Pyr6 (Synonyms: N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide) |
| カタログ番号GC33443 |
Ｐｙｒ６は、ＩＣ５０が０．４９μＭのＴＲＰＣ３の選択的阻害剤である（タプシガルギン枯渇天然ＲＢＬ-２Ｈ３細胞におけるＣａ２５５５５５５流入阻害）。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 245747-08-4
Sample solution is provided at 25 µL, 10mM.
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Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).IC50 value: 0.49 uM [1]Target: TRPC3 inhibitorPyr6 is a selective SOCE inhibitor (Yonetoku et al., 2008; Sweeney et al., 2009), Pyr6 displayed 37-fold (1.58 OM) higher potency for RBL SOCE than for TRPC3 ROCE, with an IC50 comparable to that of Pyr2 and Pyr3. Pyr6 at 3 uM diminished TRPC3 currents to only 52%. Consistent with inhibition of Orai channel activity Pyr2, Pyr3 or Pyr6 substantially inhibited typical Orai downstream signalling events in RBL mast cells (NFAT activation and degranulation) activated by passive store depletion.
[1]. Schleifer H, et al. Novel pyrazole compounds for pharmacological discrimination between receptor-operated and store-operated Ca(2+) entry pathways. Br J Pharmacol. 2012 Dec;167(8):1712-22.
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