Loxiglumide
Based on 4 publication(s) in Google Scholar
Loxiglumide is a cholecystokinin (CCK-1) receptor antagonist.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.0%
- CAS 番号: 107097-80-3
- 分子式: C21H30Cl2N2O5
- 分子量:461.38
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 Loxiglumide
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生物活性
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CCKAR |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
195 nM
Compound: Loxiglumide
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Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
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[PMID: 16610788] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 107097-80-3
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性状 Solid
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分子量 461.38
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分子式 C21H30Cl2N2O5
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Color White to off-white
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SMILES
O=C(O)CCC(NC(C1=CC=C(Cl)C(Cl)=C1)=O)C(N(CCCOC)CCCCC)=O
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別名
CR-1505; ロキシグルミド
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Sodium oligomannate activates the enteroendocrine-vagal afferent pathways in APP/PS1 mice. [Abstract]2024 Sep;45(9):1821-1831. PMID: 38702501 -
Neuropharmacology
Chronic stress induces wide-spread hyperalgesia: The involvement of spinal CCK1 receptors. [Abstract]2024 Jul 9:110067. PMID: 38992792 -
Peptides
Cholecystokinin regulates atrial natriuretic peptide secretion through activation of NOX4-Sirt1-LEF1 signaling in beating rat hypoxic atria. [Abstract]2024 Nov:181:171299. PMID: 39326462 -
Oxid Med Cell Longev
Cholecystokinin Octapeptide Promotes ANP Secretion through Activation of NOX4-PGC-1 α-PPAR α/PPAR γ Signaling in Isolated Beating Rat Atria. [Abstract]2022 Jun 20;2022:5905374. PMID: 35770043
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (216.74 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (275 KB)
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SDS (392 KB)
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- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1674 mL | 10.8371 mL | 21.6741 mL | 54.1853 mL |
| 5 mM | 0.4335 mL | 2.1674 mL | 4.3348 mL | 10.8371 mL | |
| 10 mM | 0.2167 mL | 1.0837 mL | 2.1674 mL | 5.4185 mL | |
| 15 mM | 0.1445 mL | 0.7225 mL | 1.4449 mL | 3.6124 mL | |
| 20 mM | 0.1084 mL | 0.5419 mL | 1.0837 mL | 2.7093 mL | |
| 25 mM | 0.0867 mL | 0.4335 mL | 0.8670 mL | 2.1674 mL | |
| 30 mM | 0.0722 mL | 0.3612 mL | 0.7225 mL | 1.8062 mL | |
| 40 mM | 0.0542 mL | 0.2709 mL | 0.5419 mL | 1.3546 mL | |
| 50 mM | 0.0433 mL | 0.2167 mL | 0.4335 mL | 1.0837 mL | |
| 60 mM | 0.0361 mL | 0.1806 mL | 0.3612 mL | 0.9031 mL | |
| 80 mM | 0.0271 mL | 0.1355 mL | 0.2709 mL | 0.6773 mL | |
| 100 mM | 0.0217 mL | 0.1084 mL | 0.2167 mL | 0.5419 mL |