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Pyr6

Names

[ CAS No. ]:
245747-08-4

[ Name ]:
Pyr6

[Synonym ]:
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

Biological Activity

[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]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel
Research Areas >> Others

[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.


[Related Small Molecules]

capsaicin | Capsazepine | EIPA | Diphenyleneiodonium chloride | HC-030031 | SKF-96365 | HC 067047 | AMG 9810 | GSK-1016790A | SAR7334 | PF-4840154 | RN-1734 | AMG-517 | SB-366791 | IcilinAG-3-5

Chemical & Physical Properties

[ 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℃

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Precautionary Statements ]:
P301 + P312 + P330

[ RIDADR ]:
NONH for all modes of transport

Related Compounds