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  • DC Chemicals Limited
  • China
  • Product Name: Pyr6
  • Price: $550.0/100mg $1100.0/250mg $2200.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

245747-08-4

245747-08-4 structure
245747-08-4 structure
  • Name: Pyr6
  • Chemical Name: Pyr6
  • CAS Number: 245747-08-4
  • Molecular Formula: C17H9F7N4O
  • Molecular Weight: 418.268
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
  • Create Date: 2018-04-17 09:20:06
  • Modify Date: 2024-01-09 19:16:47
  • 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.

Name Pyr6
Synonyms 4-Pyridinecarboxamide, N-[4-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-
MFCD28385867
N-{4-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-3-fluoropyridine-4-carboxamide
N-{4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-3-fluoroisonicotinamide
Description 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.
Related Catalog
References

[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.

Density 1.5±0.1 g/cm3
Boiling Point 368.4±42.0 °C at 760 mmHg
Molecular Formula C17H9F7N4O
Molecular Weight 418.268
Flash Point 176.6±27.9 °C
Exact Mass 418.066467
LogP 3.10
Vapour Pressure 0.0±0.8 mmHg at 25°C
Index of Refraction 1.551
Storage condition 2-8℃
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
RIDADR NONH for all modes of transport