzed rapidly by esterases in intestine, blood and liver to produce salicylate^[1].
. Gaultherin presents low antioxidant activity, ferric reducing activity, and scavenging potential towards O₂^•− with SC₅₀s of 265.69 μg/mL (DPPH), 0.64 mmol Fe^²⁺/g (FRAP), 451.76 μg/mL (O₂^•−), 488.52 μg/mL (•OH), 587.86 μg/mL (H₂O₂)^[2].
Gaultherin (25-75 μM) significantly inhibits the secretion of ROS in fMLP (HY-P0224)-stimulated human neutrophils and LPS (HY-D1056)-stimulated RAW264.7 murine macrophages^[2].
Gaultherin inhibits the release of pro-inflammatory cytokines including IL-8, IL-1β, TNF-α, MMP-9 and ELA-2 in LPS/fMLP + Cytochalasin B (HY-16928)-stimulated human neutrophils and NO, TNF-α, IL-1β and IL-6 in LPS-stimulated RAW264.7 murine macrophages^[2].
Gaultherin prevents phosphorylation and subsequent degradation of IκBα and blocks the translocation of NF-κB to the nucleus^[2].
Gaultherin inhibits directly or via upstream modulation of MAPK kinases, particularly MEK1/2, MKK3/6, and MKK4/7, and thus suppresses the phosphorylation/activation of MAPKs, including JNKs, p38, and ERKs^[2].

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

In Vivo

Gaultherin (400 mg/kg, p,o., single dose) inhibits the visceral pain induced by Acetic acid (HY-Y0319) in mice^[1].
Gaultherin (400 mg/kg, p,o., once daily for 3 days) significantly inhibits the ear swelling after the application of croton oil^[1].
Gaultherin (330 mg/kg, p,o., single dose) does not aggravate the stress-induced gastric damage and is significantly superior to Aspirin^[1].
Gaultherin (100-300 mg/kg, p,o., single dose) induces a reduction in rectal temperature in feverish mice^[2].

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

Animal Model:

Acetic acid induced visceral pain model established in male Kunming mice weighing 27 g^[1]
Dosage:

400 mg/kg
Administration:

Oral administration (p.o.), single dose
Result:

Decreased the number of writhing of mice.

Animal Model:

Croton oil induced inflammatory ear edema model established male Kunming mice weighing 27 g^[1]
Dosage:

400 mg/kg
Administration:

Oral administration (p.o.), once daily for 3 days
Result:

Inhibited the dropsical ear plug weight by 39%.

Animal Model:

Water immersion restraint stress model and gastric mucosal damage assay established in male Wistar rats weighing 250 g^[1]
Dosage:

330 mg/kg
Administration:

Oral administration (p.o.), single dose
Result:

Exhibited less lesion score less than that observed in the presence of Aspirin.
No lesion was observed in the stomach.

Animal Model:

Brewer’s yeast-induced pyrexia model established in healthy albino mice^[2]
Dosage:

100, 200 and 300 mg/kg
Administration:

Oral administration (p.o.), single dose
Result:

Significantly reduced the pyrexia significantly in the 5th hour of experiment.

Chemical Information

CAS. Nr. 490-67-5
Appearance Solid
Molecular Weight 446.40
Formel C₁₉H₂₆O₁₂
Color White to off-white
SMILES

COC(C1=C(C=CC=C1)O[C@@H]2O[C@@H]([C@H]([C@@H]([C@H]2O)O)O)CO[C@H]3[C@@H]([C@H]([C@@H](CO3)O)O)O)=O
Structure Classification
- Ketones, Aldehydes, Acids
Initial Source
- Plants
- other families
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (224.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2401 mL

11.2007 mL

22.4014 mL

5 mM

0.4480 mL

2.2401 mL

4.4803 mL

10 mM

0.2240 mL

1.1201 mL

2.2401 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhang B, et, al. Gaultherin, a natural salicylate derivative from Gaultheria yunnanensis: towards a better non-steroidal anti-inflammatory drug. Eur J Pharmacol. 2006 Jan 13;530(1-2):166-71. [Content Brief]

[2]. Michel P. Gaultherin, a Natural Alternative to Aspirin: A Comprehensive Review of Molecular Mechanisms, Pharmacokinetics, Biocompatibility, Isolation Techniques, and Plant Sources. Int J Mol Sci. 2025 Jul 28;26(15):7280. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2401 mL	11.2007 mL	22.4014 mL	56.0036 mL
	5 mM	0.4480 mL	2.2401 mL	4.4803 mL	11.2007 mL
	10 mM	0.2240 mL	1.1201 mL	2.2401 mL	5.6004 mL
	15 mM	0.1493 mL	0.7467 mL	1.4934 mL	3.7336 mL
	20 mM	0.1120 mL	0.5600 mL	1.1201 mL	2.8002 mL
	25 mM	0.0896 mL	0.4480 mL	0.8961 mL	2.2401 mL
	30 mM	0.0747 mL	0.3734 mL	0.7467 mL	1.8668 mL
	40 mM	0.0560 mL	0.2800 mL	0.5600 mL	1.4001 mL
	50 mM	0.0448 mL	0.2240 mL	0.4480 mL	1.1201 mL
	60 mM	0.0373 mL	0.1867 mL	0.3734 mL	0.9334 mL
	80 mM	0.0280 mL	0.1400 mL	0.2800 mL	0.7000 mL
	100 mM	0.0224 mL	0.1120 mL	0.2240 mL	0.5600 mL

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Gaultherin

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Alle NF-κB Isoform-spezifische Produkte anzeigen

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Alle COX Isoform-spezifische Produkte anzeigen

Alle Monoamine Oxidase Isoform-spezifische Produkte anzeigen

Alle MMP Isoform-spezifische Produkte anzeigen

Alle Interleukin Related Isoform-spezifische Produkte anzeigen

Alle TNF Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise