| Size | Price | Stock | Qty |
|---|---|---|---|
| 2mg |
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| 5mg | |||
| Other Sizes |
| Targets |
G protein-coupled bile acid receptor 1 (GPBAR1, TGR5). INT-777 R-enantiomer is a selective agonist of TGR5. Activation of TGR5 leads to an increase in intracellular cAMP levels, which stimulates the secretion of GLP-1 from intestinal L-cells. This can improve glucose homeostasis and increase energy expenditure.
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|---|---|
| ln Vitro |
INT-777 R-enantiomer is a selective agonist of the TGR5 receptor. It has been shown to stimulate GLP-1 secretion in vitro. Its potency and selectivity for TGR5 over other bile acid receptors, such as FXR, have been demonstrated. It is a more potent enantiomer compared to the S-enantiomer.
|
| ln Vivo |
Compared to CA (4), INT-777 (R enantiomer) is less powerful but more choleretic [1].
In vivo, INT-777 R-enantiomer has been shown to improve glucose tolerance and increase GLP-1 secretion in animal models. It has been investigated for its potential to treat type 2 diabetes and obesity. Its effects are mediated through the activation of TGR5. |
| Enzyme Assay |
In vitro assays for INT-777 R-enantiomer involve measuring its ability to activate TGR5. Receptor binding assays can be performed using membrane preparations from cells expressing TGR5. Functional assays measure the activation of cAMP accumulation in cells expressing TGR5. Selectivity over other receptors, such as FXR, is also assessed.
|
| Cell Assay |
In vitro cell-based assays for INT-777 R-enantiomer are performed using cells expressing TGR5, such as intestinal L-cells or recombinant cell lines. Cells are treated with the compound, and cAMP levels are measured. The compound's ability to stimulate GLP-1 secretion can be measured in L-cell lines or in primary intestinal cultures.
|
| Animal Protocol |
In vivo animal studies for INT-777 R-enantiomer are conducted in models of type 2 diabetes and obesity. The compound is administered to rodents, and glucose tolerance, insulin sensitivity, and GLP-1 levels are measured. Its effects on body weight and food intake are also assessed.
|
| ADME/Pharmacokinetics |
INT-777 R-enantiomer has a molecular weight of 450.65 and a molecular formula of C27H46O5. It is a small molecule with expected oral bioavailability. It should be stored as powder at -20°C. For in vivo administration, it can be formulated in a suitable vehicle.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are documented for INT-777 R-enantiomer in the provided sources. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. Standard laboratory safety practices should be followed when handling this compound.
|
| References | |
| Additional Infomation |
INT-777 R-enantiomer is a selective agonist of the TGR5 receptor. It has been investigated for the treatment of type 2 diabetes and obesity. It stimulates GLP-1 secretion. It is for research use only.
|
| Molecular Formula |
C₂₇H₄₆O₅
|
|---|---|
| Molecular Weight |
450.6511
|
| Exact Mass |
450.334
|
| CAS # |
1198786-98-9
|
| Related CAS # |
INT-777;1199796-29-6
|
| PubChem CID |
44605418
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
602.8±55.0 °C at 760 mmHg
|
| Flash Point |
332.4±28.0 °C
|
| Vapour Pressure |
0.0±3.9 mmHg at 25°C
|
| Index of Refraction |
1.539
|
| LogP |
3.99
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
32
|
| Complexity |
710
|
| Defined Atom Stereocenter Count |
13
|
| SMILES |
CC[C@@H]1[C@@H]2C[C@@H](CC[C@@]2([C@H]3C[C@@H]([C@]4([C@H]([C@@H]3[C@@H]1O)CC[C@@H]4[C@H](C)C[C@@H](C)C(=O)O)C)O)C)O
|
| InChi Key |
NPBCMXATLRCCLF-IRRLEISYSA-N
|
| InChi Code |
InChi Code
InChI=1S/C27H46O5/c1-6-17-20-12-16(28)9-10-26(20,4)21-13-22(29)27(5)18(14(2)11-15(3)25(31)32)7-8-19(27)23(21)24(17)30/h14-24,28-30H,6-13H2,1-5H3,(H,31,32)/t14-,15+,16-,17-,18-,19+,20+,21+,22+,23+,24-,26+,27-/m1/s1
|
| Chemical Name |
(2R,4R)-4-[(3R,5S,6R,7R,8R,9S,10S,12S,13R,14S,17R)-6-ethyl-3,7,12-trihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid
|
| Synonyms |
INT-777;INT 777;INT777;6-EMCA;S-EMCA
|
| HS Tariff Code |
2934.99.9001
|
| 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 : ≥ 100 mg/mL (~221.90 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.55 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 (5.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2190 mL | 11.0951 mL | 22.1902 mL | |
| 5 mM | 0.4438 mL | 2.2190 mL | 4.4380 mL | |
| 10 mM | 0.2219 mL | 1.1095 mL | 2.2190 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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