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首页-小分子抑制剂&激动剂-GPCR-Neurotensin Receptor-SR48692
SR48692

Chemical Structure : SR48692

CAS No.: 146362-70-1

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SR48692 (Meclinertant, SR-48692)

货号: PC-60947Not For Human Use, Lab Use Only.

SR48692 (Meclinertant) is a potent, selective and orally active nonpeptide antagonist of neurotensin receptor NTSR1 with IC50 of 0.99 nM (guinea pig), without any intrinsic agonist activity.

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5 mg ￥2480 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SR48692 (Meclinertant) is a potent, selective and orally active nonpeptide antagonist of neurotensin receptor NTSR1 with IC50 of 0.99 nM (guinea pig), without any intrinsic agonist activity.
SR48692 (Meclinertant) blocks K(+)-evoked release of [3H]dopamine stimulated by neurotensin in guinea pig striatal slices with IC50 of 0.46 nM, competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization with pA2 of 8.13 in H29 cells.
SR48692 (Meclinertant) reverses the turning behavior induced by intrastriatal injection of neurotensin in mice.

物理化学性质&存储条件

分子量 587.073
分子式 C32H31ClN4O5
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

(1r,3r,5r,7r)-2-(1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)-1H-pyrazole-3-carboxamido)adamantane-2-carboxylic acid

参考文献

1. Dubuc I, et al. Br J Pharmacol. 1994 Jun;112(2):352-4.

2. Steinberg R, et al. Neuroscience. 1994 Apr;59(4):921-9.

3. Brouard A, et al. Eur J Pharmacol. 1994 Mar 3;253(3):289-91.

4. Gully D, et al. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):65-9.

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