Art. -Nr.: HY-N0554

Escin IA

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Escin IA is an oral LOXL2 inhibitor and EMT inhibitor, with selectivity for LOXL2-expressing cells. Escin IA suppresses invasion, migration, and metastasis of breast cancer cells, and acts as the primary anti-TNBC metastasis constituent of Aesculus chinensis Bunge fruit saponin fraction. Escin IA can be used for the research of triple-negative breast cancer, acute inflammation, and ethanol-induced gastric mucosal lesions.

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Reinheit: 99.59%
CAS. Nr.: 123748-68-5
Formel: C₅₅H₈₆O₂₄
Molecular Weight:1131.26

Speicherung:

4°C, protect from light

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

Escin IA Chemical Structure

CAS. Nr.: 123748-68-5

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

Alle Monoamine Oxidase Isoform-spezifische Produkte anzeigen :

MAO-A
MAO-B

Cellular Effect

Cell Line	Type	Value	Description	References
Vero C1008	CC₅₀	25 μM Compound: 71	Cytotoxicity against African green monkey Vero E6 cells incubated for 2 days by the MTS assay Cytotoxicity against African green monkey Vero E6 cells incubated for 2 days by the MTS assay	[PMID: 32845145]

In Vitro

Escin Ia (2.5-10 μM; 24 h) inhibits the invasion of MDA-MB-231 cells in a concentration-dependent manner, with 10 μM causing the highest inhibition (76.23%)^[1].
Escin Ia (2.5-10 μM; 24 h) modulates mRNA expression of LOXL2, E-cadherin, and MMP9 in MDA-MB-231 cells, with LOXL2 down-regulation and E-cadherin up-regulation being prominent effects^[1].
Escin Ia (2.5-10 μM; 6-24 h, unspecified intervals) suppresses the epithelial-mesenchymal transition (EMT) process in MDA-MB-231 cells by modulating EMT markers and transcription factors^[1].
Escin Ia (2.5-10 μM; 6-24 h, unspecified intervals) reverses the EMT process in TNF−α/TGF−β-stimulated MCF-7 cells by normalizing EMT marker expressions^[1].
Escin Ia (2.5-10 μM; 6-24 h, unspecified intervals) down-regulates LOXL2 expression in MDA-MB-231 cells and abrogates induced LOXL2 expression in TNF-α/TGF-β-stimulated or LOXL2-transfected MCF-7 cells^[1].
Escin Ia (2.5-10 μM; unspecified intervals) inhibits the EMT process in LOXL2-transfected MCF-7 cells by down-regulating LOXL2 and normalizing EMT markers^[1].
Escin Ia (2.5-10 μM; unspecified intervals) inhibits the EMT process in hypoxia-stimulated MCF-7 cells by down-regulating LOXL2 (without affecting HIF-1α) and normalizing EMT markers^[1].

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

Cell Invasion Assay^[1]

Cell Line:

MDA-MB-231
Concentration:

5 μM; 2.5-10 μM
Incubation Time:

24 h
Result:

Inhibited MDA-MB-231 cell invasion by 68.92% at 5 μM (stronger than other escin analogs); inhibited invasion by 39.46% at 2.5 μM, 64.22% at 5 μM, and 76.23% at 10 μM.

Real Time qPCR^[1]

Cell Line:

MDA-MB-231
Concentration:

2.5-10 μM
Incubation Time:

24 h
Result:

Down-regulated LOXL2 mRNA expression and up-regulated E-cadherin mRNA expression; moderately down-regulated MMP9 mRNA expression at 10 μM; exerted slight effects on BRMS1, Keratin19, Orai1, Stim1, TGF-β, and VEGF mRNAs.

