1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. Englerin A

Englerin A 

Cat. No.: HY-133168
Handling Instructions

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

Englerin A Chemical Structure

CAS No. : 1094250-15-3

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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].

IC50 & Target[1]

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].

Molecular Weight

442.54

Formula

C₂₆H₃₄O₆

CAS No.

1094250-15-3

SMILES

O=C(O[[email protected]@H]1[[email protected]]2(C(C)C)C[[email protected]@H](OC(CO)=O)[[email protected]](O2)(C)[[email protected]]3([H])CC[[email protected]@H](C)[[email protected]@]13[H])/C=C/C4=CC=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

Englerin ATRP ChannelTransient receptor potential channelsTRPC4TRPC5channelsrenalcarcinomacancerInhibitorinhibitorinhibit

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Englerin A
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