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  2. GPCR19
  3. TC-G 1005

TC-G 1005 

Cat. No.: HY-110173
Handling Instructions

TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo.

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

TC-G 1005 Chemical Structure

TC-G 1005 Chemical Structure

CAS No. : 1415407-60-1

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Description

TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo[1][2].

IC50 & Target

IC50: 0.72 nM (hTGR5); 6.2 nM (mTGR5)[1]

In Vitro

TC-G 1005 activates human and mouse TGR5 with EC50s of 0.72 nM and 6.2 nM, respectively[1].

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

In Vivo

TC-G 1005 (25-100 mg/kg; a single p.o.) stimulates GLP-1 secretion in imprinting control region (ICR) mice[1].
TC-G 1005 (50 mg/kg; a single p.o.) causes a 49% reduction in blood glucose AUC0-120 min in ICR mice[1].
TC-G 1005 (50 mg/kg; a single p.o.) significantly reduces blood glucose at 4, 6, 10, and 24 h in db/db mice[1].
TC-G 1005 (5 mg/kg; p.o.) exhibits rather low plasma exposure, with a Cmax of 56 ng/mL and a t1/2 of 1.5 in rats[1].

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

Animal Model: Male ICR mice[1]
Dosage: 25, 50, 100 mg/kg
Administration: A single p.o.
Result: Increased the plasma active GLP-1 levels by 31, 96, and 282% at doses of 25, 50, and 100 mg/kg, respectively.
Molecular Weight

399.48

Formula

C₂₅H₂₅N₃O₂

CAS No.

1415407-60-1

SMILES

O=C(C1=CN=CC=C1OC2=C(C=CC(C)=C2)C)N3C4=CC=CC=C4N(C5CC5)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

TC-G 1005GPCR19G-protein coupled receptor 19BATakedaGproteincoupledTGR5glucoselevelsInhibitorinhibitorinhibit

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TC-G 1005
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