Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
Other Sizes |
|
FG 7142 (ZK 39106; LSU-65), a non-specificly benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex.
ln Vitro |
FG-7142 exhibits affinity for α subunit expression, with a Ki value of 91 nM; 330 nm; α1, α2, α3, and α5 subunits, respectively, being 492 nM and 2.150 μM[1]. When it comes to controlling GABA-induced chloride flux at GABAA receptors that express the α1 subunit energy (EC50 = 137 nM) micron), FG-7142 is much more effective than other α subunits (EC50: α2=507 nM, α3=1.021μM, and α5=1.439) [1].
|
---|---|
ln Vivo |
In rats, FG-7142 (ip; 15–30 mg/kg) increases dopamine in the nucleus accumbens and prefrontal cortex by activating mesolimbic cortical dopaminergic projections [1]. In vivo, FG-7142 (ip; 15 mg/kg) raises dopamine turnover and tyrosine hydroxylase activity in the ventral tegmentum and medial prefrontal cortex, but not in the mesolimbic or nigrostriatal regions [1].
|
References | |
Additional Infomation |
N-methyl-9H-pyrido[3,4-b]indole-3-carboxamide is a member of beta-carbolines.
|
Molecular Formula |
C13H11N3O
|
---|---|
Molecular Weight |
225.24594
|
Exact Mass |
225.09
|
Elemental Analysis |
C, 69.32; H, 4.92; N, 18.66; O, 7.10
|
CAS # |
78538-74-6
|
PubChem CID |
4375
|
Appearance |
Light yellow to yellow solid powder
|
Density |
1.328g/cm3
|
Boiling Point |
576.3ºC at 760 mmHg
|
Flash Point |
302.3ºC
|
Index of Refraction |
1.735
|
LogP |
2.466
|
Hydrogen Bond Donor Count |
2
|
Hydrogen Bond Acceptor Count |
2
|
Rotatable Bond Count |
1
|
Heavy Atom Count |
17
|
Complexity |
307
|
Defined Atom Stereocenter Count |
0
|
SMILES |
CNC(=O)C1=NC=C2C(=C1)C3=CC=CC=C3N2
|
InChi Key |
QMCOPDWHWYSJSA-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C13H11N3O/c1-14-13(17)11-6-9-8-4-2-3-5-10(8)16-12(9)7-15-11/h2-7,16H,1H3,(H,14,17)
|
Chemical Name |
N-methyl-9H-pyrido[3,4-b]indole-3-carboxamide
|
Synonyms |
FG-7142 FG 7142 FG7142
|
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)
|
Solubility (In Vitro) |
DMSO : ~100 mg/mL (~443.95 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.4395 mL | 22.1976 mL | 44.3951 mL | |
5 mM | 0.8879 mL | 4.4395 mL | 8.8790 mL | |
10 mM | 0.4440 mL | 2.2198 mL | 4.4395 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.