2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis MAPK/ERK Pathway PI3K/Akt/mTOR Stem Cell/Wnt
  3. PDGFR UGT Reactive Oxygen Species (ROS) Apoptosis Tyrosinase p38 MAPK Akt ERK COX Interleukin Related
  4. Gomisin D

Gomisin D is an orally active lignan that binds to PDGFRβ with a Kd of 10 μM. By targeting PDGFRβ to regulate signaling pathways, Gomisin D inhibits the activation and proliferation of hepatic stellate cells and promotes their apoptosis, thereby ameliorating hepatic fibrosis. Gomisin D exhibits multiple activities such as photoprotection, antimelanogenesis, antioxidant effects, and hypoglycemic activity. Gomisin D can be used in studies related to diabetes, Alzheimer's disease, and hepatic fibrosis.

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Gomisin D

Gomisin D Chemical Structure

CAS No. : 60546-10-3

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Based on 1 publication(s) in Google Scholar

Gomisin D Related Antibodies

Top Publications Citing Use of Products

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PDGFR PDGFRβ PDGFRα

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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Akt Akt1 Akt2 Akt3

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ERK ERK1 ERK2 ERK5 ERK8

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COX COX-1 COX-2 COX-3

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Gomisin D is an orally active lignan that binds to PDGFRβ with a Kd of 10 μM. By targeting PDGFRβ to regulate signaling pathways, Gomisin D inhibits the activation and proliferation of hepatic stellate cells and promotes their apoptosis, thereby ameliorating hepatic fibrosis. Gomisin D exhibits multiple activities such as photoprotection, antimelanogenesis, antioxidant effects, and hypoglycemic activity. Gomisin D can be used in studies related to diabetes, Alzheimer's disease, and hepatic fibrosis[1][2][3].

IC50 & Target

UDP-Glucuronosyltransferases[1]
In Vitro

Gomisin D (10-80 μM; 25 h) enhances the viability and reduces the cytotoxicity of HaCaT keratinocytes irradiated with UVA and UVB, and inhibits intracellular ROS generation[1].
Gomisin D (30 μM; 25 h) significantly inhibits apoptosis of UVA- and UVB-irradiated HaCaT keratinocytes[1].
Gomisin D (10-80 μM; 49 h) dose-dependently inhibits α-MSH-induced tyrosinase activity[1].
Gomisin D (30 μM; 49 h) significantly downregulates the mRNA and protein expression of α-MSH-induced melanogenesis-related factors MITF, tyrosinase, TRP-1 and TRP-2, as well as the phosphorylation of PKA and CREB, in B16F10 melanocytes[1].
Gomisin D (20-80 μM; 48 h) inhibits the activation of T6, LX-2 and primary mouse hepatic stellate cells by targeting PDGFRβ[3].
Gomisin D (40 μM) inhibits the downstream signaling pathways (p38, AKT, ERK pathways) of PDGFRβ in HSC-T6 cells by targeting PDGFRβ[3].
Gomisin D (5-80 μM) dose-dependently inhibits PDGF-BB-induced activation, proliferation, and PDGF-BB/PDGFRβ pathway signaling in LX-2 cells[3].

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

Gomisin D Related Antibodies

Cell Viability Assay[1]

Cell Line: HaCaT keratinocytes (UVA or UVB irradiated)
Concentration: 10, 20, 30, 40 and 80 μM
Incubation Time: 1 h pre-incubation, 24 h post-irradiation incubation
Result: Improved viability of UVA- and UVB-irradiated HaCaT keratinocytes in a dose-dependent manner at 10, 20, 40, 80 μM.
Significantly increased viability and reduced LDH release in UVA- and UVB-irradiated HaCaT keratinocytes at 30 μM, compared to respective irradiated only groups.
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ MRT0-t MRT0-∞ T1/2 Tmax CL V Cmax Bioavailability
Rat[2] 5 mg/kg i.v. 3136.2 μg/L·h 3261.1 μg/L·h 6.0 h 6.9 h 5.0 h 0.083 h 1.6 L/h/kg 11.2 L/kg 539.5 μg/L /
Rat[2] 50 mg/kg i.g. 32795.6 μg/L·h 35091.7 μg/L·h 7.8 h 10.6 h 5.6 h 3.0 h 1.5 L/h/kg 13.3 L/kg 2575.2 μg/L 107.6 %
In Vivo

