| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| Other Sizes |
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| Targets |
γ-aminobutyric acid/GABA derivative; GABA prodrug
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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)
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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. |
| References |
|
| Additional Infomation |
Pikamilon was shown to increase blood supply in cerebral cortex in conscious rats and rabbits. The increase in blood flow has been revealed under intravenous, intraperitoneal and systemic administration of the drug. There is a pronounced dilatation of pial arterioles under pikamilon action while applied locally. Most dilation occurs in arterioles with the initial diameter of 10-20 microns. With the increase of pial arterioles diameter, dilatory effect of pikamilon, is reduced.[1]
Seizures were induced in rats using repetitive injections of picrotoxin, PTX (i.p., every 30 min in a dose of 0.9 mg/kg in the first injection and 0.7 mg/kg in subsequent injections). Picamilon (PM) and isopicamilon (IPM) in doses of 20 or 50 mg/kg were i.p. injected into animals 30 min prior to injection of PTX. Epileptiform activity (EFA), recorded from the cerebral structures under conditions of preliminary systemic injections of PM and IPM, could be divided into two types characterized by exclusive development of only spike-wave discharges, SWDs (61.3 %) and regular cortical spike activity with generation of separate short-lasting SWDs (38.7%). In rats with EFA of the first type, the frequency and duration of seizure SWDs decreased significantly after injections of PM and IPM in doses of 50 mg/kg. In rats with EFA of the second type, the intensity of SWDs decreased even after injections of these agents in smaller doses (20 mg/kg). The use of IPM as an agent with a protective anticonvulsive action was more effective.[2] |
| Molecular Formula |
C10H12N2O3
|
|---|---|
| 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
|
| Index of Refraction |
1.552
|
| LogP |
0.02
|
| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
|
| Heavy Atom Count |
15
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| Complexity |
231
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
NAJVRARAUNYNDX-UHFFFAOYSA-N
|
| 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)
|
| Chemical Name |
4-(pyridine-3-carbonylamino)butanoic acid
|
| 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
|
| 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)
|
| 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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