Hypophyllanthin
Based on 1 Customer Validation
Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity.
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- Pureté : 98.48%
- CAS No.: 33676-00-5
- Formule: C24H30O7
- Masse moléculaire:430.49
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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HY-N4108R
Hypophyllanthin (Standard)P-glycoprotein -
HY-10550
TariquidarP-gp Inhibitor -
HY-15255
ZosuquidarP-gp Inhibitor -
HY-50671
Zosuquidar trihydrochlorideP-gp Inhibitor -
HY-10550A
Tariquidar methanesulfonate, hydrateP-gp Inhibitor -
HY-50879
ElacridarP-gp And BCRP Dual-Inhibitor -
HY-17013A
Dofequidar fumarateP-glycoprotein Inhibitor -
HY-10550R
Tariquidar (Standard)P-gp Inhibitor -
HY-N2453
ConvallatoxinPPARγ Activator -
HY-50879R
Elacridar (Standard)P-gp And BCRP Dual-Inhibitor -
HY-17013
DofequidarP-glycoprotein Inhibitor -
HY-13574A
BiricodarP-glycoprotein Modulator
Activité biologique
Description
IC50 & Target
P-gp[2]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A10 | IC50 |
580 μM
Compound: 2
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Displacement of [125I]endothelin-1 from ETA receptor in rat A10 cells by scintillation counting
Displacement of [125I]endothelin-1 from ETA receptor in rat A10 cells by scintillation counting
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10.1021/np50124a006 |
| A-431 | ED50 |
>20 μg/mL
Compound: 2
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Cytotoxicity against human A431 cells after 2 to 4 days by SRB assay
Cytotoxicity against human A431 cells after 2 to 4 days by SRB assay
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[PMID: 8385184] |
| Col2 | ED50 |
>20 μg/mL
Compound: 2
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Cytotoxicity against human Col2 cells after 2 to 4 days by SRB assay
Cytotoxicity against human Col2 cells after 2 to 4 days by SRB assay
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[PMID: 8385184] |
| KB-V1 | ED50 |
>20 μg/mL
Compound: 2
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Cytotoxicity against multidrug-resistant human KBV1 cells after 2 to 4 days by SRB assay in absence of vinblastine
Cytotoxicity against multidrug-resistant human KBV1 cells after 2 to 4 days by SRB assay in absence of vinblastine
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[PMID: 8385184] |
| KB-V1 | ED50 |
3.8 μg/mL
Compound: 2
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Cytotoxicity against multidrug-resistant human KBV1 cells after 2 to 4 days by SRB assay in presence of vinblastine
Cytotoxicity against multidrug-resistant human KBV1 cells after 2 to 4 days by SRB assay in presence of vinblastine
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[PMID: 8385184] |
| LNCaP | ED50 |
>20 μg/mL
Compound: 2
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Cytotoxicity against human LNCAP cells after 2 to 4 days by SRB assay
Cytotoxicity against human LNCAP cells after 2 to 4 days by SRB assay
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[PMID: 8385184] |
| P388 | ED50 |
>20 μg/mL
Compound: 2
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Cytotoxicity against mouse P388 cells after 2 to 4 days by SRB assay
Cytotoxicity against mouse P388 cells after 2 to 4 days by SRB assay
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[PMID: 8385184] |
| SK-MEL-2 | ED50 |
>20 μg/mL
Compound: 2
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Cytotoxicity against human SK-MEL-2 cells after 2 to 4 days by SRB assay
Cytotoxicity against human SK-MEL-2 cells after 2 to 4 days by SRB assay
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[PMID: 8385184] |
| ZR-75-1 | ED50 |
>20 μg/mL
Compound: 2
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Cytotoxicity against human ZR-75-1 cells after 2 to 4 days by SRB assay
Cytotoxicity against human ZR-75-1 cells after 2 to 4 days by SRB assay
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[PMID: 8385184] |
In Vitro
Hypophyllanthin down-regulates COX-2, TNF-α, and IL-1β gene expressions in U937 macrophages by interfering with the activation of NF-κB, MAPKs, and Akt[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 33676-00-5
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Appearance Solid
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Masse moléculaire 430.49
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Formule C24H30O7
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Color White to off-white
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SMILES
COC[C@@H]1[C@@H](COC)CC2=CC(OC)=C(OCO3)C3=C2[C@H]1C4=CC=C(OC)C(OC)=C4
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 33.33 mg/mL (77.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.81 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
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Cotton Pellet Granuloma
Cotton pellet granuloma is a classical in vivo chronic inflammation model used to evaluate the anti-inflammatory potential of test substances by measuring their ability to inhibit granuloma tissue formation around an implanted foreign body (cotton pellet) in rodents. The method is based on the biological response to a sterile implanted material, which induces proliferative phase inflammation characterized by fibroblast proliferation and collagen-rich granuloma formation, and the final readout reflects the extent of chronic inflammatory tissue growth surrounding the pellet. In multiple preclinical pharmacological evaluations, inhibition of cotton pellet-induced granuloma formation has been used as an indicator of anti-inflammatory activity in both synthetic and natural product screening contexts.
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Carrageenan-Induced Paw Edema
Carrageenan-induced paw edema is an acute inflammation model in which intraplantar injection of carrageenan induces localized inflammatory swelling characterized by vascular permeability, leukocyte infiltration, and production of inflammatory mediators such as prostaglandins and cytokines, making it widely used to evaluate anti-inflammatory agents in vivo. The resulting paw volume or thickness increase is quantified over time as a direct readout of inflammatory intensity and drug efficacy, typically reflecting cyclooxygenase-mediated prostaglandin-driven edema formation and immune cell recruitment in peripheral tissue[20].
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
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Fiche technique (279 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[1]. Harikrishnan H, et al. Anti-Inflammatory Effects of Hypophyllanthin and Niranthin Through Downregulation of NF-κB/MAPKs/PI3K-Akt Signaling Pathways. Inflammation. 2018 Jun;41(3):984-995. [Content Brief]
[2]. Sukhaphirom N, et al. Phyllanthin and hypophyllanthin inhibit function of P-gp but not MRP2 in Caco-2 cells. J Pharm Pharmacol. 2013 Feb;65(2):292-9. [Content Brief]
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3229 mL | 11.6147 mL | 23.2293 mL | 58.0734 mL |
| 5 mM | 0.4646 mL | 2.3229 mL | 4.6459 mL | 11.6147 mL | |
| 10 mM | 0.2323 mL | 1.1615 mL | 2.3229 mL | 5.8073 mL | |
| 15 mM | 0.1549 mL | 0.7743 mL | 1.5486 mL | 3.8716 mL | |
| 20 mM | 0.1161 mL | 0.5807 mL | 1.1615 mL | 2.9037 mL | |
| 25 mM | 0.0929 mL | 0.4646 mL | 0.9292 mL | 2.3229 mL | |
| 30 mM | 0.0774 mL | 0.3872 mL | 0.7743 mL | 1.9358 mL | |
| 40 mM | 0.0581 mL | 0.2904 mL | 0.5807 mL | 1.4518 mL | |
| 50 mM | 0.0465 mL | 0.2323 mL | 0.4646 mL | 1.1615 mL | |
| 60 mM | 0.0387 mL | 0.1936 mL | 0.3872 mL | 0.9679 mL |
Hypophyllanthin Related Classifications
HY-N4108 Related Classifications
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