ZSET1446 (ST101) is a novel cognitive enhancer that significantly improves learning deficits in various types of Alzheimer disease (AD) models. ZSET1446 is also a T-type calcium channel activator. ZSET1446 potentiates the facilitatory effect of nAChR stimulation on sPSC frequency.
ZSET1446 (ST101) shows ameliorating effects on senescence accelerated prone mouse strain 8 (SAMP8) partly due to the suppression of an increase of amyloid-beta-deposition in the hippocampus. Moreover, oral administration of ZSET1446 or memantine increased the extracellular level of ACh in the hippocampus as compared with the control. Further, concomitant administration of subeffective doses of ZSET1446 and memantine significantly increased the extracellular level of ACh as compared with the group of ZSET1446 or memantine alone.
Molecular Weight | 236.27 |
Formula | C15H12N2O |
CAS Number | 887603-94-3 |
Solubility (25°C) | DMSO 48 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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