TGFβ1-IN-1 |
| Catalog No.GC70021 |
TGFβ1-IN-1 is a highly effective, orally active transforming growth factor β1 (TGF-β1) specific inhibitor that can significantly block the TGF-β1 signaling pathway and inhibit the upregulation of fibrosis-related proteins (such as α-smooth muscle actin and fibronectin) mediated by it. It is suitable for the mechanism research and treatment development of fibroproliferative diseases such as liver fibrosis.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2348795-14-0
Sample solution is provided at 25 µL, 10mM.
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TGFβ1-IN-1 is a highly effective, orally active transforming growth factor β1 (TGF-β1) specific inhibitor that can significantly block the TGF-β1 signaling pathway and inhibit the upregulation of fibrosis-related proteins (such as α-smooth muscle actin and fibronectin) mediated by it. It is suitable for the mechanism research and treatment development of fibroproliferative diseases such as liver fibrosis[1]. TGF-β1 is a potent fibrogenic factor responsible for the synthesis of extracellular matrix and plays a key role in epithelial-mesenchymal transition (EMT), extracellular matrix (ECM) deposition and immunosuppressive microenvironment[2, 3].
In vitro, treatment of HK2 cells with TGFβ1-IN-1 (20μM) for 24h significantly inhibited the expression of intracellular S100 calcium-binding protein A2 (S100A2)[4].
In vivo, oral administration of TGFβ1-IN-1 (15, 30mg/kg) to mice with carbon tetrachloride (CCl4)-induced liver fibrosis model for 3 weeks prevented CCl4-induced liver damage, reduced liver weight factor, serum ALT, AST, CHO and TG levels, significantly improved liver structural damage and inflammatory cell infiltration, reduced liver tissue collagen deposition, and reduced the accumulation of immune cells. The effect was better than that of Tranilast[5].
References:
[1] Zhu J, Fan J, Xia Y, et al. Potential therapeutic targets of macrophages in inhibiting immune damage and fibrotic processes in musculoskeletal diseases[J]. Frontiers in immunology, 2023, 14: 1219487.
[2] Laping N J, Grygielko E, Mathur A, et al. Inhibition of transforming growth factor (TGF)-β1–induced extracellular matrix with a novel inhibitor of the TGF-β type I receptor kinase activity: SB-431542[J]. Molecular pharmacology, 2002, 62(1): 58-64.
[3] Chung J Y F, Chan M K K, Li J S F, et al. TGF-β signaling: from tissue fibrosis to tumor microenvironment[J]. International Journal of Molecular Sciences, 2021, 22(14): 7575.
[4] Yang X, Zheng F, Yan P, et al. S100A2 activation promotes interstitial fibrosis in kidneys by FoxO1-mediated epithelial-mesenchymal transition[J]. Cell Biology and Toxicology, 2024, 40(1): 86.
[5] Yue L, Xue T, Su X, et al. Discovery and evaluation of phenacrylanilide derivatives as novel potential anti-liver fibrosis agents[J]. European journal of medicinal chemistry, 2022, 242: 114685.
| Cell experiment [1]: | |
Cell lines | HK2 cells |
Preparation Method | HK2 cells were treated with TGFβ1-IN-1, a specific TGF-β1 inhibitor, at a concentration of 20μM for 24h to evaluate its efficacy in blocking the effects of TGF-β1 on S100A2 expression. |
Reaction Conditions | 20μM; 24h |
Applications | TGFβ1-IN-1 antagonized the protein expression of S100A2. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6J mice |
Preparation Method | Male C57BL/6J mice were divided into five groups: a CCl4+Tranliast (30mg/kg) group; CCl4+TGFβ1-IN-1(15mg/kg and 30mg/kg) groups; a control group and a CCl4 group. To establish a CCl4-induced mouse hepatic fibrosis model, mice were subjected to intraperitoneal injection of CCl4 (damas-beta, CAS: 56-23-5, 1mL/kg bodyweight, 1:4 v/v dissolved in olive oil) for 6 weeks (three times a week). Control mice were received an equal volume of olive oil. After 3 weeks of injection of oil/CCl4, drug therapy was initiated. The control and CCl4 groups received daily oral administration of dissolvent (5:45:55 ratio of DMSO: polyethylene glycol 400: normal saline); the drug groups received daily oral administration of low-dose TGFβ1-IN-1 (15mg/kg), high-dose TGFβ1-IN-1 (30mg/kg) and high-dose Tranilast (30mg/kg) for the last 3 weeks. Mice were sacrificed 24h after the final drug injection. Mouse livers, other organs and serum were obtained for subsequent analysis. |
Dosage form | 15, 30mg/kg; three times a week for 3 weeks; p.o. |
Applications | After treatment with TGFβ1-IN-1, the spleen weight coefficient decreased in a dose-dependent manner, and kidney injury and inflammatory cell infiltration after CCl4 stimulation were alleviated. |
References: | |
| Cas No. | 2348795-14-0 | SDF | |
| Formula | C22H24N2O3 | M.Wt | 364.44 |
| Solubility | DMSO : 100 mg/mL (274.39 mM; Need ultrasonic) | Storage | 4°C, away from moisture and light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7439 mL | 13.7197 mL | 27.4394 mL |
| 5 mM | 0.5488 mL | 2.7439 mL | 5.4879 mL |
| 10 mM | 0.2744 mL | 1.372 mL | 2.7439 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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