| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
CCK receptors (pancreatic CCK receptors). Schild plot analysis for antagonism of caerulein‑induced amylase release gave a pA₂ value of 7.31 ± 0.45. [1]
|
|---|---|
| ln Vitro |
Lorglumide (3×10⁻⁷ M, 1×10⁻⁶ M, 1×10⁻⁵ M) displaced the concentration‑response curves of caerulein for amylase release from isolated and perfused rat pancreatic segments to the right without affecting the maximum response, indicating competitive antagonism. The Schild plot slope was 0.78±0.22 (not significantly different from unity). Lorglumide at concentrations up to 10⁻⁴ M did not affect basal amylase release. When tested against bombesin‑induced amylase release, lorglumide (1×10⁻⁵ M) was completely ineffective. [1]
The potency (pD₂) of caerulein was 9.97±0.21 and of bombesin 8.29±0.11; maximum effects were not significantly different between the two peptides. [1] |
| ln Vivo |
In anaesthetized rats, caerulein (1 μg kg⁻¹ i.p.) increased pancreatic juice volume to 119±10 μl 60 min⁻¹ and protein output to 14.3±1.1 mg 60 min⁻¹. Pretreatment with lorglumide (5 mg kg⁻¹ i.p.) reduced protein output to 10.2±1.2 mg 60 min⁻¹ (P<0.05), and lorglumide (10 mg kg⁻¹) reduced juice volume to 56±9 μl 60 min⁻¹ and protein output to 5.7±1.3 mg 60 min⁻¹ (P<0.05 vs caerulein). Lorglumide did not affect bombesin (10 μg kg⁻¹ i.p.)‑stimulated pancreatic secretion (juice volume 119±12 to 128±7 μl 60 min⁻¹; protein output 14.4±1.5 to 15.4±1.1 mg 60 min⁻¹). [1]
In a 5‑day trophic study, caerulein (1 μg kg⁻¹ s.c., three times daily) increased pancreatic weight, total protein, DNA, trypsin and amylase content. Co‑administration of lorglumide (10 mg kg⁻¹ i.p., 15 min before caerulein) significantly reduced the caerulein‑induced increases in pancreatic weight, protein and enzyme content. Lorglumide given with bombesin (10 μg kg⁻¹ s.c.) did not alter any of the bombesin‑induced trophic parameters. Lorglumide alone did not significantly affect pancreatic size or composition. [1] |
| Animal Protocol |
For in vivo secretory studies, male OFA rats (180‑200 g) were anaesthetized with urethane (1.2 g kg⁻¹ i.p.). The pylorus and common bile duct at the hepatic hilum were ligated, and a polyethylene cannula was introduced into the duodenal part of the duct for collecting pure pancreatic juice. Basal juice was collected for 60 min. Rats received caerulein (1 μg kg⁻¹ i.p.) or bombesin (10 μg kg⁻¹ i.p.). Lorglumide (5 or 10 mg kg⁻¹) or saline was given intraperitoneally 15 min before the peptide. Pancreatic juice was then collected for another 60 min. [1]
For trophic studies, male OFA rats (60‑80 g) were treated three times daily for 5 days. Groups received: saline; lorglumide (10 mg kg⁻¹ i.p.); caerulein (1 μg kg⁻¹ s.c.); caerulein + lorglumide (same doses); bombesin (10 μg kg⁻¹ s.c.); bombesin + lorglumide. Lorglumide was injected i.p. 15 min before the peptide. The last peptide dose was given 12 h before sacrifice, then the whole pancreas was excised. [1] For in vitro superfusion experiments, rat pancreatic segments (3‑5 mg each, total ~150 mg) were placed in a 1 ml tissue flow chamber and superfused at 1.4 ml min⁻¹ with modified Krebs‑Henseleit solution (pH 7.4, 37°C, gassed with 95% O₂:5% CO₂). The effluent was discarded for the first 30 min, then fractions collected every 3 min. Peptides and lorglumide were added directly to the superfusion solution. When testing inhibition, lorglumide superfusion started 15 min before peptide application and continued throughout. Cumulative concentration‑response curves were constructed (each concentration applied for 12 min). [1] |
| References | |
| Additional Infomation |
Lorglumide is a selective CCK receptor antagonist that does not affect bombesin‑induced pancreatic secretion or growth, demonstrating that bombesin acts through its own receptors and not via CCK release in the rat. The compound is a useful tool for characterizing CCK‑receptor interactions in peripheral organs. [1]
|
| Molecular Formula |
C22H31CL2N2NAO4
|
|---|---|
| Molecular Weight |
481.3883
|
| Exact Mass |
480.155
|
| CAS # |
1021868-76-7
|
| PubChem CID |
23681233
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
31
|
| Complexity |
544
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JCNPYMDDOUQTBK-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C22H32Cl2N2O4.Na/c1-3-5-7-13-26(14-8-6-4-2)22(30)19(11-12-20(27)28)25-21(29)16-9-10-17(23)18(24)15-16;/h9-10,15,19H,3-8,11-14H2,1-2H3,(H,25,29)(H,27,28);/q;+1/p-1
|
| Chemical Name |
sodium;4-[(3,4-dichlorobenzoyl)amino]-5-(dipentylamino)-5-oxopentanoate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~207.73 mM)
H2O : ≥ 100 mg/mL (~207.73 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.32 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 50 mg/mL (103.87 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0773 mL | 10.3866 mL | 20.7732 mL | |
| 5 mM | 0.4155 mL | 2.0773 mL | 4.1546 mL | |
| 10 mM | 0.2077 mL | 1.0387 mL | 2.0773 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
