SML2635
Z944 hydrochloride
≥98% (HPLC), T-type calcium channel blocker, powder
别名:
4-[[(3-Chloro-5-fluorobenzoyl)amino]methyl]-N-(1,1-dimethylethyl)-1-piperidineacetamide hydrochloride, N-((1-(2-(tert-Butylamino)-2-oxoethyl)piperidin-4-yl)methyl)-3-chloro-5-fluorobenzamide hydrochloride, Z 944 hydrochloride, Z-944
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关于此项目
经验公式（希尔记法）:
C19H27ClFN3O2 · xHCl
分子量:
383.89 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
Z944 hydrochloride, ≥98% (HPLC)
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
Orally available, state-dependent, potent and selective T-type calcium channel blocker (Cav3.1, Cav3.2, Cav3.3) with in vivo absence seizure-reducing efficacy.
Z944 is an orally available, state-dependent, potent and selective T-type calcium channel blocker (hCav3.1/Cav3.2/Cav3.3 IC50 by voltage clamp = 50/160/110 nM under ~30% inactivated state & 130/540/260 nM in the closed state) over non-T-type voltage-gated channels (rCaV2.2 IC50 = 11 μM/30% inactivated & 150 μM/closed; hERG/rCaV1.2/hNaV1.5 IC50 = 7.8/32/100 μM). Z944 effectively suppresses seizure activity in the GAERS (absence epilepsy rats from Strasbourg) model in vivo (10-30 mg/kg qod ip.) with no adverse cardiovascular effects or neurotoxicity.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Elizabeth Tringham et al.
Science translational medicine, 4(121), 121ra19-121ra19 (2012-02-22)
Absence seizures are a common seizure type in children with genetic generalized epilepsy and are characterized by a temporary loss of awareness, arrest of physical activity, and accompanying spike-and-wave discharges on an electroencephalogram. They arise from abnormal, hypersynchronous neuronal firing
Wendie N Marks et al.
Neurobiology of disease, 94, 106-115 (2016-06-11)
Childhood absence epilepsy (CAE) is often comorbid with behavioral and cognitive symptoms, including impaired visual memory. Genetic Absence Epilepsy Rats from Strasbourg (GAERS) is an animal model closely resembling CAE; however, cognition in GAERS is poorly understood. Crossmodal object recognition
Andrew J Roebuck et al.
Psychopharmacology, 235(11), 3339-3350 (2018-09-27)
Currently available antipsychotics are unsatisfactory given their side effects and limited efficacy for the cognitive symptoms of schizophrenia. Many currently available drugs, such as haloperidol, are T-type calcium channel antagonists in addition to their well-established antagonism of dopamine D2 receptors.
Z944: a first in class T-type calcium channel modulator for the treatment of pain.
M Lee
Journal of the peripheral nervous system : JPNS, 19 Suppl 2, S11-S12 (2014-10-02)
Mark T Henbid et al.
Experimental neurology, 296, 16-22 (2017-06-29)
Childhood absence epilepsy (CAE) is associated with interictal co-morbid symptoms including abnormalities in social behaviour. Genetic Absence Epilepsy Rats from Strasbourg (GAERS) is a model of CAE that exhibits physiological and behavioural alterations characteristic of the human disorder. However, it
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