Hypophyllanthin (Synonyms: NSC 619044) |
| Catalog No.GC10391 |
P-glycoprotein (P-gp) inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 33676-00-5
Sample solution is provided at 25 µL, 10mM.
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Hypophyllanthin is a P-glycoprotein (P-gp) inhibitor.
P-glycoprotein (P-gp) and multidrug resistance protein 2 (MRP2), two major drug efflux pumps, play a key role in the translocation of certain drugs and xenobiotics via restrictive barriers. The presence of P-gp and other efflux transporters on the apical membrane of enterocytes can limit absorption and therefore oral bioavailability. Inhibition of the activity of these transporters can increase plasma levels of various drugs that are their substrates, resulting in changes in drug efficacy and adverse reactions.
In vitro: Previous study found that hypophyllanthin could inhibit P-gp function with comparable potencies, but could not affect MRP2 activity. When hypophyllanthin was washed out before addition of substrate, the inhibitory action against P-gp function was lost. These results indicated the reversibility of the inhibition. Moreover, prolonged exposure of the Caco-2 cells to hypophyllanthin up to 7 days had no effect on P-gp function [1].
In vivo: A previous study was conducted to evaluate the effect of carbofuran on estrous cycle and follicular growth in virgin Wister rats as well as recovering from the damaged estrous cycle with treatment of hypophyllanthin. Hypophyllanthin is non-steroidal plant molecule with estrogen-like activities, but with an estrogen-type activity. Hypophyllanthin was capable of interacting with estrogen receptors, showing both agonist and antagonist methods of action. Therefore, hypophyllanthin was found to be systemically transformed into enterolignan, which is known to be responsible for augmenting estrus cycle in rats [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] N. Sukhaphirom, N. Vardhanabhuti, H. Chirdchupunseree, et al. Phyllanthin and hypophyllanthin inhibit function of P-gp but not MRP2 in Caco-2 cells. Journal of Pharmacy and Pharmacology 65, 292-299 (2012).
[2] Aminul Islam et al. Estrogenic Properties of Phyllanthin and Hypophyllanthin from Phyllanthus amarus against Carbofuran Induced Toxicity in Female Rats. Pharmacologyonline 3: 1006-1016 (2008).
| Cas No. | 33676-00-5 | SDF | |
| Synonyms | NSC 619044 | ||
| Chemical Name | (7S,8S,9R)-9-(3,4-dimethoxyphenyl)-6,7,8,9-tetrahydro-4-methoxy-7,8-bis(methoxymethyl)-naphtho[1,2-d]-1,3-dioxole | ||
| Canonical SMILES | COC[C@@H]1[C@@H](COC)CC(C=C(OC)C2=C3OCO2)=C3[C@H]1C4=CC(OC)=C(OC)C=C4 | ||
| Formula | C24H30O7 | M.Wt | 430.5 |
| Solubility | ≤0.2mg/ml in ethanol;10mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3229 mL | 11.6144 mL | 23.2288 mL |
| 5 mM | 0.4646 mL | 2.3229 mL | 4.6458 mL |
| 10 mM | 0.2323 mL | 1.1614 mL | 2.3229 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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