TGR5

SKU: orb1226821

Description

TGR5 Receptor Agonist, a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5).

Research Area

Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1197300-24-5
MW	361.22
Purity	>98% (HPLC)
Formula	C₁₈H₁₄Cl₂N₂O₂
SMILES	O=C(C1=C(C)ON=C1C2=CC=CC=C2Cl)N(C3=CC=C(Cl)C=C3)C
Target	GPCR19
Solubility	DMSO, Ethanol: 100 mM

Bioactivity

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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. TGR5 Receptor Agonist (CCDC) (2 or 5 μg; ICV) reduces food intake and body weight in diet-induced obese mice. Animal model: Female C57BL/6J mice [12-18 weeks; TRPV1 knockout (trpv1-/-), TRPA1 knockout (trpa1-/-), or TGR5 knockout (Gpbar1-/-)]. 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). 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). 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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TGR5 Receptor Agonist | MDK00245 | MDK-00245 | MDK 00245

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Quick Database Links

Gene Symbol

GPCR19

Protocol Information

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Reactivity:	Rat
Dynamic Range:	0.63-40 ng/mL
Sensitivity:	0.11 ng/mL

Reactivity:	Human
Dynamic Range:	0.16-10 ng/mL
Sensitivity:	0.055 ng/mL

Applications:	IF, IHC-Fr, IHC-P
Reactivity:	Human
Species/Host:	Rabbit
Clonality:	Polyclonal
Conjugation:	Unconjugated

Applications:	IHC, IHC-P
Reactivity:	Human
Species/Host:	Rabbit
Clonality:	Polyclonal
Conjugation:	Unconjugated

Applications:	IHC, IHC-P
Reactivity:	Human
Species/Host:	Rabbit
Clonality:	Polyclonal
Conjugation:	Unconjugated

TGR5

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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