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首页-小分子抑制剂&激动剂-GPCR-Neurokinin Receptor-SR140333B
SR140333B

Chemical Structure : SR140333B

CAS No.: 155418-06-7

SR140333B (SR-140333B, Nolpitantium besilate)

货号: PC-22655Not For Human Use, Lab Use Only.

Nolpitantium besilate (SR140333B) is a potent, selective, non-peptide NK1 receptor antagonist with Ki of 0.74 nM, IC50 of 1.6 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Nolpitantium besilate (SR140333B) is a potent, selective, non-peptide NK1 receptor antagonist with Ki of 0.74 nM, IC50 of 1.6 nM.
Nolpitantium (SR140333) shows no effect in bioassays for NK2 and NK3 receptors.
Nolpitantium (SR140333) blocks substance P-induced release of acetylcholine from rat striatum, exerts highly potent antagonism toward substance P-induced hypotension in vivo.
Nolpitantium (SR140333) also blocks the activation of rat thalamic neurons after nociceptive stimulation.

物理化学性质&存储条件

分子量 777.84
分子式 C43H50Cl2N2O5S
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

1-Azoniabicyclo[2.2.2]octane, 1-[2-[(3S)-3-(3,4-dichlorophenyl)-1-[2-[3-(1-methylethoxy)phenyl]acetyl]-3-piperidinyl]ethyl]-4-phenyl-, benzenesulfonate (1:1)

参考文献

1. Emonds-Alt X, et al. Eur J Pharmacol. 1993 Dec 21;250(3):403-13.

2. Jung M, et al. Neuropharmacology. 1994 Feb;33(2):167-79.

3. Oury-Donat F, et al. J Neurochem. 1994 Apr;62(4):1399-407.

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