| Field | Specification |
|---|---|
| Alternative names | CCDC |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C18H14Cl2N2O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
TGR5 Receptor Agonist, also known as CCDC, is a potent agonist of Takeda G protein-coupled receptor 5 (TGR5; GPCR19) that shows improved potency in U2-OS cells and melanophore cells, with pEC50 values of 6.8 and 7.5, respectively. It can induce peripheral and central hypersensitivity to bladder distension in mice and increase intracellular Ca2+ concentration, and it can also reduce food intake and improve insulin responsiveness in diet-induced obese mice. It can be used to research diabetes, bladder hypersensitivity, and anti-obesity[1][2][3]. It is supplied as a white to off-white solid (C18H14Cl2N2O2, MW 361.22) at 99.67% purity.
Physical & Chemical Properties
| CAS Number | 1197300-24-5 |
|---|---|
| Molecular Formula | C18H14Cl2N2O2 |
| Molecular Weight | 361.22 g/mol |
| Purity | 99.67% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | ClC1=CC=CC=C1C2=NOC(C)=C2C(N(C)C3=CC=C(Cl)C=C3)=O |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling; Membrane Transporter/Ion Channel |
| Solubility | In Vitro: DMSO: ≥ 48 mg/mL (132.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 48 mg/mL (132.88 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 10 mg/mL (27.68 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 10 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (100.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 10 mg/mL (27.68 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 10 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (100.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vivo
In Trpv1-/- mice, TGR5 Receptor Agonist (CCDC) directly activates a sub-population of bladder-innervating dorsal root ganglia (DRG) neurons, as well as a small percentage of non-neuronal cells[2]. In diet-induced obese mice, TGR5 Receptor Agonist (CCDC) (2 or 5 μg; ICV) lowers food intake and body weight[3].
| Animal Model | Female C57BL/6J mice [12-18 weeks; TRPV1 knockout (trpv1-/-), TRPA1 knockout (trpa1-/-), or TGR5 knockout (Gpbar1-/-)][2] |
|---|---|
| Dosage | 100 μM, 100 μL |
| Administration | Infused gently, to fill but not fully distend the bladder, and allowed to incubate for 5 min |
| Result | Activated directly a sub-population of bladder-innervating dorsal root ganglia (DRG) neurons in Trpv1-/- mice, also activated a small percentage of non-neuronal cells. Increased intracellular Ca2+ in bladder-innervating DRG neurons. Increased intracellular Ca2+ in a small proportion of non-neuronal cells. |
| Animal Model | Male C57BL/6J mice (obese induced by high-fat diet)[3] |
|---|---|
| Dosage | 2 or 5 μg at a volume of 0.2 μL per brain side and a rate of 0.6 μL/min |
| Administration | ICV (acute intra-hypothalamic experiment) |
| Result | Significantly reduced food intake over time, with a robust reduction in 24 h food intake and body weight gain. |
| Animal Model | Male C57BL/6J mice (obese induced by high-fat diet; implanted with micro-osmotic pumps that were filled with CCDC)[3] |
|---|---|
| Dosage | 5 μg/day; 91.9 μL, pumping rate of 0.09 μL/h |
| Administration | ICV; for 4 weeks (chronic experiment) |
| Result | Reduced food intake and improved insulin responsiveness. Increased energy expenditure during the dark phase. Increased mRNA expression of β1, 2, and 3 adrenoreceptors (Adrb1, Adrb2, and Adrb3) in the epidydimal white adipose tissue, and increased Dio2 (the gene expressing the enzyme D2) in brown adipose tissue. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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