selective par1 antagonist Search Results


selective par1 antagonist vorapaxar  (Takeda)
90
Takeda selective par1 antagonist vorapaxar
FXa- and thrombin-induced MCP-1 production in HUVECs. MCP-1 concentration was determined in cell supernatant collected 20 h after the addition of the agonist, FXa (A) or thrombin (B) . In inhibition studies (C,D) , each inhibitor was added 1 h prior to the addition of the agonist and effects of TAK-442 (TAK), melagatran (Mel), and <t>vorapaxar</t> (Vor) on MCP-1 productions induced by 1 U/mL FXa (C) and 0.3 U/mL thrombin (D) were measured. Data are shown as mean ± SEM ( n = 3). ∗ P ≤ 0.025 compared with the control value of cells treated without FXa or thrombin (one-tailed Williams’ test) (A,B) . ∗ P ≤ 0.025 and † P ≤ 0.05 compared with the control value of cells treated with FXa or thrombin and no inhibitor (one-tailed Williams’ test and Student’s t -test, respectively, following ANOVA) (C,D) .
Selective Par1 Antagonist Vorapaxar, supplied by Takeda, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/result/selective par1 antagonist vorapaxar/product/Takeda
Average 90 stars, based on 1 article reviews
selective par1 antagonist vorapaxar - by Bioz Stars, 2026-03
90/100 stars
  Buy from Supplier

Image Search Results


FXa- and thrombin-induced MCP-1 production in HUVECs. MCP-1 concentration was determined in cell supernatant collected 20 h after the addition of the agonist, FXa (A) or thrombin (B) . In inhibition studies (C,D) , each inhibitor was added 1 h prior to the addition of the agonist and effects of TAK-442 (TAK), melagatran (Mel), and vorapaxar (Vor) on MCP-1 productions induced by 1 U/mL FXa (C) and 0.3 U/mL thrombin (D) were measured. Data are shown as mean ± SEM ( n = 3). ∗ P ≤ 0.025 compared with the control value of cells treated without FXa or thrombin (one-tailed Williams’ test) (A,B) . ∗ P ≤ 0.025 and † P ≤ 0.05 compared with the control value of cells treated with FXa or thrombin and no inhibitor (one-tailed Williams’ test and Student’s t -test, respectively, following ANOVA) (C,D) .

Journal: Frontiers in Pharmacology

Article Title: TAK-442, a Direct Factor Xa Inhibitor, Inhibits Monocyte Chemoattractant Protein 1 Production in Endothelial Cells via Involvement of Protease-Activated Receptor 1

doi: 10.3389/fphar.2018.01431

Figure Lengend Snippet: FXa- and thrombin-induced MCP-1 production in HUVECs. MCP-1 concentration was determined in cell supernatant collected 20 h after the addition of the agonist, FXa (A) or thrombin (B) . In inhibition studies (C,D) , each inhibitor was added 1 h prior to the addition of the agonist and effects of TAK-442 (TAK), melagatran (Mel), and vorapaxar (Vor) on MCP-1 productions induced by 1 U/mL FXa (C) and 0.3 U/mL thrombin (D) were measured. Data are shown as mean ± SEM ( n = 3). ∗ P ≤ 0.025 compared with the control value of cells treated without FXa or thrombin (one-tailed Williams’ test) (A,B) . ∗ P ≤ 0.025 and † P ≤ 0.05 compared with the control value of cells treated with FXa or thrombin and no inhibitor (one-tailed Williams’ test and Student’s t -test, respectively, following ANOVA) (C,D) .

Article Snippet: The selective FXa inhibitor TAK-442, 1-(1-{(2S)-3-[(6-chloro–2-naphthyl) sulfonyl]-2-hydroxypropanoyl}piperidin-4-yl)tetra hydropyrimidin-2(1H)-one, the selective thrombin inhibitor melagatran, N-((1R)-2-{(2S)–2-[({4-[amino(imino)methyl]benzyl}amino)carbonyl]azetidin-1-yl}-1–cyclohexyl-2-oxoethyl) glycine, and the selective PAR1 antagonist vorapaxar, ethyl(9-{(E)–2-[5-(3-fluorophenyl)pyridin-2-yl]vinyl}-1-methyl-3-oxododecahydronaphtho[2,3-c]furan-6-yl)carbamate, were synthesized at Takeda Pharmaceutical Co., Ltd. (Osaka, Japan).

Techniques: Concentration Assay, Inhibition, Control, One-tailed Test

Effects of TAK-442, melagatran, and vorapaxar on the intracellular calcium ion concentration ([Ca 2+ ]i) induced by FXa, thrombin, and SFLLRN-NH2 in human PAR1-transfected Chinese hamster ovary (hPAR1/CHO-K1) cells. Calcium signal was recorded after the addition of FXa (0.03 U/mL) (A) , thrombin (0.003 U/mL) (B) , or PAR1 agonist peptide SFLLRN-NH2 (3 nM) (C) using FRIPR. Each inhibitor, TAK-442, melagatran, or vorapaxar, was pre-incubated with the cells for 10 min before the treatment with each agonist. Data are expressed as the percentage inhibition of calcium signal obtained after the addition of agonist in inhibitor-treated wells ( n = 4) compared with control wells (no inhibitor added). The drug concentration need to suppress the [Ca 2+ ]i by 50% (IC 50 ) was determined.

Journal: Frontiers in Pharmacology

Article Title: TAK-442, a Direct Factor Xa Inhibitor, Inhibits Monocyte Chemoattractant Protein 1 Production in Endothelial Cells via Involvement of Protease-Activated Receptor 1

doi: 10.3389/fphar.2018.01431

Figure Lengend Snippet: Effects of TAK-442, melagatran, and vorapaxar on the intracellular calcium ion concentration ([Ca 2+ ]i) induced by FXa, thrombin, and SFLLRN-NH2 in human PAR1-transfected Chinese hamster ovary (hPAR1/CHO-K1) cells. Calcium signal was recorded after the addition of FXa (0.03 U/mL) (A) , thrombin (0.003 U/mL) (B) , or PAR1 agonist peptide SFLLRN-NH2 (3 nM) (C) using FRIPR. Each inhibitor, TAK-442, melagatran, or vorapaxar, was pre-incubated with the cells for 10 min before the treatment with each agonist. Data are expressed as the percentage inhibition of calcium signal obtained after the addition of agonist in inhibitor-treated wells ( n = 4) compared with control wells (no inhibitor added). The drug concentration need to suppress the [Ca 2+ ]i by 50% (IC 50 ) was determined.

Article Snippet: The selective FXa inhibitor TAK-442, 1-(1-{(2S)-3-[(6-chloro–2-naphthyl) sulfonyl]-2-hydroxypropanoyl}piperidin-4-yl)tetra hydropyrimidin-2(1H)-one, the selective thrombin inhibitor melagatran, N-((1R)-2-{(2S)–2-[({4-[amino(imino)methyl]benzyl}amino)carbonyl]azetidin-1-yl}-1–cyclohexyl-2-oxoethyl) glycine, and the selective PAR1 antagonist vorapaxar, ethyl(9-{(E)–2-[5-(3-fluorophenyl)pyridin-2-yl]vinyl}-1-methyl-3-oxododecahydronaphtho[2,3-c]furan-6-yl)carbamate, were synthesized at Takeda Pharmaceutical Co., Ltd. (Osaka, Japan).

Techniques: Concentration Assay, Transfection, Incubation, Inhibition, Control