Art. -Nr.: HY-133168

Englerin A

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Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC₅₀s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca²⁺ influx and Ca²⁺ cell overload.

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Reinheit: 99.43%
CAS. Nr.: 1094250-15-3
Formel: C₂₆H₃₄O₆
Molecular Weight:442.54

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Englerin A Chemical Structure

CAS. Nr.: 1094250-15-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

hTRPC4

11.2 nM (EC₅₀)

hTRPC5

7.6 nM (EC₅₀)

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	GI₅₀	1.1 μM Compound: 1	Growth inhibition of human 786-0 cells after 48 hrs by SRB assay Growth inhibition of human 786-0 cells after 48 hrs by SRB assay	[PMID: 22280462]
A498	GI₅₀	0.011 μM Compound: 1	Growth inhibition of human A498 cells after 48 hrs Growth inhibition of human A498 cells after 48 hrs	[PMID: 22280462]
A498	GI₅₀	10 nM Compound: 1	Growth inhibition of human A498 cells incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human A498 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 27107948]
A498	GI₅₀	11 nM Compound: 1	Growth inhibition of human A498 cells incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human A498 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 32944138]
A498	GI₅₀	11 nM Compound: 1a	Growth inhibition of human A498 cells assessed as cell growth inhibition Growth inhibition of human A498 cells assessed as cell growth inhibition	[PMID: 36105325]
A498	IC₅₀	45 nM Compound: 1	Cytotoxicity against human A498 cells assessed as reduction in cell viability Cytotoxicity against human A498 cells assessed as reduction in cell viability	[PMID: 28170253]
ACHN	GI₅₀	0.017 μM Compound: 1	Growth inhibition of human ACHN cells after 48 hrs by SRB assay Growth inhibition of human ACHN cells after 48 hrs by SRB assay	[PMID: 22280462]
CAKI-1	GI₅₀	16 μM Compound: 1	Growth inhibition of human CAKI-1 cells after 48 hrs by SRB assay Growth inhibition of human CAKI-1 cells after 48 hrs by SRB assay	[PMID: 22280462]
Hs-578T	GI₅₀	10 nM Compound: 1	Growth inhibition of human Hs 578T cells incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human Hs 578T cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 27107948]
RXF 393	GI₅₀	0.011 μM Compound: 1	Growth inhibition of human RXF393 cells after 48 hrs by SRB assay Growth inhibition of human RXF393 cells after 48 hrs by SRB assay	[PMID: 22280462]
RXF 393	GI₅₀	59 nM Compound: 1	Growth inhibition of human RXF393 cells incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human RXF393 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 32944138]
RXF 393	GI₅₀	59 nM Compound: 1a	Growth inhibition of human RXF 393 cells assessed as inhibition of cell growth Growth inhibition of human RXF 393 cells assessed as inhibition of cell growth	[PMID: 36105325]
SN12C	GI₅₀	1.1 μM Compound: 1	Growth inhibition of human SN12C cells after 48 hrs by SRB assay Growth inhibition of human SN12C cells after 48 hrs by SRB assay	[PMID: 22280462]
TK-10	GI₅₀	1.9 μM Compound: 1	Growth inhibition of human TK10 cells after 48 hrs by SRB assay Growth inhibition of human TK10 cells after 48 hrs by SRB assay	[PMID: 22280462]
UO-31	GI₅₀	0.015 μM Compound: 1	Growth inhibition of human UO31 cells after 48 hrs Growth inhibition of human UO31 cells after 48 hrs	[PMID: 22280462]
UO-31	GI₅₀	15 nM Compound: 1	Growth inhibition of human UO31 cells incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human UO31 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 32944138]
UO-31	GI₅₀	15 nM Compound: 1a	Growth inhibition of human UO-31 cells assessed as cell growth inhibition Growth inhibition of human UO-31 cells assessed as cell growth inhibition	[PMID: 36105325]

In Vitro

Englerin A (0.15-2500 nM; 48 h) characteristic concentration-dependent suppresses cells growth of the A-498 cells treated with the control siRNA while has little effect on the growth of cells treated with TRPC4 siRNAs^[3].
Englerin A (0.001nM-10 μM; 48 h) inhibits cells viability in HEK293T cells overexpressing TRPC5^[3].
Englerin A (3 nM; 1-240 s) evokes sustained elevation of the intracellular Ca²⁺ concentration within 1 min in HEK 293 cells over-expressing human TRPC4^[1].
Englerin A (0.1-1000 nM; 1-300 s) evokes intracellular Ca²⁺ elevations in A498 cells as well with an EC₅₀ of 10 nM^[1].

