THPP-1


CAS No. : 1257051-63-0

1257051-63-0
Price and Availability of CAS No. : 1257051-63-0
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5mg $50 In-stock
10mg $80 In-stock
25mg $155 In-stock
50mg $245 In-stock
100mg $395 In-stock
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Cat. No. : HY-117604
M.Wt: 464.90
Formula: C23H21ClN6O3
Purity: >98 %
Solubility: DMSO : 31.25 mg/mL (ultrasonic)
Introduction of 1257051-63-0 :

THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species[1]. IC50 & Target: IC50: 1-1.3 nM (PDE10A)[1]. In Vivo: THPP-1 (0.1-1.0 mg/kg, p.o.) shows novel object recognition in rats[1].
THPP-1 (p.o., 1-30 mg/kg) dose-dependently increases phosphorylation of GluR1 S845 in the rat striatum whereas the total levels of GluR1 in the striatum are not affected. Administration of THPP-1 also results in an associated increase in the pGluR1/GluR1 ratios at all doses examined in this study[1].
THPP-1 (1, 3, 10 mg/kg, p.o.) significantly attenuated the stimulant effects in stimulant-induced motor activity (SIMA) in monkey[2].

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