Physicochemical Properties
| Molecular Formula | C36H50CAN4O8 |
| Molecular Weight | 706.882209300995 |
| Exact Mass | 706.325 |
| CAS # | 85068-56-0 |
| Related CAS # | Proglumide sodium;99247-33-3;Proglumide;6620-60-6 |
| PubChem CID | 44144966 |
| Appearance | Typically exists as solid at room temperature |
| LogP | 4.284 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 8 |
| Rotatable Bond Count | 18 |
| Heavy Atom Count | 49 |
| Complexity | 408 |
| Defined Atom Stereocenter Count | 0 |
| SMILES | [Ca+2].O=C(C(CCC(=O)O)NC(C1C=CC=CC=1)=O)N(CCC)CCC.O=C(C(CCC(=O)[O-])/N=C(/C1C=CC=CC=1)\[O-])N(CCC)CCC |
| InChi Key | CKVJNBJBVWVPGO-UHFFFAOYSA-L |
| InChi Code | InChI=1S/2C18H26N2O4.Ca/c2*1-3-12-20(13-4-2)18(24)15(10-11-16(21)22)19-17(23)14-8-6-5-7-9-14;/h2*5-9,15H,3-4,10-13H2,1-2H3,(H,19,23)(H,21,22);/q;;+2/p-2 |
| Chemical Name | calcium;4-benzamido-5-(dipropylamino)-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 |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| 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]. |
| 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]. |
| 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 |
[1]. The effects of quinacrine, proglumide, and pentoxifylline on seizure activity, cognitive deficit, and oxidative stress in rat lithium-pilocarpine model of status epilepticus. Oxid Med Cell Longev. 2014;2014:630509. [2]. In vitro and in vivo effect of proglumide on cholecystokinin-stimulated amylase release in mouse pancreatic acini. Gastroenterol Jpn. 1984 Feb;19(1):53-8. [3]. Selective CCK-A but not CCK-B receptor antagonists inhibit HT-29 cell proliferation: synergism with pharmacological levels of melatonin. J Pineal Res. 2005 Oct;39(3):243-50. [4]. Further studies on the specificity of proglumide as a selective cholecystokinin antagonist in the central nervous system. Ann N Y Acad Sci. 1985;448:345-51. [5]. Gastric and duodenal antiulcer and cytoprotective effects of proglumide in rats. J Pharmacol Exp Ther. 1987 May;241(2):602-7. |
Solubility Data
| Solubility (In Vitro) | May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples |
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4147 mL | 7.0733 mL | 14.1467 mL | |
| 5 mM | 0.2829 mL | 1.4147 mL | 2.8293 mL | |
| 10 mM | 0.1415 mL | 0.7073 mL | 1.4147 mL |