| Identification | Back Directory | [Name]
5-[5-Bromo-2-(trifluoromethoxy)phenyl]-1-(cyclohexylmethyl)-2-methyl-1H-pyrrole-3-carboxylic Acid | [CAS]
2804595-86-4 | [Synonyms]
5-[5-Bromo-2-(trifluoromethoxy)phenyl]-1-(cyclohexylmethyl)-2-methyl-1H-pyrrole-3-carboxylic Acid |
| Hazard Information | Back Directory | [Uses]
TPC2-A1-P is a powerful and membrane permeable agonist of?two pore?channel?2?(TPC2) with an EC50 of 10.5 μM. TPC2-A1-P plays its role by mimicking the physiological actions?of?PI(3,5)P2. TPC2-A1-P also shows higher potency to induce Na2+ mobilisation from TPC2 than TPC-A1-N (HY-131614). TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells[1][2][3]. | [Biological Activity]
TPC2-A1-P is a selective two pore segment channel 2 (TCP2) agonist th at mimics the action of PI(3,5)P2 where it preferentially induces Na+ signals (EC50 = 0.6 μM). In contrastTPC2-A1-N is a much weaker Ca2+ current inducer when compared to NAADP and TPC2-A1-N. TPC2-A1-Pbut not the Ca2+ signals agonist TPC2-A1-Nactivates TPC2-dependent lysosomal exocytosis (30 μMmurine macrophages)while TPC2-A1-Nbut not TPC2-A1-Pcauses TPC2-dependent alkalinization of lysosomal lumen Ca2+ stores (10 μMTPC2-expressing HeLa cells). | [References]
[1] Susanne Gerndt, et al. Agonist-mediated switching of ion selectivity in TPC2 differentially promotes lysosomal function. Elife. 2020 Mar 16;9:e54712. DOI:10.7554/eLife.54712
[2] Gerndt S, et al. Discovery of lipophilic two-pore channel agonists. FEBS J. 2020;287(24):5284-5293. DOI:10.1111/febs.15432
[3] Xuhui Jin, et al. Targeting Two-Pore Channels: Current Progress and Future Challenges. Trends Pharmacol Sci. 2020 Aug;41(8):582-594. DOI:10.1016/j.tips.2020.06.002 |
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