Loxiglumide (CR-1505)
(Synonyms: 氯谷胺,CR-1505) 目录号 : GC31382
A CCK receptor antagonist
Cas No.:107097-80-3
Sample solution is provided at 25 µL, 10mM.
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Loxiglumide is a cholecystokinin (CCK) receptor antagonist that inhibits CCK-8 binding to central and peripheral CCK receptors with Ki values of 9.1 and 0.33 μM, respectively.1 It inhibits CCK-8-induced release of acetylcholine from isolated guinea pig gallbladder (IC50 = 10 nM).2 Loxiglumide (50 μM) reduces the invasion of PANC-1 and MiaPaCa-2 human pancreatic cancer cells by 83.1 and 82.9%, respectively, in vitro.3 Loxiglumide (10-5,000 μM) reduces DNA synthesis in PC-TI and PC-YY human pancreatic cancer cells in a concentration-dependent manner (IC50s = 160 and 74 μM, respectively).4 It reduces the tumor growth rate by 37.5 and 38%, respectively, in PC-TI and PC-YY mouse xenograft models when administered at a dose of 250 mg/kg. Loxiglumide is toxic to mice with LD50 values ranging from 440 to 500 mg/kg dependent on the route of administration. In a rat model of acute pancreatitis, loxiglumide (50 mg/kg, s.c.) reduces serum concentrations of CCK, amylase, and lipase by greater than 60%, as well as tissue hemorrhaging and acinar cell necrosis.5
1.Setnikar, I., Bani, M., Cereda, R., et al.Pharmacological characterisation of a new potent and specific nonpolypeptidic cholecystokinin antagonistArzneimittelforschung37(6)703-707(1987) 2.Rakovska, A., Sgaragli, G., Mantovani, P., et al.Effect of loxiglumide (CR 1505) on CCK-induced contractions and 3H-acetylcholine release from guinea-pig gallbladderNeuropeptides25(5)271-276(1993) 3.Hirata, M., Itoh, M., Tsuchida, A., et al.Cholecystokinin receptor antagonist, loxiglumide, inhibits invasiveness of human pancreatic cancer cell linesFEBS. Lett.383(3)241-244(1996) 4.Nio, Y., Tsubono, M., Morimoto, H., et al.Loxiglumide (CR 1 505), a cholecystokinin antagonist, specifically inhibits the growth of human pancreatic cancer lines xenografted into nude miceCancer72(12)3599-3606(1993) 5.Tani, S., Itoh, H., Koide, M., et al.Involvement of endogenous cholecystokinin in the development of acute pancreatitis induced by closed duodenal loopPancreas8(1)109-115(1993)
Animal experiment: | Rats[1] At 24 h after induction of acute hemorrhagic pancreatitis, rats are divided into four different treatment groups: standard rat chow (AP-C); standard rat chow with pancreatic rest (AP-R); standard rat chow with pancreatic stimulation (AP-S); and standard rat chow with pancreatic rest, followed by pancreatic stimulation (AP-R/S). Rats in the AP-C group receive 2 mL/kg body weight saline orally (po) via an orogastric tube twice daily (09:00 and 21:00 h) for 10 d; the AP-R group receive 50 mg/kg body weight of CCK-1 receptor antagonist Loxiglumide dissolved in 2 mL distilled water po twice daily for 10 d; the AP-S group receive 25 mg/kg body weight protease inhibitor Camostat, which is known to stimulate endogenous CCK release, dissolved in 2 mL distilled water po twice daily for 10 d; and the AP-R/S group receive 50 mg/kg body weight Loxiglumide twice daily for the first 5 d followed by 25 mg/kg body weight camostat twice daily for the next 5 d. Rats are fed ad libitum. On day 12 at 24 h after the last treatment and overnight fasting, pancreatic exocrine function and histological examination of the pancreas are performed. |
References: [1]. Jia D, et al. Effect of endogenous cholecystokinin on the course of acute pancreatitis in rats. World J Gastroenterol. 2015 Jul 7;21(25):7742-53. | |
| Cas No. | 107097-80-3 | SDF | |
| 别名 | 氯谷胺,CR-1505 | ||
| Canonical SMILES | O=C(O)CCC(NC(C1=CC=C(Cl)C(Cl)=C1)=O)C(N(CCCOC)CCCCC)=O | ||
| 分子式 | C21H30Cl2N2O5 | 分子量 | 461.38 |
| 溶解度 | DMSO : ≥ 150 mg/mL (325.11 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1674 mL | 10.8371 mL | 21.6741 mL |
| 5 mM | 0.4335 mL | 2.1674 mL | 4.3348 mL |
| 10 mM | 0.2167 mL | 1.0837 mL | 2.1674 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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