PF-04995274 , 10mMinDMSO , 1331782-27-4

CAS NO.：1331782-27-4

Empirical Formula: C23H32N2O6

Molecular Weight: 432.51

MDL number:

PRODUCT Properties

• storage temp.: Store at -20°C
• solubility: DMSO:20.0(Max Conc. mg/mL);46.2(Max Conc. mM)
• form: A crystalline solid
• color: White to off-white

Description and Uses

PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT_4A, 5-HT_4B, 5-HT_4D, and 5-HT_4E (K_is = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay). It increases cAMP levels in HEK293 cells expressing 5-HT_4A, 5-HT_4B, 5-HT_4D, and 5-HT_4E receptors (EC₅₀s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.

PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease[1][2][3].