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首页-小分子抑制剂&激动剂-GPCR-Neurokinin Receptor-Talnetant
Talnetant

Chemical Structure : Talnetant

CAS No.: 174636-32-9

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Talnetant (SB 223412, SB223412)

货号: PC-21365Not For Human Use, Lab Use Only.

Talnetant (SB223412) is a potent, selective, competitive and brain-permeable neurokinin-3 receptor (NK3R) antagonist with Ki of 1.4 nM in hNK-3-CHO cells.

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10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg ￥3880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Talnetant (SB223412) is a potent, selective, competitive and brain-permeable neurokinin-3 receptor (NK3R) antagonist with Ki of 1.4 nM in hNK-3-CHO cells.
Talnetant (SB223412) displays >100-fold selectivity for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant (SB223412) reduces the accumulation of NKB-induced IP in U-2OS cells expressing the human NK3 receptor.
Talnetant (SB223412) inhibit the miosis induced by senktide in a dose-dependent manner with an ED50 of 0.44mg/kg in conscious rabbits.
Talnetant (SB223412) significantly attenuate senktide-induced "wet dog wagging" behavior in a dose-dependent manner.
Talnetant (SB223412) significantly increase extracellular dopamine and norepinephrine in the medial prefrontal cortex and reduce haloperidol-induced increases in dopamine levels in the vomeronasal nucleus of freely moving guinea pigs.

物理化学性质&存储条件

分子量 382.46
分子式 C25H22N2O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-Hydroxy-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide

参考文献

1. Giardina GA, et al. J Med Chem. 1999 Mar 25;42(6):1053.

2. Dawson LA, et al. Neuropsychopharmacology. 2008 Jun;33(7):1642-52.

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