Gomisin D (25-50 mg/kg; i.g.; 4 weeks) alleviates CCl4-induced hepatic fibrosis in male BALB/c mice[3].
Gomisin D (50 mg/kg; p.o.; 30 days) causes no observable histotoxicity in male BALB/c mice[3].

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

Animal Model: BALB/c (male, 6-8 weeks old, 18-22 g, CCl4-induced hepatic fibrosis)[3]
Dosage: 25 mg/kg; 50 mg/kg
Administration: i.g.; once daily; 4 weeks
Result: Improved survival status and liver morphology.
Reduced hepatocyte necrosis, preserved hepatic lobule structure, and decreased collagen deposition in both dose groups, with more significant improvements in the 50 mg/kg group.
Significantly reduced serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels compared to the model group in both dose groups.
Significantly decreased mRNA and protein levels of α-smooth muscle actin (α-SMA) and collagen I in liver tissue and isolated primary hepatic stellate cells (HSCs) from both dose groups, with the 50 mg/kg group showing greater reductions.
Significantly decreased protein levels of phosphorylated AKT (p-AKT), phosphorylated ERK (p-ERK), and phosphorylated p38 (p-p38) in liver tissue from both dose groups.
Significantly decreased mRNA levels of inflammatory factors IL-1β, IL-6, TNF-α, TGF-β, and COX-2 in liver tissue from both dose groups.
Molecular Weight

530.56

Formula

C28H34O10
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

COC1=C(OC)C(OC)=CC2=C1C3=C(CC(C)C(C)(O)C2O4)C=C(OCO5)C5=C3OCC(C)C(C)(O)C4=O
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 : 100 mg/mL (188.48 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 1.8848 mL 9.4240 mL 18.8480 mL
5 mM 0.3770 mL 1.8848 mL 3.7696 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (4.71 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 (4.71 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.56%

SDS (393 KB)

COA (259 KB) HNMR (271 KB) LCMS (102 KB)

Handling Instructions (2659 KB)
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8848 mL 9.4240 mL 18.8480 mL 47.1200 mL
5 mM 0.3770 mL 1.8848 mL 3.7696 mL 9.4240 mL
10 mM 0.1885 mL 0.9424 mL 1.8848 mL 4.7120 mL
15 mM 0.1257 mL 0.6283 mL 1.2565 mL 3.1413 mL
20 mM 0.0942 mL 0.4712 mL 0.9424 mL 2.3560 mL
25 mM 0.0754 mL 0.3770 mL 0.7539 mL 1.8848 mL
30 mM 0.0628 mL 0.3141 mL 0.6283 mL 1.5707 mL
40 mM 0.0471 mL 0.2356 mL 0.4712 mL 1.1780 mL
50 mM 0.0377 mL 0.1885 mL 0.3770 mL 0.9424 mL
60 mM 0.0314 mL 0.1571 mL 0.3141 mL 0.7853 mL
80 mM 0.0236 mL 0.1178 mL 0.2356 mL 0.5890 mL
100 mM 0.0188 mL 0.0942 mL 0.1885 mL 0.4712 mL
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Gomisin D Related Classifications

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:

Gomisin D60546-10-3PDGFRUGTReactive Oxygen Species (ROS)ApoptosisTyrosinasep38 MAPKAktERKCOXInterleukin RelatedPlatelet-derived growth factor receptorUDP-glucuronosyltransferaseUridine diphosphate glucuronosyltransferasePKBProtein kinase BExtracellular signal regulated kinasesCyclooxygenaseILtyrosinaseTRP-2PDGFRβPKAMITFCREBhepatic stellate cellsTRP-1HaCaT keratinocytesB16F10 melanocytesInhibitorinhibitorinhibit

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