Phytolaccagenin

Name: Phytolaccagenin
Brand: MedChemExpress
SKU: HY-N1433
Rating: 4.5 (0 reviews)

Cat. No.: HY-N1433 Purity: 99.86%: Data Sheet
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Phytolaccagenin is a triterpenoid saponin aglycone, Antifungal agent, vasodilator, antihypertensive agent, and anti-inflammatory agent. Phytolaccagenin activates vascular and cardiac Muscarinic receptors, blocks cardiac β-adrenergic receptors, and inhibits voltage-dependent calcium channels in blood vessels. Phytolaccagenin inhibits the growth of Candida albicans and Cryptococcus neoformans. Phytolaccagenin induces vasodilation, produces negative inotropic and negative chronotropic effects, reduces mean arterial pressure, and inhibits LPS-induced inflammation. Phytolaccagenin exhibits enhanced antihypertensive effects in high salt-induced hypertensive rats. Phytolaccagenin can be used in the research of candidiasis, cryptococcosis, hypertension, and inflammation-related diseases.

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

Phytolaccagenin Chemical Structure

CAS No. : 1802-12-6

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
20 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Other Forms of Phytolaccagenin:

Phytolaccagenin (Standard) Get quote

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

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α adrenergic receptor β adrenergic receptor

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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

IC₅₀ & Target^[2]

β-adrenoceptor

In Vitro

Phytolaccagenin inhibits phenylephrine (HY-B0769)- and high K⁺-induced contraction of isolated aortic rings from Sprague-Dawley rats^[2].
Phytolaccagenin (10-100 μM; 30-45 min) inhibits voltage-dependent Ca²⁺ influx in aortic rings isolated from Sprague-Dawley rats, which is confirmed by the rightward shift of the CaCl₂ concentration-response curve^[2].
Phytolaccagenin produces negative inotropic and negative chronotropic effects on isolated spontaneously beating atrial strips from Sprague-Dawley rats, and these effects are partially mediated by cardiac muscarinic receptors and β-adrenergic receptors^[2].
Phytolaccagenin (5-100 μM; 24 h) potently inhibits lipopolysaccharide (LPS)-induced nitric oxide production in RAW 264.7 macrophages, with an IC₅₀ of 18.4 μM, and exhibits stronger activity than Esculentoside A (HY-N0632)^[3].
Phytolaccagenin (60 min) shows no hemolytic activity against red blood cells of New Zealand rabbits, with an HD₅₀ > 500 μM at the maximum concentration of 500 μM^[3].
Phytolaccagenin (100 μM) reduces the viability of RAW 264.7 macrophages^[3].

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

Cell Viability Assay^[3]

Cell Line:	RAW 264.7 murine celiac macrophages
Concentration:	100 μM
Incubation Time:	A certain period of time
Result:	Reduced RAW 264.7 macrophage growth by 39%.

Parmacokinetics

Species	Dose	Route	C₀	T_1/2	AUC_0-last	AUC_0-∞	MRT	V_z	CL
Rat^[4]	10 mg/kg	i.v.	8277 ng/mL	1.4 h	5821 ng·h/mL	5999 ng·h/mL	0.9 h	4.2 L/kg	2.1 L/h/kg

In Vivo

Phytolaccagenin (0.3-300 µg/kg; i.v.; single dose) produces a dose-dependent antihypertensive effect in high-salt-induced hypertensive SD rats, with a maximum 77.4% fall in MAP at 300 µg/kg i.v., via mechanisms involving muscarinic receptors and nitric oxide pathways^[2].
Phytolaccagenin (0.3-300 µg/kg; i.v.; single dose) produces a dose-dependent hypotensive effect in normotensive anesthetized SD rats, with a maximum 61% fall in MAP at 300 µg/kg i.v^[2].

