| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vivo |
An agonist of the gamma-aminobutyric acid receptor (GABA) is progabide. When Progabide was injected intraperitoneally at 50, 100, and 200 mg/kg, the corresponding increases in plasma corticosterone levels were 244, 365, and 476% (t=6.44 to 12.55, p<0.01). The dose of progabide (10 mg/kg) had no effect on plasma corticosterone levels (t=0.76, NS). Increases in plasma corticosterone levels at 30 minutes (t=2.625, p<0.05), 60 minutes (t=13.13, p<0.001), and 120 minutes (t=4.07, p<0.01) were significantly produced by 200 mg/kg Progabide. pharmacological injection, but 240 minutes later (t=0.86, NS), the values went back to control. Progabide is administered for 60 minutes to achieve the maximum corticosterone rise (in comparison to matched controls) [1].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Well absorbed with a bioavailability of 60% Metabolism / Metabolites Hepatic Biological Half-Life 4 hours |
| Toxicity/Toxicokinetics |
Protein Binding
95% |
| References | |
| Additional Infomation |
Progabide is a diarylmethane.
Progabide is an analog and prodrug of gamma-aminobutyric acid. It is commonly used in the treatment of epilepsy. It has agonistic activity for both the GABAA and GABAB receptors. In clinical trials, progabide has been investigated for Parkinson's disease, schizophrenia, clinical depression and anxiety disorder; its therapeutic effectiveness in these conditions is not fully elucidated. Drug Indication Indicated for the treatment of epilepsy. Mechanism of Action Progabide binds to both GABAA and GABAB receptors located on the terminals of primary afferent fibers. Binding to GABAA results in an increased affinity of the GABA receptor for the amino acid, an augmented flux of chloride ions across the terminal membrane, and an increase in the amount of presynaptic inhibition. Activation of the GABAB receptors retards the influx of calcium ions into the terminals, thereby reducing the evoked release of excitatory amino acids and possibly other transmitters. Pharmacodynamics Progabide, a fatty acid derivative, is a GABA receptor agonist used to treat the symptoms of epilepsy. |
| Molecular Formula |
C17H16CLFN2O2
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|---|---|
| Molecular Weight |
334.77
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| Exact Mass |
334.088
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| CAS # |
62666-20-0
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| PubChem CID |
44115
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3g/cm3
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| Boiling Point |
525.363ºC at 760 mmHg
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| Melting Point |
133-135°; mp 142.5° (Kaplan, J. Med. Chem.)
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| Flash Point |
271.53ºC
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| Index of Refraction |
1.59
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| LogP |
3.987
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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 |
6
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| Heavy Atom Count |
23
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| Complexity |
425
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IBALRBWGSVJPAP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H16ClFN2O2/c18-12-5-3-11(4-6-12)17(21-9-1-2-16(20)23)14-10-13(19)7-8-15(14)22/h3-8,10,22H,1-2,9H2,(H2,20,23)
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| Chemical Name |
4-[[(4-chlorophenyl)-(5-fluoro-2-hydroxyphenyl)methylidene]amino]butanamide
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| Synonyms |
Gabrene; Halogabide; Progabide
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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 : ~250 mg/mL (~746.78 mM)
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|---|---|
| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9871 mL | 14.9356 mL | 29.8713 mL | |
| 5 mM | 0.5974 mL | 2.9871 mL | 5.9743 mL | |
| 10 mM | 0.2987 mL | 1.4936 mL | 2.9871 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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