| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
(S)-UFR2709 hydrochloride targets nicotinic acetylcholine receptors (nAChRs). It is a competitive antagonist that displays strong affinity for the α4β2 nAChR, with higher affinity for this receptor compared to the α7 nAChR. By inhibiting these receptors, it modulates cholinergic neurotransmission.
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| ln Vitro |
One biological target for the treatment of alcohol misuse and dependence is the brain's nicotinic acetylcholine receptors (nAChRs), a diverse family of pentameric acetylcholine-gated cation channels[1].
In vitro, (S)-UFR2709 hydrochloride acts as a competitive nAChR antagonist. It shows selectivity for the α4β2 nAChR over the α7 nAChR. Its activity is typically measured using receptor binding studies and functional assays on cells expressing these receptor subtypes to determine its affinity and potency as an antagonist. |
| ln Vivo |
UFR2709 significantly and dose-dependently reduces bottom dwelling time to 52.9 and 87.0 s, respectively, at 50 and 100 μg/ml. (S)-UFR2709 (hydrochloride) (50-100 μg/ml; 3 min and then maintained for another 5 min in a holding tank before testing the swimming behavior in the test tank for a period of 5 min[2]). (S)-UFR2709 (hydrochloride) (50-100 μg/ml) reduces the α4 nACh receptor subunit's nicotine-evoked mRNA expression, although UFR2709 has less of an impact on the subunit in the adult zebrafish brain[2]. In a dose-dependent manner, intraperitoneal injection of (S)-UFR2709 (hydrochloride; 1- 10 mg/kg; daily; 17 days) increases water consumption while decreasing ethanol consumption and preference. UFR2709's most potent dosage is 2.5 mg/kg, which results in a 56% decrease in alcohol intake. (S)-UFR2709 (hydrochloride) has no effect on the rats' body weight or level of locomotor activity[1].
In vivo, (S)-UFR2709 hydrochloride decreases anxiety and reduces ethanol consumption and preference in alcohol-preferring rats. It also shows potential for studying nicotine addiction. These effects are attributed to its antagonism of nAChRs and subsequent modulation of cholinergic and dopaminergic systems involved in reward and anxiety. |
| Enzyme Assay |
Non-cell-based assays for (S)-UFR2709 hydrochloride involve radioligand binding studies. Membrane preparations from cells expressing α4β2 or α7 nAChRs are incubated with a radiolabeled ligand and various concentrations of the compound. The displacement of the ligand is measured to determine its binding affinity (Ki) and selectivity for the different subtypes.
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| Cell Assay |
For in vitro cellular assays, cell lines expressing α4β2 or α7 nAChRs are used. The compound's antagonist activity is assessed by measuring its ability to inhibit agonist (e.g., nicotine)-induced responses. This is typically done by measuring calcium influx or using electrophysiological techniques. The IC50 values for receptor inhibition are determined from these experiments.
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| Animal Protocol |
Animal/Disease Models: High-alcohol-drinking UChB rats[1]
Doses: 10 mg/kg, 5 mg/kg, 2.5 mg/ kg, or 1 mg/kg Route of Administration: intraperitoneal (ip) injection; 1-10 mg/kg; daily; 17 days Experimental Results: Did not affect the weight or locomotor activity and decreased ethanol consumption and preference. In vivo animal studies for (S)-UFR2709 hydrochloride involve administering the compound to rodents, such as alcohol-preferring rats. Its effects on anxiety-like behavior (e.g., elevated plus maze) and ethanol consumption are then measured. This helps to establish its potential as a therapeutic agent for addiction and anxiety disorders. |
| ADME/Pharmacokinetics |
(S)-UFR2709 hydrochloride has a molecular formula of C13H18ClNO2. Its CAS number is 2934318-93-9. It is a research compound and should be stored according to the manufacturer's instructions. It is intended for research use only and should be handled with appropriate safety precautions.
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| Toxicity/Toxicokinetics |
The toxicity profile of (S)-UFR2709 hydrochloride is not extensively detailed. As a research compound, comprehensive toxicological data are not typically available. Its anxiolytic and anti-addictive effects are being studied, but its safety profile for human use is not established. It is not for human consumption.
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| References | |
| Additional Infomation |
(S)-UFR2709 hydrochloride (CAS#: 2934318-93-9) is a selective nAChR antagonist with potential therapeutic applications in treating anxiety and addiction. Its selectivity for α4β2 nAChRs makes it a valuable tool for studying the role of this receptor subtype in reward, anxiety, and cognitive processes.
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| Molecular Formula |
C13H18CLNO2
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| Molecular Weight |
255.740522861481
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| Exact Mass |
255.102
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| CAS # |
2934318-93-9
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| Related CAS # |
(S)-UFR2709;1431628-22-6
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| PubChem CID |
162642465
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
236
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN1CCC[C@H]1COC(=O)C2=CC=CC=C2.Cl
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| InChi Key |
IJJHQEXZNVTJHI-YDALLXLXSA-N
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| InChi Code |
InChI=1S/C13H17NO2.ClH/c1-14-9-5-8-12(14)10-16-13(15)11-6-3-2-4-7-11;/h2-4,6-7,12H,5,8-10H2,1H3;1H/t12-;/m0./s1
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| Chemical Name |
[(2S)-1-methylpyrrolidin-2-yl]methyl benzoate;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 (e.g. under nitrogen), 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) |
H2O: 100 mg/mL (391.02 mM)
DMSO: 50 mg/mL (195.51 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.78 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 (9.78 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 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: ≥ 2.5 mg/mL (9.78 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: 50 mg/mL (195.51 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9102 mL | 19.5511 mL | 39.1022 mL | |
| 5 mM | 0.7820 mL | 3.9102 mL | 7.8204 mL | |
| 10 mM | 0.3910 mL | 1.9551 mL | 3.9102 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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