2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Picamilon

Picamilon  (Synonyms: Nicotinoyl-GABA; Nicotinoyl-γ-aminobutyric acid)

Cat. No.: HY-107482 Purity: 98.25%
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Picamilon is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats.

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Picamilon Chemical Structure

Picamilon Chemical Structure

CAS No. : 34562-97-5

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Description

Picamilon is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats[1][2][3].

In Vivo

Picamilon (PM) (20 or 50 mg/kg; i.p.) significantly decreases the frequency and duration of seizure spike-wave discharges (SWDs) in Picrotoxin (HY-101391)-induced convulsive activity in rats[2].
Picamilon (250 mg/kg; p.o.) inhibits NLRP3 inflammasome activation in pancreatic cells during Alloxan (HY-W017227) -induced diabetes mellitus rats model[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Picrotoxin (HY-101391)-induced epilepsy model in rats [2]
Dosage: 20 or 50 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Significantly decreased the frequency and duration of seizure spike-wave discharges (SWDs) in doses of 50 mg/kg.
Decreased the intensity of SWDs in smaller doses (20 mg/kg).
Animal Model: Alloxan (HY-W017227)-induced diabetes mellitus model in rats [3]
Dosage: 250 mg/ kg
Administration: Oral gavage (p.o.)
Result: Suppressed NLRP3 activity, as indicated by a significant decrease in the area of immunopositive pancreatocytes to (21,30 ± 5,44) and (39,31 ± 5,24) %, respectively, relative to the value in the group of animals that were not treated (75,19±7,69%).
Promoted correction of functional disorders of the pancreas during alloxan-induced diabetes mellitus by inhibiting activation of NLRP3 inflammasome in pancreatocytes.
Molecular Weight

208.21

Formula

C10H12N2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(CCCNC(C1=CN=CC=C1)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (300.18 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.8028 mL 24.0142 mL 48.0284 mL
5 mM 0.9606 mL 4.8028 mL 9.6057 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.8028 mL 24.0142 mL 48.0284 mL 120.0711 mL
5 mM 0.9606 mL 4.8028 mL 9.6057 mL 24.0142 mL
10 mM 0.4803 mL 2.4014 mL 4.8028 mL 12.0071 mL
15 mM 0.3202 mL 1.6009 mL 3.2019 mL 8.0047 mL
20 mM 0.2401 mL 1.2007 mL 2.4014 mL 6.0036 mL
25 mM 0.1921 mL 0.9606 mL 1.9211 mL 4.8028 mL
30 mM 0.1601 mL 0.8005 mL 1.6009 mL 4.0024 mL
40 mM 0.1201 mL 0.6004 mL 1.2007 mL 3.0018 mL
50 mM 0.0961 mL 0.4803 mL 0.9606 mL 2.4014 mL
60 mM 0.0800 mL 0.4002 mL 0.8005 mL 2.0012 mL
80 mM 0.0600 mL 0.3002 mL 0.6004 mL 1.5009 mL
100 mM 0.0480 mL 0.2401 mL 0.4803 mL 1.2007 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Picamilon34562-97-5Nicotinoyl-GABA Nicotinoyl-γ-aminobutyric acidGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorseizure spike-wave dischargesseizureratdiabetes mellitusInhibitorinhibitorinhibit

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