| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Proglumide sodium targets cholecystokinin (CCK)-A and CCK-B receptors. It acts as an antagonist, blocking the effects of the neuropeptide CCK in both the central nervous system and the periphery. By inhibiting CCK's actions, it can modulate various physiological processes, including gastric acid secretion, gallbladder contraction, and neuronal excitability. Its antiepileptic activity is also attributed to its CCK antagonism.
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| ln Vitro |
Proglutamine at concentrations of 0.3–10 mM quantitatively suppressed CCK-stimulated amylase production in an in vitro investigation, but proglutamine at values of 0–3 mM had no effect on basal amylase. liberated. The dose-response curve of amylase release vs CCK moves to the right as proglutamine concentration rises. Proglumide's inhibitory action is reversible. Proglumide is additionally selective for CCK and related peptides [2]. Proglumide dosage dramatically decreased [3H]-bust daily injection into HT29 cells with an IC50 of 6.5 mM in a dose-dependent manner. Proglumide has a dose-dependent effect in reducing the overall number of questions, with a dose-dependence of up to 70% on cells [3].
In vitro, Proglumide sodium is characterized as a CCK-A/B receptor antagonist. Its ability to inhibit gastric secretion and protect the gastroduodenal mucosa has been demonstrated. It also exhibits antiepileptic and antioxidant activities in various in vitro models. Its activity is primarily measured by its ability to block CCK-induced effects in receptor binding and functional assays. |
| ln Vivo |
Proglumide treatment (250–750 mg/kg; intraperitoneal injection; adult Sprague Dawley Project) dramatically reduces brain oxidation, cognitive dysfunction, and engineering activity [1].
In vivo, Proglumide sodium selectively blocks CCK's effects in the central nervous system (CNS). It inhibits gastric secretion and protects the gastroduodenal mucosa. It has been studied for its antiepileptic activity, suggesting it can modulate neuronal excitability in vivo. Its oral activity makes it suitable for administration in animal models. |
| Enzyme Assay |
In vitro receptor binding assays for Proglumide sodium involve measuring its affinity for CCK-A and CCK-B receptors. Radioligand binding studies using ¹²⁵I-CCK or other CCK analogs are performed on membranes from tissues or cells expressing these receptors. The compound is incubated with increasing concentrations, and its Ki value is determined. Functional assays measure its ability to antagonize CCK-induced intracellular calcium mobilization or other signaling events.
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| Cell Assay |
For in vitro cell-based assays, cells expressing CCK-A or CCK-B receptors are cultured and treated with Proglumide sodium. Its antagonism is confirmed by its ability to block CCK-induced signaling, such as calcium flux or cAMP modulation. Its antioxidant activity can be assessed by measuring its ability to scavenge free radicals in cell cultures. Its effects on cell viability are measured using MTT assays.
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| Animal Protocol |
Animal/Disease Models: Adult male Sprague Dawley rats (200) -250 g; 2 months old) induced status epilepticus (SE) [1]
Doses: 250 mg/kg, 500 mg/kg and 750 mg/kg administered Methods: intraperitoneal (ip) injection Experimental Results: Dose-dependent and significant increase in latency to seizures and SE. Significant and dose-dependent attenuated Li-PC (SE)-induced increases in thiobarbituric acid (TBARS) and catalase (CAT), attenuated Li-Pc-induced decreases in SOD, and attenuated GSH and Depletion of glutathione-S transferase (GST). Hippocampus and striatum. In vivo animal studies with Proglumide sodium are conducted in models of gastric secretion, epilepsy, and pain. The compound is administered orally or intraperitoneally. Its ability to inhibit gastric acid secretion is measured in pylorus-ligated rats. Its antiepileptic activity is assessed in seizure models. Its neuroprotective effects are evaluated in models of neurodegeneration. |
| ADME/Pharmacokinetics |
Proglumide sodium (CAS: 99247-33-3) has a molecular weight of 356.40 g/mol and a molecular formula of C18H25N2NaO4. It is also known as dl-4-benzamido-N,N-dipropylglutaramic acid sodium salt. It is a white to off-white solid and is soluble in water. It is typically stored at room temperature. The compound is a nonpeptide and orally active CCK-A/B receptor antagonist.
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| Toxicity/Toxicokinetics |
Proglumide sodium has been studied in clinical trials for its potential in treating gastrointestinal disorders and epilepsy. It is generally well-tolerated. Common side effects may include gastrointestinal disturbances. It is not currently an FDA-approved drug for these indications. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptor antagonist. It selectively blocks CCK's effects in the central nervous system (CNS) and inhibits gastric secretion. It also has antiepileptic and antioxidant activities. It is not an FDA-approved drug and is intended for research use only.
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| Molecular Formula |
C18H25N2O4NA
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|---|---|
| Molecular Weight |
356.3919
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| Exact Mass |
356.171
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| CAS # |
99247-33-3
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| Related CAS # |
Proglumide;6620-60-6;Proglumide hemicalcium;85068-56-0
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| PubChem CID |
23677833
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| Appearance |
White to off-white solid powder
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| LogP |
1.538
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
25
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| Complexity |
419
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UFMWGCINVOIJSO-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C18H26N2O4.Na/c1-3-12-20(13-4-2)18(24)15(10-11-16(21)22)19-17(23)14-8-6-5-7-9-14;/h5-9,15H,3-4,10-13H2,1-2H3,(H,19,23)(H,21,22);/q;+1/p-1
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| Chemical Name |
sodium;4-benzamido-5-(dipropylamino)-5-oxopentanoate
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), 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)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~280.59 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (280.59 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8059 mL | 14.0296 mL | 28.0591 mL | |
| 5 mM | 0.5612 mL | 2.8059 mL | 5.6118 mL | |
| 10 mM | 0.2806 mL | 1.4030 mL | 2.8059 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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