Englerin A

Modify Date: 2024-01-08 08:28:20

Englerin A Structure
Englerin A structure
Common Name Englerin A
CAS Number 1094250-15-3 Molecular Weight 442.54500
Density N/A Boiling Point N/A
Molecular Formula C26H34O6 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Englerin A


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[1][2][3].

 Names

Name (1S,2R,5R,6R,7S,8R,10R)-10-(Glycoloyloxy)-8-isopropyl-1,5-dimethyl-11-oxatricyclo[6.2.1.02,6]undec-7-yl (2E)-3-phenylacrylate
Synonym More Synonyms

 Englerin A Biological Activity

Description 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[1][2][3].
Related Catalog
Target

hTRPC4:11.2 nM (EC50)

hTRPC5:7.6 nM (EC50)

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].
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].
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.

[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.

[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.

[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.

 Chemical & Physical Properties

Molecular Formula C26H34O6
Molecular Weight 442.54500
Exact Mass 442.23600
PSA 82.06000
LogP 3.76540

 Synthetic Route

 Synonyms

6',7',10,11-tetramethoxyemetan hydrobromide
EMETINE HBR
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