123653-11-2 Usage
Description
NS-398 is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 μM, respectively. The IC50 values for ovine COX-1 and -2 are 220 and 0.15 μM, respectively.
Uses
NS-398 is a selective Cox-2 inhibitor neuroprotective agent.
Definition
ChEBI: A C-nitro compound that is N-methylsulfonyl-4-nitroaniline bearing an additional cyclohexyloxy substituent at position 2.
Biological Activity
Selective cyclooxygenase-2 inhibitor (IC 50 values are 3.8 and > 100 μ M for COX-2 and COX-1 respectively). Induces apoptosis in colorectal tumor cells and elevates COX-2 protein expression in vitro . Orally active and non-ulcerogenic analgesic and anti-inflammatory in vivo .
references
[1]. futaki n, takahashi s, yokoyama m, et al. ns-398, a new anti-inflammatory agent, selectively inhibits prostaglandin g/h synthase/cyclooxygenase (cox-2) activity in vitro. prostaglandins, 1994, 47(1): 55-59.[2]. elder dj, halton de, crew te, et al. apoptosis induction and cyclooxygenase-2 regulation in human colorectal adenoma and carcinoma cell lines by the cyclooxygenase-2-selective non-steroidal anti-inflammatory drug ns-398. int j cancer, 2000, 86(4): 553-560.[3]. mack strong ve, mackrell pj, concannon em, et al. ns-398 treatment after trauma modifies nf-kappab activation and improves survival. j surg res, 2001, 98(1): 40-46.
Check Digit Verification of cas no
The CAS Registry Mumber 123653-11-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,2,3,6,5 and 3 respectively; the second part has 2 digits, 1 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 123653-11:
(8*1)+(7*2)+(6*3)+(5*6)+(4*5)+(3*3)+(2*1)+(1*1)=102
102 % 10 = 2
So 123653-11-2 is a valid CAS Registry Number.
InChI:InChI=1/C13H18N2O5S/c1-21(18,19)14-12-8-7-10(15(16)17)9-13(12)20-11-5-3-2-4-6-11/h7-9,11,14H,2-6H2,1H3
123653-11-2Relevant articles and documents
SULFONANILIDE ANALOGS AS SELECTIVE AROMATASE MODULATORS
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Page/Page column title page; 18-19; 1/15, (2010/11/28)
Compounds and methods suppressing aromatase activity expression in cancer cells. Provided are compounds are those of formula I: wherein R1 may be alkyl, cycloakyl, haloalkyl, aryl, substituted aryl, haloaryl, alkoxy, alkylaryl, and arylalkyl; R2 is H, alk
Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition
Su, Bin,Diaz-Cruz, Edgar S.,Landini, Serena,Brueggemeier, Robert W.
, p. 1413 - 1419 (2007/10/03)
Aromatase is a particularly attractive target in the treatment of estrogen receptor positive breast cancer. Aromatase levels in breast cancer cells are enhanced by prostaglandins and reduced by COX inhibitors. The synthesis and biological evaluation of a
Antiangiogenic combination therapy for the treatment of cancer
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, (2008/06/13)
The present invention provides combinations of a DNA topoisomerase I inhibiting agent and a selective COX-2 inhibiting agent for preventing, treating, and/or reducing the risk of developing a neoplasia disorder in a mammal.
