Englerin A

Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC 50 s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+ influx and Ca 2+ cell overloadIn VitroEnglerin 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. Englerin A (0.001nM-10 μM; 48 h) inhibits cells viability in HEK293T cells overexpressing TRPC5. Englerin A (3 nM; 1-240 s) evokes sustained elevation of the intracellular Ca 2+ concentration within 1 min in HEK 293 cells over-expressing human TRPC4. Englerin A (0.1-1000 nM; 1-300 s) evokes intracellular Ca 2+ elevations in A498 cells as well with an EC 50 of 10 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoEnglerin A (5 mg/kg; i.p daily except Sunday) markedly inhibits tumor growth during the 2-week treatment period in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:hTRPC4 11.2 nM (EC 50 ) hTRPC5 7.6 nM (EC 50 ). Specifications and Purity: ≥99.0%. Molecular Formula: C26H34O6. Molecular Weight: 442.54. PubChem CID: 46242512. Isomeric SMILES: C[C@@H]1CC[C@@H]2[C@@H]1[C@@H]([C@@]3(C[C@H]([C@]2(O3)C)OC(=O)CO)C(C)C)OC(=O)/C=C/C4=CC=CC=C4.