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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
References |
1: Vogt BA. Cingulate impairments in ADHD: Comorbidities, connections, and treatment. Handb Clin Neurol. 2019;166:297-314. doi: 10.1016/B978-0-444-64196-0.00016-9. PMID: 31731917. 2: Zimmerman CN, Eskow Jaunarajs KL, Meringolo M, Rizzo FR, Santoro M, Standaert DG, Pisani A. Evaluation of AZD1446 as a Therapeutic in DYT1 Dystonia. Front Syst Neurosci. 2017 Jun 13;11:43. doi: 10.3389/fnsys.2017.00043. PMID: 28659770; PMCID: PMC5468415. 3: Buoli M, Serati M, Cahn W. Alternative pharmacological strategies for adult ADHD treatment: a systematic review. Expert Rev Neurother. 2016;16(2):131-44. doi: 10.1586/14737175.2016.1135735. Epub 2016 Jan 14. PMID: 26693882. 4: Boström E, Bohnstedt KC, Jostell KG, Alverlind S, Huledal G, Paulsson B, Hårdemark HG, Öhd J, Lindholm S. Population pharmacokinetics and safety of AZD1446, a neuronal nicotinic receptor agonist, administered in healthy volunteers. Clin Pharmacol Drug Dev. 2014 Jan;3(1):63-71. doi: 10.1002/cpdd.59. Epub 2013 Sep 9. PMID: 27128232. 5: Jucaite A, Öhd J, Potter AS, Jaeger J, Karlsson P, Hannesdottir K, Boström E, Newhouse PA, Paulsson B. A randomized, double-blind, placebo-controlled crossover study of α4β 2* nicotinic acetylcholine receptor agonist AZD1446 (TC-6683) in adults with attention-deficit/hyperactivity disorder. Psychopharmacology (Berl). 2014 Mar;231(6):1251-65. doi: 10.1007/s00213-013-3116-7. Epub 2013 May 3. PMID: 23640072; PMCID: PMC3838503. 6: Mazurov AA, Miao L, Bhatti BS, Strachan JP, Akireddy S, Murthy S, Kombo D, Xiao YD, Hammond P, Zhang J, Hauser TA, Jordan KG, Miller CH, Speake JD, Gatto GJ, Yohannes D. Discovery of 3-(5-chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane (TC-6683, AZD1446), a novel highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders. J Med Chem. 2012 Nov 8;55(21):9181-94. doi: 10.1021/jm3006542. Epub 2012 Jul 27. PMID: 22793665.
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Molecular Formula |
C18H21CLN2O5S
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Molecular Weight |
412.885
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Exact Mass |
0
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Elemental Analysis |
C, 52.36; H, 5.13; Cl, 8.59; N, 6.78; O, 19.37; S, 7.76
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CAS # |
1392330-84-5
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Related CAS # |
1025007-04-8;1788894-06-3 (HCl);1392330-84-5;1025007-65-1 (TFA);
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Appearance |
Solid powder
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SMILES |
O=C(N1CC2CNCC2C1)C3=CC=C(Cl)O3.OS(=O)(C4=CC=C(C)C=C4)=O
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InChi Key |
GWTRGLDVMRLRSS-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C11H13ClN2O2.C7H8O3S/c12-10-2-1-9(16-10)11(15)14-5-7-3-13-4-8(7)6-14;1-6-2-4-7(5-3-6)11(8,9)10/h1-2,7-8,13H,3-6H2;2-5H,1H3,(H,8,9,10)
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Chemical Name |
3-(5-Chloro-2-furoyl)-3,7-diazabicyclo(3.3.0)octane tosylate
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Synonyms |
AZD1446 tosylate; AZD 1446, AZD-1446, AZD1446, TC 6683, TC-6683, TC6683
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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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.4220 mL | 12.1098 mL | 24.2195 mL | |
5 mM | 0.4844 mL | 2.4220 mL | 4.8439 mL | |
10 mM | 0.2422 mL | 1.2110 mL | 2.4220 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.