WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H530684
CAS#: 1190221-43-2
Description: TM-5441, also known as EBP 883 and BMS-790052, is a potent plasminogen activator inhibitor-1 (PAI-1). TM-5441 inhibits several tumor cell lines with IC50 values between 9.7 and 60.3 μM. TM5441 protects against high-fat diet-induced obesity and adipocyte injury in mice.
Hodoodo Cat#: H530684
Name: TM-5441
CAS#: 1190221-43-2
Chemical Formula: C21H17ClN2O6
Exact Mass: 428.08
Molecular Weight: 428.825
Elemental Analysis: C, 58.82; H, 4.00; Cl, 8.27; N, 6.53; O, 22.39
Synonym: TM-5441; TM 5441; TM5441; BMS-790052; BMS-790052; BMS790052; EBP 883; EBP-883; EBP883.
IUPAC/Chemical Name: 5-chloro-2-(2-(2-((3-(furan-3-yl)phenyl)amino)-2-oxoethoxy)acetamido)benzoic acid
InChi Key: BGGMLMAPVODXAU-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H17ClN2O6/c22-15-4-5-18(17(9-15)21(27)28)24-20(26)12-30-11-19(25)23-16-3-1-2-13(8-16)14-6-7-29-10-14/h1-10H,11-12H2,(H,23,25)(H,24,26)(H,27,28)
SMILES Code: O=C(O)C1=CC(Cl)=CC=C1NC(COCC(NC2=CC=CC(C3=COC=C3)=C2)=O)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 428.83 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Ghosh AK, Rai R, Park KE, Eren M, Miyata T, Wilsbacher LD, Vaughan DE. A small molecule inhibitor of PAI-1 protects against doxorubicin-induced cellular senescence. Oncotarget. 2016 Nov 8;7(45):72443-72457. doi: 10.18632/oncotarget.12494. PubMed PMID: 27736799; PubMed Central PMCID: PMC5341920.
2: Piao L, Jung I, Huh JY, Miyata T, Ha H. A novel plasminogen activator inhibitor-1 inhibitor, TM5441, protects against high-fat diet-induced obesity and adipocyte injury in mice. Br J Pharmacol. 2016 Sep;173(17):2622-32. doi: 10.1111/bph.13541. Epub 2016 Jul 28. PubMed PMID: 27339909; PubMed Central PMCID: PMC4978161.
3: Jeong BY, Uddin MJ, Park JH, Lee JH, Lee HB, Miyata T, Ha H. Novel Plasminogen Activator Inhibitor-1 Inhibitors Prevent Diabetic Kidney Injury in a Mouse Model. PLoS One. 2016 Jun 3;11(6):e0157012. doi: 10.1371/journal.pone.0157012. eCollection 2016. PubMed PMID: 27258009; PubMed Central PMCID: PMC4892642.
4: Placencio VR, Ichimura A, Miyata T, DeClerck YA. Small Molecule Inhibitors of Plasminogen Activator Inhibitor-1 Elicit Anti-Tumorigenic and Anti-Angiogenic Activity. PLoS One. 2015 Jul 24;10(7):e0133786. doi: 10.1371/journal.pone.0133786. eCollection 2015. PubMed PMID: 26207899; PubMed Central PMCID: PMC4514594.
5: Tsuda K. Letter by Tsuda regarding article, "Plasminogen activator inhibitor-1 antagonist TM5441 attenuates Nω-nitro-L-arginine methyl ester-induced hypertension and vascular senescence". Circulation. 2014 Aug 26;130(9):e83. doi: 10.1161/CIRCULATIONAHA.113.007940. PubMed PMID: 25156921.
6: Eren M, Boe AE, Murphy SB, Place AT, Nagpal V, Morales-Nebreda L, Urich D, Quaggin SE, Budinger GR, Mutlu GM, Miyata T, Vaughan DE. PAI-1-regulated extracellular proteolysis governs senescence and survival in Klotho mice. Proc Natl Acad Sci U S A. 2014 May 13;111(19):7090-5. doi: 10.1073/pnas.1321942111. Epub 2014 Apr 28. PubMed PMID: 24778222; PubMed Central PMCID: PMC4024885.
7: Boe AE, Eren M, Murphy SB, Kamide CE, Ichimura A, Terry D, McAnally D, Smith LH, Miyata T, Vaughan DE. Plasminogen activator inhibitor-1 antagonist TM5441 attenuates Nω-nitro-L-arginine methyl ester-induced hypertension and vascular senescence. Circulation. 2013 Nov 19;128(21):2318-24. doi: 10.1161/CIRCULATIONAHA.113.003192. Epub 2013 Oct 3. PubMed PMID: 24092817; PubMed Central PMCID: PMC3933362.