Lorglumide (sodium salt)
(Synonyms: CR-1409 sodium salt) 目录号 : GC10360
A selective antagonist of CCK1
Cas No.:1021868-76-7
Sample solution is provided at 25 µL, 10mM.
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Lorglumide (sodium salt) is the first nonpeptidic, selective and potent inhibitor of the CCK-A receptor [1][2][3][4] .
Cholecystokinin (CCK) is a peptide hormone that plays important roles in the physiological regulation of pancreatic enzyme secretion, induction of pancreatic growth, smooth muscle contraction in the gall bladder and stomach, and modulation of feeding and behavior [1][2][3].
Lorglumide (CR1409) is the first nonpeptidic, selective and potent inhibitor of the CCK-A receptor. Lorglumide inhibited CCK A receptor and CCK B receptor with IC50 values of 50 nM and 3 μM, respectively [4]. In the guinea-pig isolated ileum, Lorglumide (0.06-2.1 μM) antagonized longitudinal muscle responses to ceruletide (a CCK-related decapeptide) and CCK-octapeptide (CCK-8) in a concentration dependent and competitive manner. Lorglumide (0.2-0.4 μM) also blocked contractions of the circular muscle induced by ceruletide [2].
In mice, CR1409 completely abolished the trophic effects of exogenous CCK and significantly inhibited the effects of chronic camostate feeding. CR1409 reduced pancreatic weight, DNA and protein content [3].
References:
[1]. Makovec F, Peris W, Revel L, et al. Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives. J Med Chem. 1992 Jan;35(1):28-38.
[2]. Barthó L, Holzer P, Lembeck F, et al. Evaluation of a new and potent cholecystokinin antagonist on motor responses of the guinea-pig intestine. Br J Pharmacol. 1987 Apr;90(4):753-61.
[3]. Niederau C, Liddle RA, Williams JA, et al. Pancreatic growth: interaction of exogenous cholecystokinin, a protease inhibitor, and a cholecystokinin receptor antagonist in mice. Gut. 1987;28 Suppl:63-9.
[4]. Scarpignato C, Varga G, Dobronyi I, et al. Effect of a new potent CCK antagonist, lorglumide, on caerulein- and bombesin-induced pancreatic secretion and growth in the rat. Br J Pharmacol. 1989 Mar;96(3):661-9.
| Cas No. | 1021868-76-7 | SDF | |
| 别名 | CR-1409 sodium salt | ||
| 化学名 | 4-[(3,4-dichlorobenzoyl)amino]-5-(dipentylamino)-5-oxo-pentanoic acid, monosodium salt | ||
| Canonical SMILES | ClC1=C(Cl)C=CC(C(NC(C(N(CCCCC)CCCCC)=O)CCC([O-])=O)=O)=C1.[Na] | ||
| 分子式 | C22H31Cl2N2O4 • Na | 分子量 | 481.4 |
| 溶解度 | ≤1mg/ml in ethanol;1mg/ml in DMSO;1mg/ml in dimethyl formamide | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0773 mL | 10.3864 mL | 20.7727 mL |
| 5 mM | 0.4155 mL | 2.0773 mL | 4.1545 mL |
| 10 mM | 0.2077 mL | 1.0386 mL | 2.0773 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet