| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
hTGR5 ( IC50 = 0.72 nM ); mTGR5 ( IC50 = 6.2 nM )
TC-G 1005 targets Takeda G protein-coupled receptor 5 (TGR5, also known as GPBAR1), a bile acid receptor involved in energy metabolism and glucose homeostasis. By activating TGR5, TC-G 1005 increases plasma GLP-1 levels and reduces blood glucose in mice. The compound is selective for TGR5 over FXR (farnesoid X receptor). |
|---|---|
| ln Vitro |
TC-G 1005 induces mouse TGR5 with EC50 of 0.72 nM and 6.2 nM respectively[1].
In vitro, TC-G 1005 is a potent TGR5 agonist with EC50 values of 0.72 nM for hTGR5 and 6.2 nM for mTGR5. It is selective for TGR5 over FXR. The compound's activity is assessed by measuring TGR5 activation in cell-based assays using receptor-expressing cells and downstream signaling readouts such as cAMP accumulation. |
| ln Vivo |
TC-G 1005 (25-100 mg/kg; single oxygen dose) activates GLP-1 in the imprinted control region (ICR)[1]
TC-G 1005 (50 mg/kg; single po) can lower blood pressure AUC0-120 minutes by 49% in ICR mice.[1] TC-G 1005 (50 mg/kg; oral single dose) lowered blood pressure at 4, 6, 10, and 24 hours using db/db electrodes.[1] TC-G 1005 (5 mg/kg; po) showed a fairly low toxic exposure in FX, with a t1/2 of 1.5 and a Cmax of 56 ng/mL.[1] In vivo, TC-G 1005 increases plasma GLP-1 levels and reduces blood glucose in mice. The compound is orally active and has potential applications in the treatment of metabolic disorders such as type 2 diabetes. Its effects on glucose metabolism are mediated through TGR5 activation and GLP-1 secretion. |
| Enzyme Assay |
In vitro receptor binding assays for TC-G 1005 measure its affinity for TGR5 using radioligand displacement or functional assays. The compound's activity is assessed in cells expressing human or mouse TGR5 by measuring cAMP accumulation as a readout of receptor activation. EC50 values of 0.72 nM for hTGR5 and 6.2 nM for mTGR5 are determined.
|
| Cell Assay |
In vitro cell-based assays for TC-G 1005 use cells expressing human or mouse TGR5. Cells are treated with serial dilutions of the compound, and cAMP levels are measured by ELISA or other immunoassay methods. The EC50 for TGR5 activation is calculated from dose-response curves. Selectivity over FXR is confirmed by testing against FXR in parallel assays.
|
| Animal Protocol |
Male ICR mice
25, 50, 100 mg/kg A single p.o. In vivo animal models for TC-G 1005 include mouse models of diabetes and metabolic syndrome. The compound is administered orally, and its effects on blood glucose, plasma GLP-1 levels, and glucose tolerance are evaluated. Pharmacodynamic studies measure TGR5 activation and GLP-1 secretion in response to compound treatment. |
| ADME/Pharmacokinetics |
TC-G 1005 has a molecular formula of C25H25N3O2 and a molecular weight of 399.48 g/mol. It is soluble to 100 mM in DMSO and ethanol and is stored at -20°C. The compound has a purity of ≥98%. It is also known as GPBA agonist and TGR5 agonist.
|
| Toxicity/Toxicokinetics |
The toxicity profile of TC-G 1005 is characterized in preclinical safety studies. As a TGR5 agonist, the compound may affect bile acid metabolism and glucose homeostasis. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
|
| References |
|
| Additional Infomation |
TC-G 1005 is a potent, selective, and orally active TGR5 agonist with EC50 values of 0.72 nM for hTGR5 and 6.2 nM for mTGR5. It is selective for TGR5 over FXR. TC-G 1005 increases plasma GLP-1 levels and reduces blood glucose in mice. The compound is also known as GPBA agonist and is intended for laboratory research use only.
|
| Molecular Formula |
C25H25N3O2
|
|---|---|
| Molecular Weight |
399.49
|
| Exact Mass |
399.195
|
| Elemental Analysis |
C, 75.16; H, 6.31; N, 10.52; O, 8.01
|
| CAS # |
1415407-60-1
|
| PubChem CID |
71450251
|
| Appearance |
Off-white to yellow solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
564.5±50.0 °C at 760 mmHg
|
| Flash Point |
295.2±30.1 °C
|
| Vapour Pressure |
0.0±1.5 mmHg at 25°C
|
| Index of Refraction |
1.653
|
| LogP |
4.44
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
30
|
| Complexity |
609
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1C=NC=CC=1OC1C=C(C)C=CC=1C)N1C2C=CC=CC=2N(CC1)C1CC1
|
| InChi Key |
JQULIQJSYPZQMA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C25H25N3O2/c1-17-7-8-18(2)24(15-17)30-23-11-12-26-16-20(23)25(29)28-14-13-27(19-9-10-19)21-5-3-4-6-22(21)28/h3-8,11-12,15-16,19H,9-10,13-14H2,1-2H3
|
| Chemical Name |
(4-cyclopropyl-2,3-dihydroquinoxalin-1-yl)-[4-(2,5-dimethylphenoxy)pyridin-3-yl]methanone
|
| Synonyms |
TC-G-1005; TCG1005; TC-G 1005; TCG 1005; TC G 1005
|
| HS Tariff Code |
2934.99.03.00
|
| 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 (In Vitro) |
DMSO: ~33.3 mg/mL (~83.4 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5032 mL | 12.5160 mL | 25.0319 mL | |
| 5 mM | 0.5006 mL | 2.5032 mL | 5.0064 mL | |
| 10 mM | 0.2503 mL | 1.2516 mL | 2.5032 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.
Calculation results
Working concentration： mg/mL；
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.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
