| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
γ-aminobutyric acid/GABA derivative; GABA prodrug
Nicotinoyl-GABA is a prodrug that targets the central nervous system through delivery of its two active components: GABA (gamma-aminobutyric acid) and nicotinic acid (niacin). GABA is the primary inhibitory neurotransmitter in the brain, and its receptor activation produces anxiolytic and sedative effects. Nicotinic acid is a vitamin that acts as a vasodilator and has effects on lipid metabolism. By combining these two molecules, Nicotinoyl-GABA can deliver GABA to the brain more effectively than GABA itself, which cannot cross the blood-brain barrier. The compound's nootropic properties are attributed to the combined effects of GABA and nicotinic acid in the brain. |
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| ln Vitro |
Nicotinoyl-GABA is an antioxidant agent in neuroprotection treatment. It can improve rat epilepsy models and promote the correction of pancreatic dysfunction in Alloxan induced rat diabetes models. The compound's antioxidant properties contribute to its neuroprotective effects. As a GABA analogue, it may modulate neuronal excitability through GABA receptor activation. The nicotinic acid component provides vasodilatory effects that may improve cerebral blood flow. The combined effects of these two active components contribute to the compound's nootropic and neuroprotective activities.
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| ln Vivo |
Picamilon (PM) intraperitoneally (20 or 50 mg/kg) Picamilon (20 or 50 mg/kg; intraperitoneally) In constructed models of Picrotoxin-induced time, picamilon greatly lowers both the frequency and duration of spike wave discharges (SWD)[2]. Oral Picamilon (250 mg/kg)
Nicotinoyl-GABA improves rat epilepsy models and promotes the correction of pancreatic dysfunction in Alloxan induced rat diabetes models. This demonstrates the compound's potential for treating neurological and metabolic disorders. As an orally bioactive compound, it can be administered conveniently. Its ability to cross the blood-brain barrier allows it to exert central effects. The compound's anxiolytic and vasodilatory properties suggest additional therapeutic applications for anxiety disorders and cardiovascular conditions. |
| Enzyme Assay |
No specific non-cell assay protocol is available for Nicotinoyl-GABA. As a prodrug, its hydrolysis to GABA and nicotinic acid can be studied in vitro using plasma or tissue homogenates. The rate of hydrolysis can be measured by HPLC or LC-MS to determine the conversion kinetics. Receptor binding assays for GABA receptors or nicotinic acid targets could be used to assess the activity of the hydrolyzed products. However, these would measure the activity of the metabolites rather than the parent compound itself.
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| Cell Assay |
No specific cell-based assay protocol is available for Nicotinoyl-GABA. For neuroprotection studies, neuronal cell lines or primary neurons are treated with Nicotinoyl-GABA followed by exposure to oxidative stress or excitotoxic insults. Cell viability, ROS production, and markers of apoptosis are measured. GABA receptor activation can be assessed by measuring intracellular calcium levels or electrophysiological recordings in GABA receptor-expressing cells. The compound's antioxidant activity can be evaluated by measuring cellular oxidative stress markers.
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| Animal Protocol |
Animal/Disease Models: Alloxan-induced rat diabetes model [3]
Doses: 250 mg/ kg Route of Administration: po (oral gavage) Experimental Results: Inhibition of NLRP3 activity, immunopositive pancreatic cell area Dramatically diminished to (21,30 ± compared to the value in the untreated animal group (75,19±7,69% ), respectively (5,44) and (39,31±5,24)%. Promote the correction of pancreatic dysfunction during alloxan-induced diabetes by inhibiting the activation of NLRP3 inflammasome in pancreatic cells. No specific animal protocol is available for Nicotinoyl-GABA. For epilepsy studies, standard models such as pentylenetetrazole (PTZ)-induced seizures or kindling models are used. The compound is administered orally, and seizure parameters (latency, duration, severity) are recorded. For diabetes studies, Alloxan-induced diabetic rats are treated with Nicotinoyl-GABA, and blood glucose, insulin levels, and pancreatic function are assessed. Behavioral tests may also be performed to evaluate anxiolytic and cognitive effects. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for Nicotinoyl-GABA. The compound has a molecular weight of 208.21 and formula C10H12N2O3. It is soluble in DMSO at 33 mg/mL (158.49 mM). As a prodrug, it is hydrolyzed into GABA and nicotinic acid. The compound is orally bioactive and can cross the blood-brain barrier, indicating favorable absorption and distribution properties. Comprehensive pharmacokinetic studies would be required to determine absorption, distribution, metabolism, and excretion parameters.
