SR 142948 dihydrochloride|西域试剂

SR 142948 dihydrochloride,98.0%

产品编号：Bellancom-107664A| 分子式：C₃₉H₅₃Cl₂N₅O₆| 分子量：758.77

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货号	价格	库存与货期
Bellancom-107664A	￥1600.00	杭州北京（现货）
Bellancom-107664A	￥5440.00	杭州北京（现货）
Bellancom-107664A	￥8700.00	杭州北京（现货）

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SR 142948 dihydrochloride

产品介绍

SR 142948 dihydrochloride 是一种具有口服活性、选择性的非肽神经降压素受体 (NT) 拮抗剂，在 h-NTR1-CHO 细胞、HT-29 细胞和成年大鼠脑中的 IC₅₀ 分别为 1.19 nM、0.32 nM、3.96 nM。SR 142948 dihydrochloride 在 HT-29 细胞中拮抗 NT 诱导的肌醇单磷酸盐形成，IC₅₀ 为 3.9 nM。SR 142948 dihydrochloride 在体内阻断 NT 诱导的体温过低、镇痛和转向行为。SR 142948 dihydrochloride 可以透过血脑通透性，可用于精神疾病的研究。

生物活性

SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC₅₀s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC₅₀ of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders.

体外研究

SR 142948 (1 µM; 90 分钟) dihydrochloride 抑制 CHO-hNT1-R 细胞中 c-fos 和 krox24 的表达。
SR 142948 (0-1 µM; 1 小时) dihydrochloride 通过抑制 [¹²⁵I-Tyr³]NT 与 h-NTR1-CHO 和 HT 29 细胞膜的结合表现出良好的拮抗活性，IC₅₀ 分别为 1.19 和 0.32 nM。
SR 142948 (0-1 µM; 30 分钟) dihydrochloride 以浓度依赖性方式拮抗 h-NTR1-CHO 和 HT 29 细胞中 NT 刺激的 IP1 的产生。
SR 142948 (1, 10 nM; 60-80 秒) dihydrochloride 拮抗 h-NTR1-CHO 细胞中 NT 刺激的细胞内钙动员。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

SR 142948 (2 µg/kg; 口服; 单次) dihydrochloride 抑制 NT (10 pg/小鼠) 诱导的转向行为。
SR 142948 (0.01, 0.03, 0.3 mg/kg; 腹腔注射; 单次) dihydrochloride 以剂量依赖性方式阻止 NT (100 nM) 产生的 ACh 释放增强。
SR 142948 (90-10 mg/kg; 口服; 单次) dihydrochloride 部分但显着地阻断 NT 诱导的体温过低 (大鼠 2 mg/kg 时 53% 和小鼠 4 mg/kg 时 54%)。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Swiss albino CD1 mice (25-30 g; intrastriatal injection of 10 pg/mouse NT)
Dosage:	2 µg/kg
Administration:	Oral administration; single
Result:	Inhibited the turning behavior with maximal and significant antagonism between 1-2 h after administration.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Swiss albino CD1 mice (25-30 g; intrastriatal injection of 10 pg/mouse NT)
Dosage:	2 µg/kg
Administration:	Oral administration; single
Result:	Inhibited the turning behavior with maximal and significant antagonism between 1-2 h after administration.