1. Epigenetics
    TGF-beta/Smad
  2. PKC

TAS-301 

Cat. No.: HY-18965 Purity: 99.50%
Handling Instructions

TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.

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

TAS-301 Chemical Structure

TAS-301 Chemical Structure

CAS No. : 193620-69-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 112 In-stock
Estimated Time of Arrival: December 31
5 mg USD 102 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.

IC50 & Target[1]

PKC

 

In Vitro

TAS-301 (1-10 μM) concentration-dependently inhibits PKC activation and Ca2+ influx, induced by PDGF, with 62.7% inhibition on PKC activation at 10 μM, and reduces PMA-induced AP-1, with 38% and 67.6% inhibition at 3 and 10 μM, respectively[1]. TAS-301 (0.3-3 μM) dose-dependently reduces the migration of cells induced by growth factors (PDGF-BB, IGF-1,HB-EGF). TAS-301 (1-10 μM) also decreases bFGF-induced BrdU incorporation, especially at 3 and 10 μM[2].

In Vivo

TAS-301 (3-100 mg/kg, p.o.) dose-dependently reduces the neointimal thickening and I/M ratio and decreases the level of intimal cells in rats 14 days after balloon injury[2].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 38 mg/mL (106.32 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7980 mL 13.9899 mL 27.9799 mL
5 mM 0.5596 mL 2.7980 mL 5.5960 mL
10 mM 0.2798 mL 1.3990 mL 2.7980 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

Cell proliferation is determined by the incorporation of BrdU by quiescent cells. SMCs are seeded at 1 × 104cells/well in 96-well plates in DMEM containing 10% FBS. Two days after the seeding, their growth is arrested for 3 days in a serum-free DMEM containing 5 μg/mL insulin, 5 μg/mL transferrin and 5 ng/mL sodium selenium (ITS). Then, the DMEM/ITS is removed, and serum-free DMEM containing 0.1% BSA with or without TAS-301 or tranilast is added to the quiescent cells 2 hr before treatment with the growth factor (i.e., bFGF 0.1 ng/mL). At 24 hr after stimulation, BrdU (10 μM) is added to the cells; 24 hr later, the cells are fixed. An ELISA is used to detect and to quantify the incorporated BrdU (n = 6). The drugs are present during the entire experiment[2].

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

Animal Administration
[2]

Rats[2]
On the 14th day after the balloon injury, the rats are anesthetized with ether so as to avoid any stress to the animals and then perfused transcardially with saline, followed by 10% buffered formalin. Next, the left carotid artery (length from aortic arch to bifurcation) is removed, postfixed and embedded in paraffin. Then, 3-μm-thick artery sections (six sections for each artery) are cut and stained with hematoxylin and eosin. The cross-sectional areas of the intima and the media on photographs are measured by use of a digital analyzer. The average of the ratio of the intimal area to the medial area in each artery is determined. Experimental groups are as follows: Vehicle (n = 9), TAS-301 (3, 10, 30 and 100 mg/kg,n = 9) and tranilast (100 and 300 mg/kg,n = 9). The data on two rats (one in TAS-301 100 mg/kg group and one in tranilast 100 mg/kg group) is omitted from the evaluation because of death due to faulty oral administration[2].

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

References
Molecular Weight

357.40

Formula

C₂₃H₁₉NO₃

CAS No.

193620-69-8

SMILES

O=C1NC2=C(C=CC=C2)/C1=C(C3=CC=C(OC)C=C3)/C4=CC=C(OC)C=C4

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

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
TAS-301
Cat. No.:
HY-18965
Quantity:

TAS-301

Cat. No.: HY-18965