2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. G protein-coupled Bile Acid Receptor 1 Calcium Channel
  4. TGR5 Receptor Agonist

TGR5 Receptor Agonist  (Synonyms: CCDC)

Cat. No.: HY-14229 Purity: 99.71%
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TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity.

For research use only. We do not sell to patients.

TGR5 Receptor Agonist Chemical Structure

TGR5 Receptor Agonist Chemical Structure

CAS No. : 1197300-24-5

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

TGR5 Receptor Agonist Related Antibodies

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Description

TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity[1][2][3][4].

IC50 & Target

TGR5[1]
In Vivo

TGR5 Receptor Agonist (CCDC) activates directly a sub-population of bladder-innervating dorsal root ganglia (DRG) neurons and a small percentage of non-neuronal cells in Trpv1-/- mice[2].
? TGR5 Receptor Agonist (CCDC) (2?or 5 μg; ICV) reduces food intake and body weight in diet-induced obese mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

361.22

Formula

C18H14Cl2N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=CC=C1C2=NOC(C)=C2C(N(C)C3=CC=C(Cl)C=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & 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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7684 mL 13.8420 mL 27.6840 mL
5 mM 0.5537 mL 2.7684 mL 5.5368 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 10 mg/mL (27.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 10 mg/mL (27.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7684 mL 13.8420 mL 27.6840 mL 69.2099 mL
5 mM 0.5537 mL 2.7684 mL 5.5368 mL 13.8420 mL
10 mM 0.2768 mL 1.3842 mL 2.7684 mL 6.9210 mL
15 mM 0.1846 mL 0.9228 mL 1.8456 mL 4.6140 mL
20 mM 0.1384 mL 0.6921 mL 1.3842 mL 3.4605 mL
25 mM 0.1107 mL 0.5537 mL 1.1074 mL 2.7684 mL
30 mM 0.0923 mL 0.4614 mL 0.9228 mL 2.3070 mL
40 mM 0.0692 mL 0.3460 mL 0.6921 mL 1.7302 mL
50 mM 0.0554 mL 0.2768 mL 0.5537 mL 1.3842 mL
60 mM 0.0461 mL 0.2307 mL 0.4614 mL 1.1535 mL
80 mM 0.0346 mL 0.1730 mL 0.3460 mL 0.8651 mL
100 mM 0.0277 mL 0.1384 mL 0.2768 mL 0.6921 mL
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TGR5 Receptor Agonist Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TGR5 Receptor Agonist1197300-24-5CCDCG protein-coupled Bile Acid Receptor 1Calcium ChannelG-protein coupled receptor 19GPCR19TGR5GPBAR1Ca2+ channelsCa channelsU2-OS cellsmelanophore cellsdiabetesbladder hypersensitivityanti-obesityC57BL/6J miceInhibitorinhibitorinhibit

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