Lorglumide (sodium salt) (Synonyms: CR-1409 sodium salt) |
| رقم الكتالوجGC10360 |
Lorglumide (ملح الصوديوم) (CR-1409 ملح الصوديوم) هو مضاد قوي لمستقبلات الكوليسيستوكينين (CCK).
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| المرادفات | CR-1409 sodium salt | ||
| Chemical Name | 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] | ||
| Formula | C22H31Cl2N2O4 • Na | M.Wt | 481.4 |
| الذوبان | ≤1mg/ml in ethanol;1mg/ml in DMSO;1mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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