Parmacokinetics

Species	Dose	Route	C_max	T_1/2	AUC_0-t	AUC_0-∞	CL	V_d	MRT
Rat^[3]	0.5 mg/kg	i.v.	2280 ng/mL	7.5 h	10,036 ng·h/mL	10,145 ng·h/mL	4.82 mL/min/kg	2.86 L/kg	5.46 h
Rat^[3]	1.0 mg/kg	i.v.	4362 ng/mL	9.6 h	12989 ng·h/mL	13185 ng·h/mL	6.05 mL/min/kg	5.02 L/kg	5.39 h
Rat^[3]	2.0 mg/kg	i.v.	11220 ng/mL	12.2 h	29156 ng·h/mL	29941 ng·h/mL	5.81 mL/min/kg	6.16 L/kg	6.29 h

In Vivo

Escin Ia (2-4 mg/kg; i.p.; three times per week; five weeks) suppresses TNBC metastasis and EMT in MDA-MB-231 xenograft mice by down-regulating LOXL2, with 4 mg/kg showing greater efficacy than 2 mg/kg^[1].
Escin Ia (50-200 mg/kg; p.o.) dose-dependently inhibits acetic acid-induced vascular permeability in Mus musculus, with 43.6% inhibition at 200 mg/kg^[2].
Escin Ia (25-200 mg/kg; p.o.) inhibits compound 48/80-induced scratching in mice, with significant 42.4% inhibition at 200 mg/kg^[2].
Escin Ia (200 mg/kg; p.o.) significantly inhibits the early phase (1 hour) of carrageenin-induced hind paw edema in rats^[2].
Escin Ia (25-200 mg/kg; p.o.) dose-dependently inhibits histamine-induced vascular permeability in rats (significant at 50-200 mg/kg) but does not inhibit serotonin-induced vascular permeability^[2].
Escin IA (10-50 mg/kg; p.o.; single dose 1 hour before ethanol administration) potently protects against ethanol-induced gastric mucosal lesions in rats via mechanisms involving capsaicin-sensitive afferent neurons, endogenous nitric oxide, and prostaglandins, with no gastric antisecretory activity at effective doses^[4].
Escin IA (10 mg/kg; p.o.; single dose 1 hour before ethanol administration) relies on capsaicin-sensitive afferent neurons for its gastroprotective effect in rats^[4].
Escin IA (10 mg/kg; p.o.; single dose 1 hour before ethanol administration) relies on endogenous prostaglandins for its gastroprotective effect in rats^[4].
Escin IA (10 mg/kg; p.o.; single dose 1 hour before ethanol administration) relies on endogenous nitric oxide for its gastroprotective effect in rats^[4].
Escin IA (10 mg/kg; p.o.; single dose 1 hour before ethanol administration) does not rely on endogenous sulfhydryls for its gastroprotective effect in rats^[4].
Escin IA (10-20 mg/kg; p.o.; single dose 1 hour before ethanol administration) relies on the sympathetic nervous system for its gastroprotective effect in rats^[4].

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

Animal Model:

athymic nude mice (female, 4-6 week-old)^[1]
Dosage:

2 mg/kg; 4 mg/kg
Administration:

i.p.; three times per week; five weeks
Result:

Down-regulated LOXL2, vimentin, α-SMA, Snail, Slug, Zeb1, Zeb2, and Twist, and up-regulated E-cadherin at protein and mRNA levels in breast tumors (4 mg/kg); showed little effect on HIF-1α expression in breast tumors (2 mg/kg, 4 mg/kg)

Animal Model:

ddY mice (male, 27-30 g, acetic acid-induced vascular permeability model)^[2]
Dosage:

50, 100, 200 mg/kg
Administration:

p.o.
Result:

Inhibited acetic acid-induced vascular permeability with 12.1% inhibition at 50 mg/kg, 30.6% inhibition at 100 mg/kg, and 43.6% inhibition at 200 mg/kg.

Animal Model:

ddY mice (male, 26-29 g, compound 48/80-induced scratching model)^[2]
Dosage:

25, 50, 100, 200 mg/kg
Administration:

p.o.
Result:

Inhibited compound 48/80-induced scratching with 16.8% inhibition at 25 mg/kg, 32.4% inhibition at 50 mg/kg, 31.5% inhibition at 100 mg/kg, and 42.4% inhibition at 200 mg/kg (significant at 200 mg/kg).

Animal Model:

Wistar rats (male, 140-160 g, carrageenin-induced hind paw edema model)^[2]
Dosage:

200 mg/kg
Administration:

p.o.
Result:

Significantly inhibited carrageenin-induced hind paw swelling at 1 hour but showed no effect at 3-5 hours.

Animal Model:

Wistar rats (male, 140-150 g, histamine/serotonin-induced vascular permeability model)^[2]
Dosage:

25, 50, 100, 200 mg/kg
Administration:

p.o.
Result:

Inhibited histamine-induced vascular permeability with significant effects at 50 mg/kg (28.4 μg/site dye leakage), 100 mg/kg (28.5 μg/site), and 200 mg/kg (19.4 μg/site); did not significantly inhibit serotonin-induced vascular permeability at any dose.

Animal Model:

Sprague-Dawley (male, 250 g, fasted 24-26 hours prior to experiments; ethanol-induced gastric mucosal lesions)^[4]
Dosage:

10, 20, 50 mg/kg
Administration:

p.o.; single dose 1 hour before ethanol administration
Result:

Dose-dependently reduced ethanol-induced gastric lesion scores; showed potent protective effect at 10-50 mg/kg. Did not decrease gastric secretion (volume, acid output, pepsin output) in pylorus-ligated rats at 10 and 20 mg/kg. Had gastroprotective effect attenuated by pretreatment with capsaicin, indomethacin, or L-NAME at 10 mg/kg. Had gastroprotective effect not attenuated by pretreatment with N-ethylmaleimide at 10 mg/kg. Showed marked attenuation of gastroprotective effect in streptozotocin-induced diabetic rats at 10 and 20 mg/kg.

Animal Model:

Sprague-Dawley (male, 180-200 g for capsaicin pretreatment; 250 g for other pretreatments, fasted 24-26 hours prior to experiments; capsaicin-pretreated, ethanol-induced gastric mucosal lesions)^[4]
Dosage:

10 mg/kg
Administration:

p.o.; single dose 1 hour before ethanol administration
Result:

Showed gastroprotective effect against ethanol-induced lesions markedly attenuated by capsaicin pretreatment.

Animal Model:

Sprague-Dawley (male, 250 g, fasted 24-26 hours prior to experiments; indomethacin-pretreated, ethanol-induced gastric mucosal lesions)^[4]
Dosage:

10 mg/kg
Administration:

p.o.; single dose 1 hour before ethanol administration
Result:

Showed gastroprotective effect against ethanol-induced lesions partly reduced by indomethacin pretreatment.

Animal Model:

Sprague-Dawley (male, 250 g, fasted 24-26 hours prior to experiments; L-NAME-pretreated, ethanol-induced gastric mucosal lesions)^[4]
Dosage:

10 mg/kg
Administration:

p.o.; single dose 1 hour before ethanol administration
Result:

Showed gastroprotective effect against ethanol-induced lesions partly reduced by L-NAME pretreatment.

Animal Model:

Sprague-Dawley (male, 250 g, fasted 24-26 hours prior to experiments; N-ethylmaleimide-pretreated, ethanol-induced gastric mucosal lesions)^[4]
Dosage:

10 mg/kg
Administration:

p.o.; single dose 1 hour before ethanol administration
Result:

Showed gastroprotective effect against ethanol-induced lesions not attenuated by N-ethylmaleimide pretreatment.

