TM-5275 sodium salt is an inhibitor of plasminogen activator inhibitor-1 with antithrombotic activity in nonhuman primates.
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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
To investigate the effect of TM5275 on TGF-β1-stimulated proliferation and fibrogenic activity in HSC-T6 cells. Results showed that TM5275 significantly suppressed TGF-β1-stimulated HSC-T6 cell proliferation and the expression of fibrotic genes (e.g., Tgfb1 and Col1a1), and attenuated TGF-β1-stimulated fibrogenic activity by inhibiting AKT phosphorylation.
Mol Med Rep. 2020 Oct;22(4):2948-2956
Human lung fibroblasts (CCL-210 cells)
75 µM
24 hours
TM5275 induced apoptosis in both TGF-β1-treated and untreated human lung fibroblasts, associated with activation of caspase-3/7, induction of p53, and inhibition of α-smooth muscle actin, fibronectin, and PAI-1 expression.
Am J Respir Cell Mol Biol. 2012 Jan;46(1):87-95
RAW264.7 macrophages
100 µM
24 hours
TM5275 significantly inhibited LPS-induced mRNA expression of PAI-1, TNF, and MIP-2
J Inflamm (Lond). 2018 Jan 10;15:3
Mouse proximal tubular epithelial (mProx24) cells
50 µM
4 hours
Inhibited PAI-1-induced mRNA expression of fibrosis and inflammation markers and reversed PAI-1-induced inhibition of plasmin activity
PLoS One. 2016 Jun 3;11(6):e0157012
Valve Interstitial Cells (VICs)
100 µM
7 days
Inhibit PAI-1 activity and shorten clot lysis time (CLT)
Cells. 2023 May 16;12(10):1402
JHOC-8 cells
>100 µM
72 hours
TM5275 treatment showed no significant inhibitory effect on JHOC-8 cell proliferation.
Cancer Biol Ther. 2015;16(2):253-60
JHOC-7 cells
>100 µM
72 hours
TM5275 treatment showed no significant inhibitory effect on JHOC-7 cell proliferation.
Cancer Biol Ther. 2015;16(2):253-60
SKOV3 cells
>100 µM
72 hours
TM5275 treatment showed no significant inhibitory effect on SKOV3 cell proliferation.
Cancer Biol Ther. 2015;16(2):253-60
JHOC-5 cells
>100 µM
72 hours
TM5275 treatment showed no significant inhibitory effect on JHOC-5 cell proliferation.
Cancer Biol Ther. 2015;16(2):253-60
JHOC-9 cells
100 µM
72 hours
TM5275 treatment significantly inhibited the proliferation of JHOC-9 cells with an IC50 of 92.5 μM.
Cancer Biol Ther. 2015;16(2):253-60
ES-2 cells
100 µM
72 hours
TM5275 treatment significantly inhibited the proliferation of ES-2 cells with an IC50 of 67 μM.
Cancer Biol Ther. 2015;16(2):253-60
TM5275 sodium 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rats
Arteriovenous shunt thrombosis model and ferric chloride-treated carotid artery thrombosis model
Oral
1 to 10 mg/kg
Single dose
To evaluate the antithrombotic effect of TM5275, results showed its efficacy was comparable to ticlopidine and clopidogrel without affecting bleeding time
J Cereb Blood Flow Metab. 2010 May;30(5):904-12
BALB/c mice
TNBS-induced chronic colitis model
Oral
10 mg/kg/day and 50 mg/kg/day
Once daily for 2 weeks
To evaluate the inhibitory effect of TM5275 on TNBS-induced intestinal fibrosis. Results showed that 50 mg/kg/day TM5275 significantly reduced collagen deposition and upregulated MMP-9 expression, thereby attenuating fibrosis.
Intest Res. 2020 Apr;18(2):219-228
C57BL/6 mice
TGF-β1-induced lung fibrosis model
Oral
40 mg/kg
Once daily for 10 days
TM5275 almost completely blocked TGF-β1-induced lung fibrosis, restored uPA and tPA activities, reduced collagen deposition and hydroxyproline content, and caused no significant body weight loss.
Am J Respir Cell Mol Biol. 2012 Jan;46(1):87-95
C57BL/6 mice
Streptozotocin (STZ)-induced diabetic mouse model
Oral
50 mg/kg/day
Once daily for 16 weeks
Improved kidney function and morphology, reduced albuminuria and mesangial expansion, and inhibited kidney fibrosis and inflammation in diabetic mice
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