| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| ln Vitro |
Proglumide at concentrations between 0.3 and 10 mM decreased CCK-stimulated amylase release in an in vitro investigation; at concentrations between 0 and 3 mM, proglumide had no effect on baseline amylase release. The dose-response curve of CCK produced by amylase moves to the right as the concentration of proglumide rises. Proglumide's inhibitory action is reversible. Proglumide also has a selective impact on CCK and related peptides [2]. With an IC50 of 6.5 mM, proglumide treatment of HT29 cells dramatically decreased the incorporation of [3H]-thymidine into HT29 cells in a dose-dependent manner. Proglumide increases apoptosis by up to 70% while decreasing the percentage of necrosis in a dose-dependent manner [3].
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| ln Vivo |
Proglumide (250-750 mg/kg; intraperitoneal injection; adult male Sprague-Dawley rats) is an effective treatment that greatly reduces brain oxidative stress, cognitive impairment, and seizure activity [1].
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| Animal Protocol |
Animal/Disease Models: Induction of status epilepticus (SE) in adult male Sprague Dawley rats (200-250 g; 2 months old) [1]
Doses: 250 mg/kg, 500 mg/kg, and 750 mg/kg Route of Administration: Results of intraperitoneal (ip) injection: dose-dependent and significant increase in seizure and SE latency. 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. |
| References |
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| Additional Infomation |
Proglumide is a racemate composed of equal amounts of (R)- and (S)-proglumide. A non-selective CCK antagonist that was used primarily for treatment of stomach ulcers, but has been replaced by newer drugs. It has a role as a drug metabolite, a xenobiotic metabolite, a cholinergic antagonist, an anti-ulcer drug, a cholecystokinin antagonist, a gastrointestinal drug, a delta-opioid receptor agonist and an opioid analgesic. It contains a (R)-proglumide and a (S)-proglumide.
Proglumide is an orally bioavailable cholecystokinin (CCK) receptor antagonist, with gastric acid reducing and potential antineoplastic activities. Upon oral administration, proglumide binds to and blocks both cholecystokinin receptor type A (CCK-AR; CCK1-R) and gastrin/cholecystokinin type B receptor (CCK-BR; CCK2-R). This prevents the binding of cholecystokinin and gastrin to the CCK receptors, and inhibits both gastrointestinal (GI) motility and gastric secretions. This may also decrease fibrosis in the tumor microenvironment (TME), increase both the infiltration of T-cells and the penetration of chemotherapeutic agents, and inhibit tumor growth and metastasis. CCK receptors, normally expressed in the GI tract and the nervous system, are overexpressed on fibroblasts and certain cancers. A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers. |
| Exact Mass |
334.189
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|---|---|
| CAS # |
6620-60-6
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| Related CAS # |
Proglumide sodium;99247-33-3;Proglumide hemicalcium;85068-56-0
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| PubChem CID |
4922
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
589.8±45.0 °C at 760 mmHg
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| Melting Point |
148.5--152ºC
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| Flash Point |
310.5±28.7 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.534
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| LogP |
2.53
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
24
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| Complexity |
413
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(O)CCC(NC(C1=CC=CC=C1)=O)C(N(CCC)CCC)=O
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| InChi Key |
DGMKFQYCZXERLX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H26N2O4/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)
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| Chemical Name |
4-benzamido-5-(dipropylamino)-5-oxopentanoic acid
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| Synonyms |
Proglumide W-5219 W 5219W5219
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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 : ≥ 65 mg/mL (~194.37 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (6.49 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 21.7 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: ≥ 2.17 mg/mL (6.49 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 21.7 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. View More
Solubility in Formulation 3: ≥ 2.17 mg/mL (6.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04814602 | COMPLETED | Drug: Proglumide | Cirrhosis, Liver | Georgetown University | 2021-03-30 | Early Phase 1 |
| NCT04152473 | COMPLETED | Drug: Proglumide | Nonalcoholic Steatohepatitis | Georgetown University | 2019-12-13 | Phase 1 |
| NCT05551858 | ACTIVE, NOT RECRUITING | Drug: Proglumide Drug: Placebo |
Pain Pancreas Fibrosis Safety Issues |
Georgetown University | 2022-11-17 | Phase 1 Phase 2 |
| NCT05827055 | RECRUITING | Drug: Gemcitabine Drug: Nab paclitaxel Drug: Proglumide Drug: Placebo |
Metastatic Pancreatic Cancer | Georgetown University | 2024-01-31 | Phase 2 |
| NCT06017323 | WITHDRAWN | Drug: Gemcitabine Drug: Nab paclitaxel Drug: Proglumide Dose level 1 Drug: Proglumide Dose level 2 |
Metastatic Pancreatic Cancer | Georgetown University | 2023-10 | Phase 1 |
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