Animal Model:

Sprague-Dawley (male, 250 g, fasted 24-26 hours prior to experiments; streptozotocin-induced diabetic, ethanol-induced gastric mucosal lesions)^[4]
Dosage:

10, 20 mg/kg
Administration:

p.o.; single dose 1 hour before ethanol administration
Result:

Showed marked attenuation of gastroprotective effect against ethanol-induced lesions in streptozotocin-induced diabetic rats at 10 and 20 mg/kg.

Chemical Information

CAS. Nr. 123748-68-5
Appearance Solid
Molecular Weight 1131.26
Formel C₅₅H₈₆O₂₄
Color White to off-white
SMILES

OC[C@]1([C@H]2OC(C)=O)[C@](CC(C)(C)[C@H]2OC(/C(C)=C/C)=O)([H])C3=CC[C@@]4([H])[C@@](C)(CC[C@]5([H])[C@@]4(CC[C@H](O[C@@](O[C@H](C(O)=O)[C@@H](O[C@]([C@@H]([C@@H](O)[C@@H]6O)O)([H])O[C@@H]6CO)[C@@H]7O)([H])[C@@H]7O[C@]([C@@H]([C@@H](O)[C@@H]8O)O)([H])O[C@@H]8CO)[C@]5(C)CO)C)[C@]3(C)C[C@H]1O
Structure Classification
- Terpenoids
- Triterpenes
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)

Publications (1)

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Journal Impact Factor

Microbiome

Maternal intestinal L. vaginalis facilitates embryo implantation and survival through enhancing uterine receptivity in sows. [Abstract]

2025 Jun 18;13(1):145. PMID: 40533850

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (88.40 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

0.8840 mL

4.4199 mL

8.8397 mL

5 mM

0.1768 mL

0.8840 mL

1.7679 mL

10 mM

0.0884 mL

0.4420 mL

0.8840 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 (2.21 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.

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 (297 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)
- 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]. Wang Y, et al. Escin Ia suppresses the metastasis of triple-negative breast cancer by inhibiting epithelial-mesenchymal transition via down-regulating LOXL2 expression. Oncotarget. 2016;7(17):23684-23699. [Content Brief]

[2]. Matsuda H, et al. Effects of escins Ia, Ib, IIa, and IIb from horse chestnut, the seeds of Aesculus hippocastanum L., on acute inflammation in animals. Biol Pharm Bull. 1997;20(10):1092-1095. [Content Brief]

[3]. Wu XJ, et al. Pharmacokinetics of escin Ia in rats after intravenous administration. J Ethnopharmacol. 2014;156:125-129. [Content Brief]

[4]. Matsuda H, et al. Gastroprotections of escins Ia, Ib, IIa, and IIb on ethanol-induced gastric mucosal lesions in rats. Eur J Pharmacol. 1999;373(1):63-70. [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	0.8840 mL	4.4199 mL	8.8397 mL	22.0993 mL
	5 mM	0.1768 mL	0.8840 mL	1.7679 mL	4.4199 mL
	10 mM	0.0884 mL	0.4420 mL	0.8840 mL	2.2099 mL
	15 mM	0.0589 mL	0.2947 mL	0.5893 mL	1.4733 mL
	20 mM	0.0442 mL	0.2210 mL	0.4420 mL	1.1050 mL
	25 mM	0.0354 mL	0.1768 mL	0.3536 mL	0.8840 mL
	30 mM	0.0295 mL	0.1473 mL	0.2947 mL	0.7366 mL
	40 mM	0.0221 mL	0.1105 mL	0.2210 mL	0.5525 mL
	50 mM	0.0177 mL	0.0884 mL	0.1768 mL	0.4420 mL
	60 mM	0.0147 mL	0.0737 mL	0.1473 mL	0.3683 mL
	80 mM	0.0110 mL	0.0552 mL	0.1105 mL	0.2762 mL

Keywords

Escin IA

1 Cited Publications

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Escin IA

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Publications Citing Use of MedChemExpress (MCE) Escin IA

Alle Monoamine Oxidase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Escin IA Related Classifications

Art. -Nr.: HY-N0554