Product Name :
PF-05180999
Description:
PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM.
CAS:
1394033-54-5
Molecular Weight:
414.39
Formula:
C19H17F3N8
Chemical Name:
2-4-[4-(azetidin-1-yl)-7-methylimidazo[4,3-f][1,2,4]triazin-5-yl]-1-methyl-1H-pyrazol-5-yl-5-(trifluoromethyl)pyridine
Smiles :
CN1N=CC(=C1C1=CC=C(C=N1)C(F)(F)F)C1N=C(C)N2N=CN=C(C2=1)N1CCC1
InChiKey:
CLGCHUKGBICQTE-UHFFFAOYSA-N
InChi :
InChI=1S/C19H17F3N8/c1-11-27-15(17-18(29-6-3-7-29)24-10-26-30(11)17)13-9-25-28(2)16(13)14-5-4-12(8-23-14)19(20,21)22/h4-5,8-10H,3,6-7H2,1-2H3
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM.|Product information|CAS Number: 1394033-54-5|Molecular Weight: 414.39|Formula: C19H17F3N8|Chemical Name: 2-4-[4-(azetidin-1-yl)-7-methylimidazo[4,3-f][1,2,4]triazin-5-yl]-1-methyl-1H-pyrazol-5-yl-5-(trifluoromethyl)pyridine|Smiles: CN1N=CC(=C1C1=CC=C(C=N1)C(F)(F)F)C1N=C(C)N2N=CN=C(C2=1)N1CCC1|InChiKey: CLGCHUKGBICQTE-UHFFFAOYSA-N|InChi: InChI=1S/C19H17F3N8/c1-11-27-15(17-18(29-6-3-7-29)24-10-26-30(11)17)13-9-25-28(2)16(13)14-5-4-12(8-23-14)19(20,21)22/h4-5,8-10H,3,6-7H2,1-2H3|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 50 mg/mL (120.Protease Inhibitor Cocktail MedChemExpress 66 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.Crizotinib Autophagy |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.PMID:33113334 6 nM. PF-05180999 binds to the rat, dog and monkey PDE2A, with Kis of 4.2, 8.4, and 5.5 nM and IC50s of 2.6, 5.2, and 3.4 nM, respectively. PF-05180999 shows weak activity against PDE, with IC50s of 2.03 μM (PDE10A1), 26.969 μM (PDE7B), 50.09 μM (PDE11A4), and >56.25 μM (PDE1B1, PDE3A1, PDE4D3, PDE5A1, PDE6 (bovine), PDE8B, PDE9A1), respectively. PF-05180999 is also a weak inducer of CYP3A4, and with no direct inhibition of human recombinant cytochrome P450 (CYP) enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A) and no induction of CYP1A2.|In Vivo:|PF-05180999 (Compound 30; 0.032-0.32 mg/kg mg/kg, s.c.) dramatically reduces the working memory errors produced by ketamine in a working memory radial arm maze (RAM) model in rats. PF-05180999 causes acute and exposure-dependent elevation in the accumulation of cGMP bulk levels in the cortex, striatum, and hippocampus, but with no changes in cAMP and the associated downstream phospho-cAMP response element-binding protein (p-CREB) in mice.|Products are for research use only. Not for human use.|
