2. TGF-beta/Smad
  3. TGF-β Receptor
  4. TGFβ1-IN-1

TGFβ1-IN-1 (compound 42) is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in liver fibrosis disease studies.

For research use only. We do not sell to patients.

TGFβ1-IN-1 Chemical Structure

TGFβ1-IN-1 Chemical Structure

CAS No. : 2348795-14-0

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Based on 1 publication(s) in Google Scholar

TGFβ1-IN-1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

TGFβ1-IN-1 (compound 42) is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in liver fibrosis disease studies[1].

In Vitro

TGFβ1-IN-1 (compound 42) (0-20 μM, 72 h) inhibits the proliferation of TGF-β1 (5 ng/mL)-treated LX- 2 cells and inhibits LO2 cell viability with an IC 50 of 105 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TGFβ1-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: HSCs (LX-2) cells
Concentration: 20 μM
Incubation Time: 24 or 72 hours
Result: Showed the survival rate of 77.5% and the inhibition rate of 30.3% for LX-2 cells.
Significantly inhibited fibronectin and α-SMA protein expression.
In Vivo

TGFβ1-IN-1 (compound 42) (p.o., 15 or 30 mg/kg, daily, 3weeks) prevents CCl4-induced liver injury and fibrosis, inhibits the activation of hepatic stellate cell (HSC) and epithelial-mesenchymal transition (EMT), and improves the immune microenvironment of CCl4-induced liver fibrosis as well as CCl4-induced systemic toxicity in C57BL/6J mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Liver fibrosis C57BL/6J mice induced by CCl4[1]
Dosage: 15 or 30 mg/kg
Administration: Oral administration; daily; 3 weeks
Result: Significantly prevented CCl4-induced liver injury and reduced liver weight factor, serum ALT, AST, CHO and TG levels.
Significantly improved structural damage and inflammatory cell infiltration in the liver, and reduced collagen deposition in liver tissue.
Reduced accumulation of CCl4-induced immune cells, such as hepatic macrophages (F4/80+ CD11b+), Th1 cells (CD69+ CD4+), and Th2 cells (CD69+ CD8+) so on.
Molecular Weight

364.44

Formula

C22H24N2O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1CCCC1)C2=CC=CC(NC(/C=C/C3=CC=C(OC)C=C3)=O)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (274.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7439 mL 13.7197 mL 27.4394 mL 68.5984 mL
5 mM 0.5488 mL 2.7439 mL 5.4879 mL 13.7197 mL
10 mM 0.2744 mL 1.3720 mL 2.7439 mL 6.8598 mL
15 mM 0.1829 mL 0.9146 mL 1.8293 mL 4.5732 mL
20 mM 0.1372 mL 0.6860 mL 1.3720 mL 3.4299 mL
25 mM 0.1098 mL 0.5488 mL 1.0976 mL 2.7439 mL
30 mM 0.0915 mL 0.4573 mL 0.9146 mL 2.2866 mL
40 mM 0.0686 mL 0.3430 mL 0.6860 mL 1.7150 mL
50 mM 0.0549 mL 0.2744 mL 0.5488 mL 1.3720 mL
60 mM 0.0457 mL 0.2287 mL 0.4573 mL 1.1433 mL
80 mM 0.0343 mL 0.1715 mL 0.3430 mL 0.8575 mL
100 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6860 mL
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TGFβ1-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TGFβ1-IN-12348795-14-0TGF-β ReceptorTransforming growth factor beta receptorsLiver fibrosisTGF-β1Hepatic stellate cellsImmune microenvironmentα-SMAInhibitorinhibitorinhibit

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