| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
5-HT2B Receptor 11.2 nM (Ki) 5-HT2A Receptor 1516 nM (Ki) 5-HT2C Receptor 324 nM (Ki)
|
|---|---|
| ln Vitro |
In rats, arteries with a significant drop in threshold (the mesenteric resistance artery and the aorta) contract when exposed to (1 nM to 100 μM) with (+)-norfenfluramine[1]. Aortic contraction is induced in tissues of normotensive and hypertensive rats by (+)-Norfenfluramine (1 and 10 μM, 3 min)[1]. Rat hippocampus synaptosomes release 5-HT in a Ca2+-dependent manner when exposed to (0–10 μM)-Norfenfluramine for three minutes [2].
|
| ln Vivo |
In conscious SHAM and DOCA-salt rats, (+)-Norfenfluramine (1-300 μg/kg, iv) generates a pressor response[1]. Rat telencephalon and brainstem 5-HT and 5-HIAA levels are decreased by (+)-Norfenfluramine (2.5 and 5 mg/kg, ip)[3].
|
| Animal Protocol |
Animal/Disease Models: Conscious SHAM and DOCA-salt rats[1].
Doses: 1-300 μg/kg Route of Administration: intravenous (iv) injection (iv), given in a cumulative fashion at 6-min intervals. Experimental Results: Induced pressor response in conscious SHAM and DOCA-salt rats. (change in mean arterial blood pressure at 300 μg/kg, mm Hg, SHAM vehicle=36, SHAM ketanserin=7, DOCA=51, DOCA ketanserin=19). |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
(s)-norfenfluramine has known human metabolites that include 2-(3-(Trifluoromethyl)phenyl)ethanamine. |
| References |
|
| Additional Infomation |
(2S)-1-[3-(trifluoromethyl)phenyl]-2-propanamine is a member of amphetamines.
A FENFLURAMINE analog that inhibits serotonin uptake and may provoke release of serotonin. It is used as an appetite depressant and an experimental tool in animal studies. See also: Norfenfluramine (annotation moved to). |
| Molecular Formula |
C10H12F3N
|
|---|---|
| Molecular Weight |
203.20
|
| Exact Mass |
203.092
|
| CAS # |
19036-73-8
|
| Related CAS # |
(+)-Norfenfluramine hydrochloride;37936-89-3;Norfenfluramine;1886-26-6
|
| PubChem CID |
9815618
|
| Appearance |
Colorless to light yellow liquid
|
| Density |
1.152g/cm3
|
| Boiling Point |
215.2ºC at 760mmHg
|
| Flash Point |
88.9ºC
|
| Vapour Pressure |
0.15mmHg at 25°C
|
| Index of Refraction |
1.467
|
| LogP |
3.295
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
14
|
| Complexity |
179
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
FC(C1=CC=CC(=C1)C[C@H](C)N)(F)F
|
| InChi Key |
MLBHFBKZUPLWBD-ZETCQYMHSA-N
|
| InChi Code |
InChI=1S/C10H12F3N/c1-7(14)5-8-3-2-4-9(6-8)10(11,12)13/h2-4,6-7H,5,14H2,1H3/t7-/m0/s1
|
| Chemical Name |
(2S)-1-[3-(trifluoromethyl)phenyl]propan-2-amine
|
| 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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (492.13 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.30 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 (12.30 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 saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (12.30 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9213 mL | 24.6063 mL | 49.2126 mL | |
| 5 mM | 0.9843 mL | 4.9213 mL | 9.8425 mL | |
| 10 mM | 0.4921 mL | 2.4606 mL | 4.9213 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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