| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
Transcription factor MondoA (deactivates); insulin signaling pathway (stimulates); TXNIP and ARRDC4 (suppresses expression).
|
|---|---|
| ln Vitro |
In vitro, SBI-477 inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes. By deactivating MondoA, it reduces TXNIP and ARRDC4 expression, relieving suppression of insulin signaling. It also inhibits TNAP activity, reducing ectopic mineral deposition. Quantitative IC50 values are not detailed in publicly available sources.
|
| ln Vivo |
In vivo activity data is not publicly available. As a chemical probe for studying insulin signaling, SBI-477 may have potential for metabolic research, but specific animal model studies have not been reported in the available literature.
|
| Enzyme Assay |
No specific cell-free enzyme/receptor binding assay protocol is detailed for SBI-477. As a MondoA deactivator, typical cell-free assays might include transcription factor binding assays (e.g., EMSA, DNA-binding ELISA), or TNAP enzyme activity assays using chromogenic substrates.
|
| Cell Assay |
Cellular activity is assessed in human skeletal myocytes. Cells are treated with serial dilutions of SBI-477. Endpoints include glucose uptake (radioactive or fluorescent 2-DG uptake), triacylglyceride synthesis measurement (radioactive or colorimetric assays), and expression analysis of TXNIP and ARRDC4 (qPCR, Western blot). TNAP inhibition can be assessed in mineralization assays.
|
| Animal Protocol |
No in vivo animal experimental protocol is publicly available for SBI-477. For similar metabolic probes, typical in vivo studies involve oral administration in rodent models of metabolic syndrome or diabetes, with endpoints including glucose tolerance tests, insulin tolerance tests, and lipid profiling.
|
| ADME/Pharmacokinetics |
Molecular weight: 483.54; molecular formula: C24H25N3O6S. Solubility: DMSO (65 mg/mL). Appearance: solid. Storage: powder at -20°C for 3 years, 4°C for 2 years.
|
| Toxicity/Toxicokinetics |
No toxicity data is publicly available. As a research chemical probe, standard toxicological profiling would be required for further development.
|
| References | |
| Additional Infomation |
SBI-477 is a research-grade chemical probe, not approved for therapeutic use. It is primarily used for studying insulin signaling, MondoA biology, and metabolic regulation. No clinical trials have been reported. Its mechanism involves MondoA deactivation, leading to reduced TXNIP and ARRDC4 expression and enhanced insulin signaling.
|
| Molecular Formula |
C24H25N3O6S
|
|---|---|
| Molecular Weight |
483.5368
|
| Exact Mass |
483.146
|
| CAS # |
781628-99-7
|
| PubChem CID |
2469116
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
2.9
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
34
|
| Complexity |
671
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=CC=C(C=C1)C2=CSC(=N2)NC(=O)C3=CC(=C(C=C3)OCC(=O)N4CCOCC4)OC
|
| InChi Key |
SJPVXFZDWAIFFT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C24H25N3O6S/c1-30-18-6-3-16(4-7-18)19-15-34-24(25-19)26-23(29)17-5-8-20(21(13-17)31-2)33-14-22(28)27-9-11-32-12-10-27/h3-8,13,15H,9-12,14H2,1-2H3,(H,25,26,29)
|
| Chemical Name |
3-methoxy-N-[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]-4-(2-morpholin-4-yl-2-oxoethoxy)benzamide
|
| Synonyms |
SBI-477SBI 477SBI477
|
| 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 : ~65 mg/mL (~134.43 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (4.49 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 21.7 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: ≥ 2.17 mg/mL (4.49 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 21.7 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: ≥ 2.17 mg/mL (4.49 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 | 2.0681 mL | 10.3404 mL | 20.6808 mL | |
| 5 mM | 0.4136 mL | 2.0681 mL | 4.1362 mL | |
| 10 mM | 0.2068 mL | 1.0340 mL | 2.0681 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
