Englerin A
Based on 1 publication(s) in Google Scholar
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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- Pureté: 99.43%
- CAS No.: 1094250-15-3
- Formule: C26H34O6
- Masse moléculaire:442.54
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Englerin A
More
Activité biologique
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hTRPC4 11.2 nM (EC50) |
hTRPC5 7.6 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | GI50 |
1.1 μM
Compound: 1
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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
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[PMID: 22280462] |
| A498 | GI50 |
0.011 μM
Compound: 1
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Growth inhibition of human A498 cells after 48 hrs
Growth inhibition of human A498 cells after 48 hrs
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[PMID: 22280462] |
| A498 | GI50 |
10 nM
Compound: 1
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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
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[PMID: 27107948] |
| A498 | GI50 |
11 nM
Compound: 1
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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
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[PMID: 32944138] |
| A498 | GI50 |
11 nM
Compound: 1a
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Growth inhibition of human A498 cells assessed as cell growth inhibition
Growth inhibition of human A498 cells assessed as cell growth inhibition
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[PMID: 36105325] |
| A498 | IC50 |
45 nM
Compound: 1
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Cytotoxicity against human A498 cells assessed as reduction in cell viability
Cytotoxicity against human A498 cells assessed as reduction in cell viability
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[PMID: 28170253] |
| ACHN | GI50 |
0.017 μM
Compound: 1
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Growth inhibition of human ACHN cells after 48 hrs by SRB assay
Growth inhibition of human ACHN cells after 48 hrs by SRB assay
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[PMID: 22280462] |
| CAKI-1 | GI50 |
16 μM
Compound: 1
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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
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[PMID: 22280462] |
| Hs-578T | GI50 |
10 nM
Compound: 1
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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
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[PMID: 27107948] |
| RXF 393 | GI50 |
0.011 μM
Compound: 1
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Growth inhibition of human RXF393 cells after 48 hrs by SRB assay
Growth inhibition of human RXF393 cells after 48 hrs by SRB assay
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[PMID: 22280462] |
| RXF 393 | GI50 |
59 nM
Compound: 1
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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
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[PMID: 32944138] |
| RXF 393 | GI50 |
59 nM
Compound: 1a
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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
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[PMID: 36105325] |
| SN12C | GI50 |
1.1 μM
Compound: 1
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Growth inhibition of human SN12C cells after 48 hrs by SRB assay
Growth inhibition of human SN12C cells after 48 hrs by SRB assay
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[PMID: 22280462] |
| TK-10 | GI50 |
1.9 μM
Compound: 1
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Growth inhibition of human TK10 cells after 48 hrs by SRB assay
Growth inhibition of human TK10 cells after 48 hrs by SRB assay
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[PMID: 22280462] |
| UO-31 | GI50 |
0.015 μM
Compound: 1
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Growth inhibition of human UO31 cells after 48 hrs
Growth inhibition of human UO31 cells after 48 hrs
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[PMID: 22280462] |
| UO-31 | GI50 |
15 nM
Compound: 1
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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
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[PMID: 32944138] |
| UO-31 | GI50 |
15 nM
Compound: 1a
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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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1094250-15-3
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Appearance Solid
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Masse moléculaire 442.54
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Formule C26H34O6
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Color White to light yellow
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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
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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
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Most Recent
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Pharmacol Res
The essential role of sphingolipids in TRPC5 ion channel localization and functionality within lipid rafts. [Abstract]2025 Feb 7:107648. PMID: 39923924
Solvant et solubilité
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (288 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[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
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.
| 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 |
| 100 mM | 0.0226 mL | 0.1130 mL | 0.2260 mL | 0.5649 mL |
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