| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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TC-G 1005 (TC-G-1005; TCG1005) is a novel, oral and potent TGR5 (GPBAR1) agonist with glucose-lowering effects. It has EC50s of 0.72 and 6.2 nM for human TGR5 and mouse TGR5, respectively, indicating that it inhibits the BA receptor Takeda G protein-coupled receptor 5 (TGR5).
| Targets |
hTGR5 ( IC50 = 0.72 nM ); mTGR5 ( IC50 = 6.2 nM )
|
|---|---|
| ln Vitro |
TC-G 1005 induces mouse TGR5 with EC50 of 0.72 nM and 6.2 nM respectively[1].
|
| 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] |
| Animal Protocol |
Male ICR mice
25, 50, 100 mg/kg A single p.o. |
| References |
|
| 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
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| PubChem CID |
71450251
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| 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
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| 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.
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