134448-10-5 Usage
Uses
Different sources of media describe the Uses of 134448-10-5 differently. You can refer to the following data:
1. CA-074 is a potent and specific inhibitor of cathepsin B in vitro.
2. Inhibitor of Cathepsin B.
Biological Activity
ca-074, a specific cathepsin b inhibitor, also abolished the neurotoxic effects caused by abeta42-activated bv2 cell [1]. co-treatment of cultures with the cathepsin b inhibitors ca-074 or z-fa-fmk suppressed the cytostatic effects of tpa and activation of pro-upa [2]. administration of ca-074 suppresses the response to exogenous antigens, such as hepatitis b virus antigen, ovalbumin and leishmania major antigen, and induces switching of the helper t cell responses from th-2 to th-1 of cd4+ t cell, thereby down regulating the production of ige and igg1 [3]. pharmacological inhibition of cat b in catb(+/+) mice with l-3-trans-(propylcarbamoyl)oxirane-2-carbonyl-lisoleucyl-l-proline (ca-074 me) also reduced tnf-alpha-induced liver damage. [4] administration of cathepsin b inhibitors, e-64, ca-074 and vitamin b6, caused the strong suppression of the th-2 type immune responses .inhibitor of cathepsin b (ki = 2-5 nm). displays selectivity over cathepsins h and l (ki = 40-200 μm). shown to reduce bone metastasis in a 4t1.2 breast cancer model.
references
1. identification of cathepsin b as a mediator of neuronal death induced by abeta-activated microglial cells using a functional genomics approach. gan, l., ye, s., chu, a., anton, k., yi, s., vincent, v.a., von schack, d., chin, d., murray, j., lohr, s., patthy, l., gonzalez-zulueta, m., nikolich, k., urfer, r. j. biol. chem. (2004) 2. phorbol ester activation of a proteolytic cascade capable of activating latent transforming growth factor-betal a process initiated by the exocytosis of cathepsin b. guo, m., mathieu, p.a., linebaugh, b., sloane, b.f., reiners, j.j. j. biol. chem. (2002) 3. insights into the roles of cathepsins in antigen processing and presentation revealed by specific inhibitors. katunuma, n., matsunaga, y., himeno, k., hayashi, y. biol. chem. (2003) 4. cathepsin b knockout mice are resistant to tumor necrosis factor-alpha-mediated hepatocyte apoptosis and liver injury: implications for therapeutic applications. guicciardi, m.e., miyoshi, h., bronk, s.f., gores, g.j. am. j. pathol. (2001)
Check Digit Verification of cas no
The CAS Registry Mumber 134448-10-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,4,4,4 and 8 respectively; the second part has 2 digits, 1 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 134448-10:
(8*1)+(7*3)+(6*4)+(5*4)+(4*4)+(3*8)+(2*1)+(1*0)=115
115 % 10 = 5
So 134448-10-5 is a valid CAS Registry Number.
InChI:InChI=1/C18H29N3O6/c1-4-8-19-15(22)13-14(27-13)16(23)20-12(10(3)5-2)17(24)21-9-6-7-11(21)18(25)26/h10-14H,4-9H2,1-3H3,(H,19,22)(H,20,23)(H,25,26)
134448-10-5Relevant articles and documents
NOVEL DRUGS FOR DEMENTIA
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Example 3, (2008/06/13)
The invention is directed to compounds that are prodrugs containing a chemical delivery system (CDS) moiety and a cysteine protease inhibitor moiety. The CDS moiety targets the prodrug to the brain or central nervous system. The cysteine protease inhibitor inhibits cysteine proteases upon release from the prodrug. Cysteine protease inhibitors are effective for treating dementia, Alzheimer's disease and vascular dementia. Targeting the brain or central nervous system offers significant advantages in treating these conditions and diseases. A preferred CDS prodrug is a dihydrotrigoneline CDS moiety coupled to an epoxysuccinyl peptide cysteine protease inhibitor moiety.
