Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
Other Sizes |
|
Purity: ≥98%
Sofiniclin (formerly also known as ABT-894 and A-422894) is a novel and potent agonist of nicotinic acetylcholine receptor (nAChR) which is used as a potential non-stimulant treatment for attention-deficit/hyperactivity disorder (ADHD). Sofinicline is under development for the treatment of attention-deficit/hyperactivity disorder. Sofinicline appears to be well tolerated and showing efficacy similar to that of atomoxetine.
ln Vitro |
With Ki values of 1.3 nM for 125I-epibatidine binding and 1.9 nM for 125I-α-conotoxinMII binding, sofiniclin is more potent than ABT-089 at both receptor subtypes[1].
|
---|---|
ln Vivo |
Compared to a vehicle monkey, sofiniclin (0.001 to 0.10 mg/kg, po) significantly lowers LIDs[1]. Monkeys with extensive nigrostriatal injury do not have a reduction in LIDs when given sofiniclin (0.1 mg/kg)[2].
|
References |
[1]. Zhang D, et al. ABT-089 and ABT-894 reduce levodopa-induced dyskinesias in a monkey model of Parkinson's disease. Mov Disord. 2014 Apr;29(4):508-17.
[2]. Zhang D, ET AL. α7 nicotinic receptor agonists reduce levodopa-induced dyskinesias with severe nigrostriatal damage. Mov Disord. 2015 Dec;30(14):1901-11 |
Molecular Formula |
C10H11N3CL2
|
---|---|
Molecular Weight |
244.12044
|
Exact Mass |
243.03
|
Elemental Analysis |
C, 49.20; H, 4.54; Cl, 29.04; N, 17.21
|
CAS # |
799279-80-4
|
Related CAS # |
799279-87-1;799279-85-9 (tartrate);869792-84-7 (acetate);869792-87-0 (mesylate); 869792-90-5 (HCl); 799279-80-4; 876170-44-4 (besylate);
|
Appearance |
Solid powder
|
SMILES |
ClC1=C(Cl)C=C(N2C[C@]3([H])CN[C@]3([H])C2)C=N1
|
InChi Key |
MBQYQLWSBRANKQ-IMTBSYHQSA-N
|
InChi Code |
InChI=1S/C10H11Cl2N3/c11-8-1-7(3-14-10(8)12)15-4-6-2-13-9(6)5-15/h1,3,6,9,13H,2,4-5H2/t6-,9+/m0/s1
|
Chemical Name |
(1S,5S)-3-(5,6-dichloropyridin-3-yl)-3,6-diazabicyclo[3.2.0]heptane
|
Synonyms |
Sofinicline; ABT-894; A-422894.0; ABT 894; A-422894; ABT894; A 422894.0
|
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 : ~35.71 mg/mL (~146.28 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.52 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 20.8 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: ≥ 2.08 mg/mL (8.52 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 20.8 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: ≥ 2.08 mg/mL (8.52 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 | 4.0963 mL | 20.4817 mL | 40.9635 mL | |
5 mM | 0.8193 mL | 4.0963 mL | 8.1927 mL | |
10 mM | 0.4096 mL | 2.0482 mL | 4.0963 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.