1094250-15-3
1094250-15-3 structure
- Name: Englerin A
- Chemical 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
- CAS Number: 1094250-15-3
- Molecular Formula: C26H34O6
- Molecular Weight: 442.54500
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
- Create Date: 2017-01-06 13:12:39
- Modify Date: 2024-01-08 08:28:20
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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[1][2][3].
| 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 |
|---|---|
| Synonyms |
6',7',10,11-tetramethoxyemetan hydrobromide
EMETINE HBR |
| 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 |
| Molecular Formula | C26H34O6 |
|---|---|
| Molecular Weight | 442.54500 |
| Exact Mass | 442.23600 |
| PSA | 82.06000 |
| LogP | 3.76540 |