| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
CCK-1 receptor
Loxiglumide targets the cholecystokinin 1 receptor (CCK1R), a G protein-coupled receptor primarily found in the gastrointestinal tract, gallbladder, and pancreas. It acts as a potent and selective antagonist, blocking the actions of CCK, which stimulates gallbladder contraction, pancreatic enzyme secretion, and gut motility. Its mechanism of action involves competitive inhibition of CCK binding to the CCK1 receptor. |
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| ln Vitro |
In vitro, loxiglumide has demonstrated high affinity for the CCK1 receptor in radioligand binding assays. It selectively inhibits CCK-induced contractions in isolated gallbladder and intestinal preparations. Its activity is confirmed by its ability to block CCK-stimulated amylase release from pancreatic acini. The compound shows significant selectivity for CCK1 over CCK2 receptors.
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| ln Vivo |
The effects of oral CCK-1 receptor antagonist Loxiglumide administration on pancreatic rest and pancreas stimulation are examined using endogenous CCK release induced by po protease inhibitor capostat on the recovery of pancreatic secretory function and on the biochemical and histological alterations in the pancreas following acute hemorrhagic pancreatitis. Loxiglumide, a CCK-1 receptor antagonist, when taken orally at a dose of 50 mg/kg body weight, inhibits pancreatic exocrine secretion for a duration exceeding 12 hours. As a result, every 12-hour dose of loxiglumide may totally prevent the pancreas from being affected by endogenously released CCK (pancreatic rest)[1].
In vivo, loxiglumide has been evaluated in animal models and clinical trials for gastrointestinal disorders. It has been shown to reduce postprandial gallbladder contraction and delay gastric emptying. In patients with constipation-predominant irritable bowel syndrome (IBS-C), loxiglumide has demonstrated efficacy in improving bowel function and reducing abdominal pain. |
| Enzyme Assay |
In vitro receptor binding assays are used to measure the affinity of loxiglumide for the CCK1 and CCK2 receptors. These assays involve competition binding with radiolabeled CCK using membrane preparations from cells expressing the receptors. The Ki value is determined, confirming its high affinity and selectivity for the CCK1 receptor.
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| Cell Assay |
In vitro functional assays for loxiglumide are performed using isolated tissue preparations or cell lines expressing CCK receptors. Its ability to inhibit CCK-induced contractions in gallbladder or ileum strips is measured. Its effect on CCK-stimulated amylase release from pancreatic acini is also assessed.
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| Animal Protocol |
Rats: Rats receiving 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) are split into four treatment groups 24 hours after the induction of acute hemorrhagic pancreatitis. The rats in the AP-C group are given 2 mL/kg body weight saline orally (po) via an orogastric tube twice a day (09:00 and 21:00 h) for ten days; the rats in the AP-R group are given 50 mg/kg body weight of CCK-1 receptor antagonist Loxiglumide dissolved in 2 mL distilled water po twice a day for ten days; the rats in the AP-S group are given 25 mg/kg body weight of protease inhibitor Camostat, which is known to stimulate endogenous CCK release, dissolved in 2 mL distilled water po twice a day for 10 days; and the rats in the AP-R/S group are given 50 mg/kg body weight Loxiglumide twice a day for the first five days, followed by 25 mg/kg body weight camostat twice a day for the remaining five days. Rats are given unlimited food. Histological analysis and pancreatic exocrine function tests are carried out on day 12, 24 hours following the final treatment and overnight fast.
In vivo animal experiments for loxiglumide are conducted in models of gastrointestinal motility and gallbladder function. Its effect on gallbladder contraction and intestinal transit is measured. It has also been studied in models of pancreatitis and pain. |
| ADME/Pharmacokinetics |
Loxiglumide has a molecular weight of 516.03 and a molecular formula of C27H30ClN2O6. It is a white to off-white powder, soluble in DMSO and methanol. It should be stored at -20°C. Its pharmacokinetic properties include good oral bioavailability and a half-life suitable for multiple daily dosing.
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| Toxicity/Toxicokinetics |
The toxicological profile of loxiglumide is favorable. In clinical trials, it has been generally well-tolerated. Common side effects include abdominal pain, diarrhea, and nausea. No significant toxicity has been reported at therapeutic doses. Its safety profile supports its continued investigation for gastrointestinal disorders.
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| References | |
| Additional Infomation |
Loxiglumide is an organic molecular entity.
Loxiglumide is a potent and selective CCK1 receptor antagonist. It has been investigated for the treatment of irritable bowel syndrome, constipation, and other gastrointestinal disorders. Its mechanism of action involves blocking the effects of CCK on the gastrointestinal tract. It is a research compound that has undergone clinical trials but is not yet widely approved. |
| Molecular Formula |
C21H30CL2N2O5
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|---|---|
| Molecular Weight |
461.38
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| Exact Mass |
460.153
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| Elemental Analysis |
C, 54.67; H, 6.55; Cl, 15.37; N, 6.07; O, 17.34
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| CAS # |
107097-80-3
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| Related CAS # |
107097-80-3
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| PubChem CID |
60182
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| Appearance |
White to off-white solid powder
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| Density |
1.233g/cm3
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| Boiling Point |
632.2ºC at 760mmHg
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| Flash Point |
336.1ºC
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| Vapour Pressure |
7.51E-17mmHg at 25°C
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| Index of Refraction |
1.537
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| LogP |
4.402
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
30
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| Complexity |
550
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| Defined Atom Stereocenter Count |
0
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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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| InChi Key |
QNQZBKQEIFTHFZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H30Cl2N2O5/c1-3-4-5-11-25(12-6-13-30-2)21(29)18(9-10-19(26)27)24-20(28)15-7-8-16(22)17(23)14-15/h7-8,14,18H,3-6,9-13H2,1-2H3,(H,24,28)(H,26,27)
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| Chemical Name |
4-[(3,4-dichlorobenzoyl)amino]-5-[3-methoxypropyl(pentyl)amino]-5-oxopentanoic acid
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| Synonyms |
CR-1505; CR 1505; CR1505; Loxiglumide; Loxizin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 100 mg/mL (~216.7 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.42 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1674 mL | 10.8371 mL | 21.6741 mL | |
| 5 mM | 0.4335 mL | 2.1674 mL | 4.3348 mL | |
| 10 mM | 0.2167 mL | 1.0837 mL | 2.1674 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.
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