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Chemical Structure| 1103926-82-4 Chemical Structure| 1103926-82-4

Structure of TM5275 sodium
CAS No.: 1103926-82-4

Chemical Structure| 1103926-82-4

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TM-5275 sodium salt is an inhibitor of plasminogen activator inhibitor-1 with antithrombotic activity in nonhuman primates.

Synonyms: TM 5275; TM 5275 sodium salt

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Product Details of TM5275 sodium

CAS No. :1103926-82-4
Formula : C28H27ClN3NaO5
M.W : 543.97
SMILES Code : O=C([O-])C1=CC(Cl)=CC=C1NC(COCC(N2CCN(C(C3=CC=CC=C3)C4=CC=CC=C4)CC2)=O)=O.[Na+]
Synonyms :
TM 5275; TM 5275 sodium salt
MDL No. :MFCD28396414
InChI Key :JSHSGBIWNPQCQZ-UHFFFAOYSA-M
Pubchem ID :53240409

Safety of TM5275 sodium

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302-H319-H332-H372-H400
Precautionary Statements:P260-P264-P270-P273-P280-P301+P312+P330-P304+P312-P305+P351+P338-P314-P337+P313-P391-P501
Class:9
UN#:3077
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Rat hepatic stellate cells (HSC-T6) 100 µM 12 hours 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

In Vivo:

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 PLoS One. 2016 Jun 3;11(6):e0157012

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.19mL

1.84mL

0.92mL

18.38mL

3.68mL

1.84mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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