| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
IC50: 71 nM (dopamine uptake)[1]
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|---|---|
| ln Vivo |
AHN 1-055 (5 mg/kg; intravenous administration) inhibits the absorption of dopamine in the brain, with an in vivo IC50 of 311.8 ng/ml[1]. Because of its 18.7 L/kg volume of distribution and 1.8 L/h/kg plasma clearance, AHN 1-055 (10 mg/kg; i.v.) has a terminal elimination half-life of 7.69 hours and a Cmax of 1.48 mg/L[1].
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| Animal Protocol |
Animal/Disease Models: Adult male Sprague Dawley rats (250-275 g)[1]
Doses: 5 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Iv administration Experimental Results: Cmax (1.48 mg/L); T1/2 (7.69 h). |
| References |
[1]. Sangeeta R, et, al. Investigation of the potential pharmacokinetic and pharmaco-dynamic drug interaction between AHN 1-055, a potent benztropine analog used for cocaine abuse, and cocaine after dosing in rats using intracerebral microdialysis. Biopharm Drug Dispos. 2006 Jul; 27(5): 229-40.
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| Molecular Formula |
C21H24CLF2NO
|
|---|---|
| Molecular Weight |
379.87
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| Exact Mass |
379.151
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| CAS # |
202646-03-5
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| PubChem CID |
24978533
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
396
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| Defined Atom Stereocenter Count |
2
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| SMILES |
Cl.FC1=CC=C(C(C2=CC=C(F)C=C2)OC2CC3CCC(N3C)C2)C=C1
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| InChi Key |
YOORVSGDAHWVMC-IIPFOPBBSA-N
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| InChi Code |
InChI=1S/C21H23F2NO.ClH/c1-24-18-10-11-19(24)13-20(12-18)25-21(14-2-6-16(22)7-3-14)15-4-8-17(23)9-5-15;/h2-9,18-21H,10-13H2,1H3;1H/t18-,19+,20?;
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| Chemical Name |
(1R,5S)-3-[bis(4-fluorophenyl)methoxy]-8-methyl-8-azabicyclo[3.2.1]octane;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO: 100 mg/mL (263.25 mM)
H2O: 33.33 mg/mL (87.74 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.48 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 (5.48 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 (5.48 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 | 2.6325 mL | 13.1624 mL | 26.3248 mL | |
| 5 mM | 0.5265 mL | 2.6325 mL | 5.2650 mL | |
| 10 mM | 0.2632 mL | 1.3162 mL | 2.6325 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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