Art. -Nr.: HY-146434

TGFβ-IN-2

1 Cited Publications

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TGFβ-IN-2 is an orally active TGF-β inhibitor. TGFβ-IN-2 suppresses the TGF-β-induced protein expression of COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 demonstrates excellent anti-fibrotic efficacy in Bleomycin (HY-108345)-induced pulmonary fibrosis model. TGFβ-IN-2 can be used for the study of pulmonary fibrosis.

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Reinheit: 99.37%
CAS. Nr.: 2387678-02-4
Formel: C₂₂H₂₂N₂O₄
Molecular Weight:378.42

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

TGFβ-IN-2 Chemical Structure

CAS. Nr.: 2387678-02-4

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle TGF-beta/Smad Isoform-spezifische Produkte anzeigen :

Smad1
Smad3

Cellular Effect

Cell Line	Type	Value	Description	References
NRK-49F	IC₅₀	4.31 μM Compound: 9d	Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis	[PMID: 31699535]

In Vitro

TGFβ-IN-2 (Compound 9d) (10 μM, 72 h) shows 85.14% inhibition at 10 μM of TGF-β-induced total collagen accumulation in NRK-49F cells with a 93.62% cell survival rate^[1].
TGFβ-IN-2 (10 μM) inhibits TGF-β-induced total collagen accumulation in NRK-49F cells with an IC₅₀ of 4.31 μM^[1].
TGFβ-IN-2 (1 μM, 24 h) exhibits the most potent inhibition on fibroblasts-driven macrophage migration in vitro compared to other compounds^[1].
TGFβ-IN-2 (20-40 μM) suppresses TGF-β1-induced protein expression of COL1A1, α-SMA, and p-Smad3 in NRK-49F cells, indicating inhibition of the TGF-β/Smad3 pathway^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	AUC_0-t	F
Rat^[1]	10 mg/kg	p.o.	74.73 μg/L	0.63 h	13.09 h	1104.95 μg/L·h	39.88 %
Rat^[1]	5 mg/kg	i.v.	316.44 μg/L	2.68 h	7.42 h	1385.24 μg/L·h	/

In Vivo

TGFβ-IN-2 (Compound 9d) (50-100 mg/kg, daily, p.o., 4 weeks) demonstrates excellent anti-fibrotic efficacy in Bleomycin (HY-108345)-induced pulmonary fibrosis model in C57BL/6 mice^[1].

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

Animal Model:

Bleomycin (HY-108345) (2 U/kg) was intratracheally instilled into 7-8-week-old male C57BL/6 mice to induce pulmonary fibrosis model^[1].
Dosage:

50, 100 mg/kg
Administration:

p.o. daily for 4 weeks
Result:

Reduced hydroxyproline content in lung tissues.
Alleviated alveolar structure destruction.
Decreased inflammatory cell infiltration in lung tissue and bronchoalveolar lavage fluid (BALF).
Improved survival rate to about 90% in bleomycin-induced pulmonary fibrosis model.
Did not inhibit fibrosis50 mg/kg.

Chemical Information

CAS. Nr. 2387678-02-4
Appearance Solid
Molecular Weight 378.42
Formel C₂₂H₂₂N₂O₄
Color White to off-white
SMILES

O=C(NC1=CC=C(C=C1)OC2=CC(OC3=CC=CC=C32)=O)CN4CCCCC4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Adv Sci (Weinh)

Highly Bioadaptable Hybrid Conduits with Spatially Bidirectional Structure for Precision Nerve Fiber Regeneration via Gene Therapy. [Abstract]

2024 May;11(19):e2309306. PMID: 38483934

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (264.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6426 mL

13.2128 mL

26.4257 mL

5 mM

0.5285 mL

2.6426 mL

5.2851 mL

10 mM

0.2643 mL

1.3213 mL

2.6426 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (13.21 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (13.21 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 5 mg/mL (13.21 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Dexin Deng, et al. Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. Eur J Med Chem. 2020 Jan 1;185:111790. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.6426 mL	13.2128 mL	26.4257 mL	66.0642 mL
	5 mM	0.5285 mL	2.6426 mL	5.2851 mL	13.2128 mL
	10 mM	0.2643 mL	1.3213 mL	2.6426 mL	6.6064 mL
	15 mM	0.1762 mL	0.8809 mL	1.7617 mL	4.4043 mL
	20 mM	0.1321 mL	0.6606 mL	1.3213 mL	3.3032 mL
	25 mM	0.1057 mL	0.5285 mL	1.0570 mL	2.6426 mL
	30 mM	0.0881 mL	0.4404 mL	0.8809 mL	2.2021 mL
	40 mM	0.0661 mL	0.3303 mL	0.6606 mL	1.6516 mL
	50 mM	0.0529 mL	0.2643 mL	0.5285 mL	1.3213 mL
	60 mM	0.0440 mL	0.2202 mL	0.4404 mL	1.1011 mL
	80 mM	0.0330 mL	0.1652 mL	0.3303 mL	0.8258 mL
	100 mM	0.0264 mL	0.1321 mL	0.2643 mL	0.6606 mL

Keywords

TGFβ-IN-2

1 Cited Publications

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TGFβ-IN-2

Angiogenesis-Related Compound Library

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Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

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Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Immunology/Inflammation Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) TGFβ-IN-2

Alle TGF-beta/Smad Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TGFβ-IN-2

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Immunology/Inflammation Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) TGFβ-IN-2

Alle TGF-beta/Smad Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TGFβ-IN-2 Related Classifications

HY-146434 Related Classifications