Lorglumide
Lorglumide (CR-1409) is an orally active Cholecystokinin Receptor antagonist. Lorglumide inhibits pancreatic cancer cell proliferation, induces G0/G1 phase arrest and apoptosis, and downregulates MMP-2. Lorglumide inhibits gastrin-stimulated Ornithine decarboxylase activity and DNA synthesis, and shows low CCKA/CCKB selectivity. Lorglumide blocks Caerulein (HY-A0190)-induced exocrine pancreatic secretion and pancreatic tissue hyperplastic changes in rats, and inhibits gallbladder emptying induced by exogenous and endogenous CCK in mice. Lorglumide can be used in research related to pancreatic cancer and pancreatic exocrine function.
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- CAS No.: 97964-56-2
- 화학식: C22H32Cl2N2O4
- 분자량:459.41
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
Other In-stock Forms of Lorglumide
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
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CCKAR |
CCKBR |
MMP-2 |
In Vitro
Lorglumide (10-5-10-4 M; 24 h) reduces Mia PaCa-2 invasion, reported as 77.6 invading cells under the 10-4 M condition marked in Table V[2].
Lorglumide (10-5 M; 24 h) attenuates MMP-2 expression in Mia PaCa-2 cells[2].
Lorglumide (CR1409) displaces gastrin binding on AR42J cells with an IC50 of 3 µM; it competitively antagonizes gastrin-stimulated ODC activity in AR42J cells with a pA2 of 6.5[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mia PaCa-2 human pancreatic adenocarcinoma cells
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Concentration:10-5 M, 10-4 M, 10-3 M
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Incubation Time:24, 48, and 72 h
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Result:Inhibited Mia PaCa-2 cell viability, with 10-4 M reducing viability to 52.1% after 48 h.
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Cell Line:Mia PaCa-2 human pancreatic adenocarcinoma cells
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Concentration:10-5 M, 10-4 M
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Incubation Time:48 h
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Result:Induced G0/G1 cell-cycle arrest in Mia PaCa-2 cells, with 10-4 M producing 40.3% G0/G1 cells after 48 h.
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Cell Line:Mia PaCa-2 human pancreatic adenocarcinoma cells
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Concentration:10-5 M, 10-4 M
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Incubation Time:48 h
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Result:Induced apoptosis in Mia PaCa-2 cells, with 10-4 M producing a 27.1% apoptosis index after 48 h.
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Cell Line:Mia PaCa-2 human pancreatic adenocarcinoma cells
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Concentration:10-5 M (procedure)
10-4 M (Table V) -
Incubation Time:24 h
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Result:Reduced Mia PaCa-2 invasion, with 77.6 invasion cells reported at the Table V-labeled 10-4 M condition.
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Cell Line:Mia PaCa-2 human pancreatic adenocarcinoma cells
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Concentration:10-5 M
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Incubation Time:24 h
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Result:Attenuated MMP-2 expression in Mia PaCa-2 cells.
In Vivo
Lorglumide (10 mg/kg; intraperitoneal injection; three times daily; for 5 consecutive days) attenuates Caerulein-induced pancreatic growth and increased enzyme content in vivo, without affecting Bombesin-induced pancreatic growth in vivo[1].
Lorglumide (CR1409) (oral or intraperitoneal) dose-dependently inhibits egg yolk-induced gallbladder emptying in mice, with ED50 values of 1.1 mg/kg for intraperitoneal administration and 5.0 mg/kg for oral administration; it effectively antagonizes CCK-8-induced gallbladder contraction in mice, with ED50 values of 1.9 mg/kg for intraperitoneal administration and 2.0 mg/kg for oral administration[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:OFA (Sprague-Dawley-derived, 180-200 g)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:i.p.; single pretreatment; 15 min before caerulein
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Result:Reduced caerulein‑stimulated pancreatic juice flow and protein output dose‑dependently at 5 mg/kg and 10 mg/kg, while barely altered Bombesin‑stimulated pancreatic secretion at both doses.
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Animal Model:OFA (Sprague-Dawley-derived, 60-80 g)[1]
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Dosage:10 mg/kg
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Administration:i.p.; three times daily; 5 days; 15 min before each caerulein dose
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Result:Reduced caerulein-evoked elevations in pancreatic weight, total pancreatic protein, amylase and trypsin contents upon co-administration with Caerulein, whereas failed to modify bombesin-triggered changes in pancreatic weight, protein, DNA, amylase and trypsin contents when co-administered with bombesin.
- Mitochondrial membrane-potential fluorescent assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- PCNA Immunodetection Proliferation Assay
- Flow cytometric DNA-content cell-cycle staining
- Protocol for Cell Counting and Cell Density Analysis
- Mitochondrial membrane-potential and mitochondrial mass staining
- Apoptosis Solutions
- MTT Cell Proliferation Assay
Chemical Information
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CAS No. 97964-56-2
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분자량 459.41
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화학식 C22H32Cl2N2O4
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SMILES
O=C(O)CCC(NC(C1=CC=C(Cl)C(Cl)=C1)=O)C(N(CCCCC)CCCCC)=O
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Synonyms
CR-1409
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Lorglumide Related Classifications
HY-B1439 Related Classifications
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Keywords
- Lorglumide
- 97964-56-2
- CR-1409
- CR1409
- CR 1409
- Cholecystokinin Receptor
- MMP
- Ornithine decarboxylase (ODC)
- Apoptosis
- CCK Receptor
- Matrix metalloproteinases
- Ornithine Decarboxylase
- CCK receptor
- CCK-1 receptor
- CCK-B/gastrin receptor
- MMP-2
- amylase release
- apoptosis
- cholecystokinin
- exocrine pancreatic tumors
- gallbladder contraction
- pancreatic cancer
- Inhibitor
- inhibitor
- inhibit