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| Toxicity/Toxicokinetics |
No detailed toxicology data is publicly available for Nicotinoyl-GABA. As a dietary supplement ingredient, it has been used in various formulations with a generally favorable safety profile. However, comprehensive toxicological evaluation would be required for therapeutic development. The compound's metabolism to GABA and nicotinic acid suggests that its safety profile would be related to the effects of these metabolites. High doses of nicotinic acid can cause flushing and other side effects, which should be considered in safety assessments. The compound is for research use only.
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| References |
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| Additional Infomation |
Pikamilon has been shown to increase blood flow to the cerebral cortex of conscious rats and rabbits. Increased blood flow was observed with intravenous, intraperitoneal and systemic administration. Topical application of pycamilone significantly dilates pial arterioles. Dilation mainly occurs in arterioles with an initial diameter of 10-20 micrometers. The dilating effect of pycamilone decreases with increasing diameter of pial arterioles. [1]
In rats, seizures were induced by repeated injections of Pikamilon (PTX) (intraperitoneal injection every 30 minutes, with an initial dose of 0.9 mg/kg and subsequent doses of 0.7 mg/kg). Pikamilon (PM) and isopiamilone (IPM) were administered intraperitoneally 30 minutes before PTX injection. Following pre-administrative injection of PM and IPM, epileptiform activity (EFA) recorded from brain structures was classified into two types: one type showed only spike-and-slow-wave discharges (SWD) (61.3%), and the other type showed regular cortical spike-and-wave activity accompanied by transient SWD (38.7%). In the first type of EFA rats, the frequency and duration of SWD were significantly reduced after injection of PM and IPM at a dose of 50 mg/kg. In the second type of EFA rats, even injection of smaller doses (20 mg/kg) of the drugs reduced the intensity of SWD. IPM was more effective as a protective anticonvulsant. [2] Nicotinoyl-GABA is also known as Picamilon, Nicotinoyl-γ-aminobutyric acid, and 4-(nicotinamido)butanoic acid. It has the molecular formula C10H12N2O3 and molecular weight 208.21. The IUPAC name is 4-(nicotinamido)butanoic acid. The compound has an MDL number of MFCD00186518. It appears as a solid powder and is soluble in DMSO. No drug development or clinical trial status applies to the pure compound; it is used as a dietary supplement ingredient and research tool. |
| Molecular Formula |
C10H12N2O3
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|---|---|
| Molecular Weight |
208.217
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| Exact Mass |
208.084
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| Elemental Analysis |
C, 64.75; H, 6.99; N, 3.60; O, 16.43; S, 8.23
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| CAS # |
34562-97-5
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| PubChem CID |
60608
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
522.4±30.0 °C at 760 mmHg
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| Melting Point |
210-212ºC
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| Flash Point |
269.8±24.6 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.552
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| LogP |
0.02
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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 |
5
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| Heavy Atom Count |
15
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| Complexity |
231
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NAJVRARAUNYNDX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H12N2O3/c13-9(14)4-2-6-12-10(15)8-3-1-5-11-7-8/h1,3,5,7H,2,4,6H2,(H,12,15)(H,13,14)
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| Chemical Name |
4-(pyridine-3-carbonylamino)butanoic acid
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| Synonyms |
Nicotinoyl GABA; Nicotinoyl GABA; 34562-97-5; 4-(Nicotinamido)butanoic acid; Pikamilone; Picamilon; Nicotinoyl-GABA; Pikamilon; N-(3-Carboxypropyl)nicotinamide; Butanoic acid, 4-[(3-pyridinylcarbonyl)amino]-;Nicotinoyl-GABA
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~62.5 mg/mL (~300.18 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 | 4.8026 mL | 24.0131 mL | 48.0261 mL | |
| 5 mM | 0.9605 mL | 4.8026 mL | 9.6052 mL | |
| 10 mM | 0.4803 mL | 2.4013 mL | 4.8026 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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