Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.
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Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.
Tiplaxtinin 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MDA-MB-231 cells
5 µM
17 hours
Inhibited PAI1 activity and reduced cell migration
Mol Cancer Res. 2019 May;17(5):1142-1154
SUM159 cells
5 µM
17 hours
Inhibited PAI1 activity and reduced cell migration
Mol Cancer Res. 2019 May;17(5):1142-1154
UROtsa cells
70.3 ± 0.1 µM (IC50)
24 hours
Inhibition of cellular proliferation and colony formation
Mol Cancer Ther. 2013 Dec;12(12):2697-708
UM-UC-14 cells
52.8 ± 1.6 µM (IC50)
24 hours
Inhibition of cellular proliferation and colony formation
Mol Cancer Ther. 2013 Dec;12(12):2697-708
T24 cells
43.7 ± 6.3 µM (IC50)
24 hours
Inhibition of cellular proliferation and colony formation
Mol Cancer Ther. 2013 Dec;12(12):2697-708
Newborn rat arterial smooth muscle cells (RASMCs)
10 µM
24 hours
To evaluate the effect of Tiplaxtinin on RASMCs apoptosis; results showed that Tiplaxtinin dose-dependently induced RASMCs apoptosis.
Cell Signal. 2015 May;27(5):923-33
HaCaT keratinocytes
10 µM
24 hours
To assess the effect of Tiplaxtinin on recombinant PAI-1-stimulated keratinocyte migration, results showed that Tiplaxtinin significantly attenuated PAI-1-induced motility.
Adv Wound Care (New Rochelle). 2015 Jun 1;4(6):321-328
Human lung microvascular endothelial cells
11 µM
4 hours
Tiplaxtinin significantly attenuated PAK-induced increase in protein permeability and RhoA activity in HMVEC monolayers.
Thorax. 2011 Sep;66(9):788-96
Bovine pulmonary arterial endothelial cells
11 µM
4 hours
Tiplaxtinin significantly attenuated PAK-induced increase in protein permeability and RhoA activity in BPAEC monolayers.
Inhibition of PAI-1 activity resulted in significant reduction in cellular proliferation
Mol Cancer Res. 2014 Mar;12(3):322-34
UM-UC-14 cells
52.8 ± 1.6 µM (IC50)
72 hours
Inhibition of PAI-1 activity resulted in significant reduction in cellular proliferation
Mol Cancer Res. 2014 Mar;12(3):322-34
T24 cells
43.7 ± 6.3 µM (IC50)
72 hours
Inhibition of PAI-1 activity resulted in significant reduction in cellular proliferation
Mol Cancer Res. 2014 Mar;12(3):322-34
KYSE-450 cells
100 ng/mL
72 hours
PAI-1 significantly promoted the proliferation and colony formation of KYSE-450 cells and reduced cisplatin-induced apoptosis.
Cell Death Dis. 2018 Jul 9;9(7):759
KYSE-30 cells
100 ng/mL
72 hours
PAI-1 significantly promoted the proliferation and colony formation of KYSE-30 cells and reduced cisplatin-induced apoptosis.
Cell Death Dis. 2018 Jul 9;9(7):759
HaCaT keratinocytes
10 µM
72 hours
To assess the effect of Tiplaxtinin on keratinocyte proliferation, results showed that Tiplaxtinin had no effect on cell cycle progression.
Adv Wound Care (New Rochelle). 2015 Jun 1;4(6):321-328
Tiplaxtinin 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
KYSE-30 cells and CAF CIS co-transplantation model
Oral gavage
10 mg/kg
Every 3 days for 3 weeks
Tiplaxtinin combined with cisplatin significantly inhibited tumor growth and enhanced the chemotherapeutic effects.
Cell Death Dis. 2018 Jul 9;9(7):759
Mice
APP/PS1 mouse model
Oral
12 mg/kg
Once daily for 8 weeks
To evaluate the effect of Tiplaxtinin on PbAc-induced CAA pathology. Results showed that Tiplaxtinin significantly reduced vascular amyloid deposition and improved cognitive function.
Environ Health Perspect. 2024 Oct;132(10):107004
Mice
Ins2WT/C96Y mice (model of adolescent-onset type 1 diabetes)
Oral
2 mg/kg
Twice daily for 5 days
Pharmacologic inhibition of PAI-1 with orally administered PAI-039 restored the early regenerative impairments in noninsulin-treated Ins2WT/C96Y mice. Results showed that PAI-039 treatment increased active uPA and MMP9 levels, reduced collagen content, and restored Myh3 expression.
Diabetes. 2011 Jul;60(7):1964-72
FVB/NJ mice
Carotid artery ligation model
Oral gavage
3 mg/kg
Once daily for 14 days
To evaluate the effect of Tiplaxtinin on neointima formation after carotid artery ligation; results showed that Tiplaxtinin significantly reduced neointimal thickening.
Cell Signal. 2015 May;27(5):923-33
Mice
Pseudomonas aeruginosa pneumonia model
Intraperitoneal injection
30 mg/kg
Twice, 1 h before and at the time of airspace instillation of P aeruginosa
Tiplaxtinin significantly attenuated P aeruginosa-induced increase in lung vascular permeability, but was associated with higher mortality at 24 h and decreased bacterial clearance in the lungs.
Thorax. 2011 Sep;66(9):788-96
C57BL/6J mice
Chronic allergic asthma model
Oral
5 mg/day
From 1 day before challenge until Day 36
Tiplaxtinin significantly decreased levels of active PAI-1 in BALF, reduced infiltration of inflammatory cells in the lungs of OVA-challenged mice, significantly attenuated goblet cell hyperplasia and collagen deposition, and effectively reduced methacholine-induced airway hyperresponsiveness.
Am J Respir Cell Mol Biol. 2012 Jun;46(6):842-6
LDL receptor-deficient mice
Western diet-induced obesity and metabolic syndrome model
Oral
5 mg/g of diet
Continued for 12-24 weeks
To evaluate the effects of PAI-039 on atherosclerosis and metabolic dysfunction, results showed PAI-039 significantly inhibited obesity and atherosclerosis formation, reduced macrophage accumulation and cell senescence
Human bladder cancer T24 xenograft model and human cervical cancer HeLa xenograft model
Oral gavage
5 mg/kg and 20 mg/kg
Once daily for 5 weeks
Inhibition of tumor growth, angiogenesis and induction of apoptosis
Mol Cancer Ther. 2013 Dec;12(12):2697-708
FVB/NJ mice
4 mm biopsy punch skin wound model
Topical administration
6 mg/kg
Once daily for 5 days
To evaluate the effect of Tiplaxtinin on skin wound healing, results showed that Tiplaxtinin significantly reduced wound closure and re-epithelialization, and decreased fibroblast proliferation and myofibroblast differentiation.
Adv Wound Care (New Rochelle). 2015 Jun 1;4(6):321-328
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