SR27897
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- CAS号:
- 136381-85-6
- 英文名:
- SR27897
- 英文别名:
- SR27897;SR 27897 hydrate;{2-[4-(2-Chloro-phenyl)-thiazol-2-ylcarbamoyl]-indol-1-yl}-acetic acid;2-[[[4-(2-Chlorophenyl)-2-thiazolyl]amino]carbonyl]-1H-indole-1-aceticacid;2-(2-((4-(2-Chlorophenyl)thiazol-2-yl)carbamoyl)-1H-indol-1-yl)acetic acid;1H-Indole-1-acetic acid,2-[[[4-(2-chlorophenyl)-2-thiazolyl]amino]carbonyl]-;2-[[[4-(2-chlorophenyl)-2-thiazolyl]amino]carbonyl]-1H-indole-1-acetic acid hydrate
- 中文名:
- SR27897
- 中文别名:
- SR 27897(LINTITRIPT),竞争性非肽CCK 1受体拮抗剂;2-(2-((4-(2-氯苯基)噻唑-2-基)氨基甲酰基)-1H-吲哚-1-基)乙酸
- CBNumber:
- CB11074591
- 分子式:
- C20H14ClN3O3S
- 分子量:
- 411.86
- MOL File:
- 136381-85-6.mol
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SR27897化学性质
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密度:
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1.49±0.1 g/cm3(Predicted)
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储存条件:
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Desiccate at +4°C
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溶解度:
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DMSO: ≥10mg/mL at warmed to 60°C
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酸度系数(pKa):
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4.00±0.10(Predicted)
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形态:
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powder
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颜色:
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white to tan
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SR27897性质、用途与生产工艺
Lintitript (SR 27897) 是一种高效，选择性，口服活性，竞争性和非肽类 CCK1 受体拮抗剂，EC50 为 6 nM，Ki 为 0.2 nM。Lintitript 对 CCK1 的选择性比对 CCK2 受体的选择性高 33 倍以上 (EC50值为 200 nM)。Lintitript 增加瘦素的血浆浓度和食物摄入以及胰岛素的血浆浓度。
EC50: 6 nM (cholecystokinin (CCK1) receptor); Ki: 0.2 nM (cholecystokinin (CCK1) receptor)
In vitro, Lintitript (SR 27897) is a competitive antagonist of cholecystokinin (CCK)-stimulated amylase release in isolated rat pancreatic acini (pA
2
= 7.50) and of CCK-induced guinea pig gall bladder contractions (pA
2
= 9.57).
Lintitript produces concentration dependent inhibition of [
125
I]CCK binding to CCK1 receptor sites in the rat pancreas (IC
50
value of 0.58 nM) and also to CCK 2 sites in the guinea pig cortex (IC
2
value of 479 nM). Lintitript inhibits [
125
I]gastrin binding to gastrin receptors. Lintitript (0.5 nM) increases the dissociation constant of CCK for the CCK A receptor (K
d
= 1.8 to 7.2 nM) without modifying the maximum number of receptors (B
max
= 1800 to 1770 fmol/mg).
Lintitript (SR 27897; 1 mg/kg, i.v.) completely reverses the CCK-induced amylase secretion. Lintitript also inhibits CCK-induced gastric and gallbladder emptying in mice (ED
50
s = 3 and 72 μg/kg, respectively). Lintitript is also very active (ED
50
= 27 μg/kg p.o.) in the gall bladder emptying protocol with egg yolk as an inducer of endogenous CCK release.
SR27897
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| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2023/01/06 | S0753 | SR27897
Lintitript | 136381-85-6 | 5mg | 4152.47元 |
136381-85-6, SR27897 相关搜索:
- 合成有机化合物配体
- SR 27897(LINTITRIPT),竞争性非肽CCK 1受体拮抗剂
- 2-(2-((4-(2-氯苯基)噻唑-2-基)氨基甲酰基)-1H-吲哚-1-基)乙酸
- 136381-85-6
- 2-(2-((4-(2-Chlorophenyl)thiazol-2-yl)carbamoyl)-1H-indol-1-yl)acetic acid
- {2-[4-(2-Chloro-phenyl)-thiazol-2-ylcarbamoyl]-indol-1-yl}-acetic acid
- 1H-Indole-1-acetic acid,2-[[[4-(2-chlorophenyl)-2-thiazolyl]amino]carbonyl]-
- SR 27897 hydrate
- 2-[[[4-(2-chlorophenyl)-2-thiazolyl]amino]carbonyl]-1H-indole-1-acetic acid hydrate
- 2-[[[4-(2-Chlorophenyl)-2-thiazolyl]amino]carbonyl]-1H-indole-1-aceticacid
- SR27897