L-745337

Names

[ CAS No. ]:
158205-05-1

[ Name ]:
L-745337

[Synonym ]:
N-[6-[(2,4-difluorophenyl)thio]-2,3-dihydro-1-oxo-1H-inden-5-yl]methanesulfonamide
N-[6-(2,4-difluorophenylthio)-1-oxoindan-5-yl]methanesulphonamide
5-Methanesulfonamido-6-(2,4-difluorophenylthio)-1-indanone
N-[6-(2,4-Difluoro-phenylsulfanyl)-1-oxo-indan-5-yl]-methanesulfonamide
L-745-337
N-[6-[(2,4-difluorophenyl)thio]-2,3-dihydro-1-oxo-1H-inden-5-yl]-methanesulfonamide
N-[6-[(2,4-difluorophenyl) thio]-2,3-dihydro-1-oxo-1H-inden-5-yl]methanesulfonamide
L-745337

Biological Activity

[Description]:

L-745337 is a selective cyclooxygenase-2 (COX2) inhibitor, with an IC50 of 2.3 nM, and shows anti-inflammatory activity.

[Related Catalog]:

Research Areas >> Inflammation/Immunology

[Target]

COX-2:2.3 nM (IC50)


[In Vivo]

In a rat model of postoperative pain, L-745337 (40-80 μg, intrathecal) coadministered with intrathecal morphine (0.5 nmol) increases the withdrawal thresholds in a dose-dependent manner. Adding 80 μg L-745337 to 1 nmol morphine produces an antiallodynic effect greater than that of morphine at twice the dose. L-745337 (0-30 mg/kg, s.c.) combined with intrathecal morphine results in the same antiallodynic response as morphine alone[1]. L-745,337 shows anti-inflammatory activity, with the effective-dose of 0.4 mg/kg, and the maximal anti-inflammation dose of 5 mg/kg in arthritic rats[2].

[References]

[1]. Kroin JS, et al. Cyclooxygenase-2 inhibition potentiates morphine antinociception at the spinal level in a postoperative pain model. Reg Anesth Pain Med. 2002 Sep-Oct;27(5):451-5.

[2]. Turull N, et al. Effect of the COX-2 selective inhibitor l-745,337 on inflammation and organ prostaglandin E2 (PGE2) levels in adjuvant arthritic rats. Inflammation. 2000 Dec;24(6):533-45.

[3]. Li CS, et al. Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. J Med Chem. 1995 Dec 8;38(25):4897-905.


[Related Small Molecules]

4-Acetamidophenol | Aspirin | Paradol | Ginsenoside Rg3 | Ginsenoside Compound K | Xanthohumol | Ibuprofen | Diclofenac | NS-398 | Meloxicam | Flufenamic Acid | Epicatechin | Salicylic acid | ketoprofen | Naproxen

Chemical & Physical Properties

[ Molecular Formula ]:
C16H13F2NO3S2

[ Molecular Weight ]:
369.40600

[ Exact Mass ]:
369.03000

[ PSA ]:
96.92000

[ LogP ]:
4.77020

Related Compounds