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ZSET1446 (ST101)

Cat. No. M21720
ZSET1446 (ST101) Structure
Synonym:

ST101; ZSET-1446

Size Price Availability Quantity
5mg USD 330  USD330 In stock
10mg USD 480  USD480 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Yasushi Yabuki, et al. J Pharmacol Sci . Cognitive enhancer ST101 improves schizophrenia-like behaviors in neonatal ventral hippocampus-lesioned rats in association with improved CaMKII/PKC pathway

[2] Kentaro Takeda, et al. J Pharmacol Exp Ther. Potentiation of Acetylcholine-Mediated Facilitation of Inhibitory Synaptic Transmission by an Azaindolizione Derivative, ZSET1446 (ST101), in the Rat Hippocampus

[3] Yoshimasa Yamaguchi, et al. J Pharmacol Sci . Combination effects of ZSET1446/ST101 with memantine on cognitive function and extracellular acetylcholine in the hippocampus

[4] Yoshimasa Yamaguchi, et al. J Pharmacol Sci. Combination effects of ZSET1446/ST101 with memantine on cognitive function and extracellular acetylcholine in the hippocampus

[5] Yui Yamamoto, et al. J Pharmacol Sci . Novel cognitive enhancer ST101 enhances acetylcholine release in mouse dorsal hippocampus through T-type voltage-gated calcium channel stimulation

[6] Yoshimasa Yamaguchi, et al. J Pharmacol Sci . Effects of ZSET1446/ST101 on cognitive deficits and amyloid β deposition in the senescence accelerated prone mouse brain

[7] Yoshimasa Yamaguchi, et al. J Pharmacol Sci. Effects of ZSET1446/ST101 on cognitive deficits and amyloid β deposition in the senescence accelerated prone mouse brain

[8] Shigeki Moriguchi, et al. J Neurochem . The T-type voltage-gated calcium channel as a molecular target of the novel cognitive enhancer ST101: enhancement of long-term potentiation and CaMKII autophosphorylation in rat cortical slices

[9] Kim N Green, et al. Ann Neurol. ST101 induces a novel 17 kDa APP cleavage that precludes Aβ generation in vivo

[10] Norifumi Shioda, et al. J Pharmacol Exp Ther . A novel cognitive enhancer, ZSET1446/ST101, promotes hippocampal neurogenesis and ameliorates depressive behavior in olfactory bulbectomized mice

[11] Norifumi Shioda, et al. J Pharmacol Exp Ther. A novel cognitive enhancer, ZSET1446/ST101, promotes hippocampal neurogenesis and ameliorates depressive behavior in olfactory bulbectomized mice

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Keywords: ZSET1446 (ST101), ST101; ZSET-1446 supplier, AChR/AChE, inhibitors, activators


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