Englerin A

Name: Englerin A
Brand: MedChemExpress
SKU: HY-133168
Rating: 4.5 (1 reviews)

Cat. No.: HY-133168 Purity: 99.43%: Data Sheet
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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.

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

Englerin A Chemical Structure

CAS No. : 1094250-15-3

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

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Englerin A:

Englerin A (Standard) Get quote

1 Publications Citing Use of MCE Englerin A

•Pharmacol Res. 2025 Feb 7:107648. [Abstract]

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View All Isoforms

TRPC TRPM TRPV TRPA TRPML

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

hTRPC4

11.2 nM (EC₅₀)

hTRPC5

7.6 nM (EC₅₀)

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]
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]
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]

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.

Molecular Weight

442.54

Formula

C₂₆H₃₄O₆

CAS No.

1094250-15-3

Appearance

Solid

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

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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. 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: ≥ 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.
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% (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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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)

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).

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: 99.50%

Select Batch:

Data Sheet (288 KB) SDS (251 KB)

COA (268 KB) HNMR (612 KB) CNMR (407 KB) RP-HPLC (1228 KB) MS (693 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Englerin A Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Englerin A1094250-15-3TRP ChannelTransient receptor potential channelsTRPC4TRPC5channelsrenalcarcinomacancerInhibitorinhibitorinhibit

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Englerin A

Customer Review

Other Forms of Englerin A:

Englerin A Related Antibodies

1 Publications Citing Use of MCE Englerin A

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All TRP Channel Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Englerin A Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Englerin A Related Classifications

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