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

In Vivo

Englerin A (5 mg/kg; i.p daily except Sunday) markedly inhibits tumor growth during the 2-week treatment period in mice^[4].

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

Chemical Information

CAS. Nr. 1094250-15-3
Appearance Solid
Molecular Weight 442.54
Formel C₂₆H₃₄O₆
Color White to light yellow
SMILES

O=C(O[C@@H]1[C@]2(C(C)C)C[C@@H](OC(CO)=O)[C@](O2)(C)[C@]3([H])CC[C@@H](C)[C@@]13[H])/C=C/C4=CC=CC=C4
Structure Classification
- Terpenoids
- Sesquiterpenes
Initial Source
- Plants
- other families
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

Pharmacol Res

The essential role of sphingolipids in TRPC5 ion channel localization and functionality within lipid rafts. [Abstract]

2025 Feb 7:107648. PMID: 39923924

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (112.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Methanol : 30 mg/mL (67.79 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

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

2.2597 mL

11.2984 mL

22.5968 mL

5 mM

0.4519 mL

2.2597 mL

4.5194 mL

10 mM

0.2260 mL

1.1298 mL

2.2597 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. 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

Konzentration

Volumen

Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)}

Konzentration _{(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: ≥ 1.25 mg/mL (2.82 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.25 mg/mL (2.82 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.25 mg/mL (2.82 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 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)
g
Dosing Volume (Per Animal)
μL
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 (288 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 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]. Akbulut Y, et, al. (-)-Englerin A is a potent and selective activator of TRPC4 and TRPC5 calcium channels. Angew Chem Int Ed Engl. 2015 Mar 16;54(12):3787-91. [Content Brief]

[2]. Rubaiy HN, et, al. Identification of an (-)-englerin A analogue, which antagonizes (-)-englerin A at TRPC1/4/5 channels. Br J Pharmacol. 2018 Mar; 175(5):830-839. [Content Brief]

[3]. Carson C, et, al. Englerin A Agonizes the TRPC4/C5 Cation Channels to Inhibit Tumor Cell Line Proliferation. PLoS One. 2015 Jun 22;10(6):e0127498. [Content Brief]

[4]. Sourbier C, et, al. Englerin A stimulates PKCθ to inhibit insulin signaling and to simultaneously activate HSF1: pharmacologically induced synthetic lethality. Cancer Cell. 2013 Feb 11;23(2):228-37. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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
Methanol / DMSO	1 mM	2.2597 mL	11.2984 mL	22.5968 mL	56.4921 mL
	5 mM	0.4519 mL	2.2597 mL	4.5194 mL	11.2984 mL
	10 mM	0.2260 mL	1.1298 mL	2.2597 mL	5.6492 mL
	15 mM	0.1506 mL	0.7532 mL	1.5065 mL	3.7661 mL
	20 mM	0.1130 mL	0.5649 mL	1.1298 mL	2.8246 mL
	25 mM	0.0904 mL	0.4519 mL	0.9039 mL	2.2597 mL
	30 mM	0.0753 mL	0.3766 mL	0.7532 mL	1.8831 mL
	40 mM	0.0565 mL	0.2825 mL	0.5649 mL	1.4123 mL
	50 mM	0.0452 mL	0.2260 mL	0.4519 mL	1.1298 mL
	60 mM	0.0377 mL	0.1883 mL	0.3766 mL	0.9415 mL
DMSO	80 mM	0.0282 mL	0.1412 mL	0.2825 mL	0.7062 mL
DMSO	100 mM	0.0226 mL	0.1130 mL	0.2260 mL	0.5649 mL

Keywords

Englerin A

1 Cited Publications

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Englerin A

MCE Bioactive Compound Library

Natural Product Library Plus

Publications Citing Use of MedChemExpress (MCE) Englerin A

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Englerin A

MCE Bioactive Compound Library

Natural Product Library Plus

Publications Citing Use of MedChemExpress (MCE) Englerin A

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Englerin A Related Classifications

Art. -Nr.: HY-133168