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

Animal Model:	Sprague-Dawley (SD) (male, 180-250 g, high-salt diet-induced hypertension model)^[2]
Dosage:	0.3 µg/kg; 3 µg/kg; 30 µg/kg; 300 µg/kg
Administration:	i.v.; single dose
Result:	Caused a dose-dependent fall in MAP: 28.4% at 0.3 µg/kg, 50.8% at 3 µg/kg, 68.8% at 30 µg/kg, and 77.4% at 300 µg/kg. Caused a dose-dependent fall in MAP in atropine-pretreated rats: 7% at 0.3 µg/kg, 27.33% at 3 µg/kg, 63.66% at 30 µg/kg, and 70% at 300 µg/kg. Caused a dose-dependent fall in MAP in L-NAME-pretreated rats: 34% at 0.3 µg/kg, 51.66% at 3 µg/kg, 57.33% at 30 µg/kg, and 72.33% at 300 µg/kg. Caused a dose-dependent fall in heart rate: 14.06% at 0.3 µg/kg, 22.53% at 3 µg/kg, 40.67% at 30 µg/kg, and 49.1% at 300 µg/kg.

Animal Model:	Sprague-Dawley (SD) (male, 180-250 g)^[2]
Dosage:	0.3 µg/kg; 3 µg/kg; 30 µg/kg; 300 µg/kg
Administration:	i.v.; single dose
Result:	Caused a dose-dependent fall in MAP: 11% at 0.3 µg/kg, 31.8% at 3 µg/kg, 38.4% at 30 µg/kg, and 61% at 300 µg/kg. Caused a dose-dependent fall in heart rate: 13.3% at 0.3 µg/kg, 23% at 3 µg/kg, 34.5% at 30 µg/kg, and 53.7% at 300 µg/kg.

Molecular Weight

532.71

Formula

C₃₁H₄₈O₇

CAS No.

1802-12-6

Appearance

Solid

Color

White to off-white

SMILES

C[C@@]1(CO)[C@@H](O)[C@@H](O)C[C@]2(C)[C@@]3([H])CC=C4[C@]5([H])C[C@@](C)(C(OC)=O)CC[C@@](C(O)=O)5CC[C@](C)4[C@@](C)3CC[C@@]12[H]

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 (93.86 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	1.8772 mL	9.3860 mL	18.7719 mL
5 mM	0.3754 mL	1.8772 mL	3.7544 mL
10 mM	0.1877 mL	0.9386 mL	1.8772 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: 2.5 mg/mL (4.69 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.69 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

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: 99.86%

Select Batch:

Data Sheet (284 KB) SDS (392 KB)

COA (256 KB)

Handling Instructions (2659 KB)

References

[1]. Di Liberto M, et al. Antifungal activity of saponin-rich extracts of Phytolacca dioica and of the sapogenins obtained through hydrolysis. Natural product communications. 2010 Jul;5(7):1013-8.

[2]. Ul Haq I, et al. Antihypertensive effect and the underlying mechanisms of action of phytolaccagenin in rat models. Clinical and experimental hypertension (New York, N.Y. : 1993). 2022 Aug 18;44(6):557-566.

[3]. Gong W, et al. Synthesis of novel derivatives of esculentoside A and its aglycone phytolaccagenin, and evaluation of their haemolytic activity and inhibition of lipopolysaccharide-induced nitric oxide production. Chemistry & biodiversity. 2011 Oct;8(10):1833-52.

[4]. Wei F, et al. Development and validation of a HPLC-MS/MS method for the determination of phytolaccagenin in rat plasma and application to a pharmacokinetic study. Journal of pharmaceutical and biomedical analysis. 2015 Mar 25;107:82-8. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8772 mL	9.3860 mL	18.7719 mL	46.9298 mL
	5 mM	0.3754 mL	1.8772 mL	3.7544 mL	9.3860 mL
	10 mM	0.1877 mL	0.9386 mL	1.8772 mL	4.6930 mL
	15 mM	0.1251 mL	0.6257 mL	1.2515 mL	3.1287 mL
	20 mM	0.0939 mL	0.4693 mL	0.9386 mL	2.3465 mL
	25 mM	0.0751 mL	0.3754 mL	0.7509 mL	1.8772 mL
	30 mM	0.0626 mL	0.3129 mL	0.6257 mL	1.5643 mL
	40 mM	0.0469 mL	0.2346 mL	0.4693 mL	1.1732 mL
	50 mM	0.0375 mL	0.1877 mL	0.3754 mL	0.9386 mL
	60 mM	0.0313 mL	0.1564 mL	0.3129 mL	0.7822 mL
	80 mM	0.0235 mL	0.1173 mL	0.2346 mL	0.5866 mL