| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Antidepressants like amitidine (DOV 21,947) are used. SERT, NET, and DAT have Ki values of 99 nM, 262 nM, and 213 nM, respectively. Serotonin uptake, norepinephrine uptake, and dopamine uptake had IC50 values of 12, 23, and 96 nM, respectively [1].
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| ln Vivo |
Amitifa at 30 mg/kg significantly decreased the amount of nicotine that people self-administered. The first fifteen minutes saw a decrease in nicotine self-administration with the 5 mg/kg and 10 mg/kg doses. when taking the maximum recommended dosage of nicotine by mouth. A significant decrease in mean locomotor activity during the one-hour session and a reduction in food-induced responses were not observed with the 30 mg/kg dose of amitifa (but lower doses). At the start of the course, the 10 mg/kg dose resulted in hypoactivity, whereas the 5 mg/kg dose had no such effect. It was also established what happened after 15 rounds of continuous amitidine treatment (10 mg/kg). Amitidine dramatically decreased the amount of nicotine that was self-administered; this reduction persisted one week after the mandatory abstinence period and during the two weeks of continuous treatment. Self-administration of nicotine is greatly decreased by amitifatin. This has led to additional investigation into whether amitidin could be a useful smoking cessation treatment [2].
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| References |
| Molecular Formula |
C11H12CL3N
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|---|---|
| Molecular Weight |
264.5787
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| Exact Mass |
263.004
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| CAS # |
410074-74-7
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| Related CAS # |
DOV-216,303 Free Base;66504-40-3
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| PubChem CID |
11680542
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| Appearance |
White to off-white solid powder
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| LogP |
3.985
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
15
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| Complexity |
245
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| Defined Atom Stereocenter Count |
2
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| SMILES |
ClC1=C(C([H])=C([H])C(=C1[H])[C@]12C([H])([H])N([H])C([H])([H])[C@@]1([H])C2([H])[H])Cl.Cl[H]
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| InChi Key |
KAGBHVBIOJBGBD-NINOIYOQSA-N
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| InChi Code |
InChI=1S/C11H11Cl2N.ClH/c12-9-2-1-7(3-10(9)13)11-4-8(11)5-14-6-11;/h1-3,8,14H,4-6H2;1H/t8-,11+;/m1./s1
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| Chemical Name |
(1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane;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 (~377.96 mM)
H2O : ~50 mg/mL (~188.98 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (10.39 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 27.5 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: ≥ 2.75 mg/mL (10.39 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 27.5 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: ≥ 2.75 mg/mL (10.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (37.80 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7796 mL | 18.8979 mL | 37.7958 mL | |
| 5 mM | 0.7559 mL | 3.7796 mL | 7.5592 mL | |
| 10 mM | 0.3780 mL | 1.8898 mL | 3.7796 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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