UCM-1306 (2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl)

Cat No.:V71726 Purity: ≥98%
UCM-1306 is an orally bioavailable allosteric modulator (PAM) of the human dopamine D1 receptor.
UCM-1306 (2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl) Chemical Structure CAS No.: 2258608-78-3
Product category: Dopamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
UCM-1306 is an orally bioavailable allosteric modulator (PAM) of the human dopamine D1 receptor. UCM-1306 maximally increases endogenous dopamine (DA) in human and mouse D1 receptors. UCM-1306 not only improves motor symptoms but also addresses key comorbid cognitive impairments associated with long-term PD/Parkinson's disease.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
The concentration-responsive enhancement of cAMP by UCM-1306 (2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl; 1-10 μM) has an EC50=60 nM.
ln Vivo
Good oral availability and brain penetration are features of UCM-1306 (2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl; 5 mg/kg; po; C57BL/6J mice). With a Tmax of 0.5 hours, plasma concentrations can be measured in 8 hours[1]. In adult mice, UCM-1306 (1 mg/kg; ip) amplifies the hyperlocomotion caused by cocaine[1]. Consolidating the establishment of long-term memory is aided by UCM-1306 (1 mg/kg; ip)[1].
Animal Protocol
Animal/Disease Models: Adult C57BL/6J mice with cocaine-induced hyperactivity model[1]
Doses: 1 mg/kg; cocaine (20 mg/kg, sc)
Route of Administration: intraperitoneal (ip) injection
Experimental Results: Increased cocaine-induced hyperlocomotion, suggesting an in vivo potentiation of DA action at the D1R.

Animal/Disease Models: Adult C57BL/6J mice
Doses: 1 mg/kg
Route of Administration: intraperitoneal (ip) injection
Experimental Results: Increased memory trace in C57BL/6J mice.
References
[1]. García-Cárceles J, et, al. 2-(Fluoromethoxy)-4'-(S-methanesulfonimidoyl)-1,1'-biphenyl (UCM-1306), an Orally Bioavailable Positive Allosteric Modulator of the Human Dopamine D1 Receptor for Parkinson's Disease. J Med Chem. 2022 Sep 22;65(18):12256-12272.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C14H14FNO2S
Molecular Weight
279.33
CAS #
2258608-78-3
SMILES
S(C)(C1C=CC(=CC=1)C1C=CC=CC=1OCF)(=N)=O
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)
Solubility Data
Solubility (In Vitro)
DMSO: 50 mg/mL (179.00 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.5800 mL 17.9000 mL 35.7999 mL
5 mM 0.7160 mL 3.5800 mL 7.1600 mL
10 mM 0.3580 mL 1.7900 mL 3.5800 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.

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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.
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