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SCH 336

Names

[ CAS No. ]:
447459-51-0

[ Name ]:
SCH 336

[Synonym ]:
Methanesulfonamide, N-[(1S)-1-[4-[[4-methoxy-2-[(4-methoxyphenyl)sulfonyl]phenyl]sulfonyl]phenyl]ethyl]-
N-{(1S)-1-[4-({4-Methoxy-2-[(4-methoxyphenyl)sulfonyl]phenyl}sulfonyl)phenyl]ethyl}methanesulfonamide

Biological Activity

[Description]:

SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice[1].

[Related Catalog]:

Research Areas >> Inflammation/Immunology
Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor

[Target]

hCB2-R


[In Vitro]

SCH 336 (Sch.336) (0-10 µM) competes with [3H]CP55,940 for binding to human CB2 on Sf9 cell membranes with Ki of 1.8 nM, and decreases GTPγS binding on human CB2-containing membranes with an EC50 of 2 nM, decreases potency on CB1-containing membranes with EC50 of 200 nM[1]. SCH 336 inhibits BaF3/CB2 migration to 100 nM 2-AG with an IC50 of 34 nM[1].

[In Vivo]

SCH 336 (0.02, 0.2, 2.0 mg/kg; i.p.) significantly inhibits the migration of leukocytes[1]. Animal Model: Female B6D2/F1 mice (HU210)[1] Dosage: 0.02, 0.2, 2.0 mg/kg Administration: I.p. Result: Significantly inhibited the migration of leukocytes into the CCL2-soaked gel foam sponge.

[References]

[1]. Lunn CA, et al. A novel cannabinoid peripheral cannabinoid receptor-selective inverse agonist blocks leukocyte recruitment in vivo. J Pharmacol Exp Ther. 2006 Feb;316(2):780-8.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
756.6±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C23H25NO8S3

[ Molecular Weight ]:
539.64

[ Flash Point ]:
411.4±35.7 °C

[ Exact Mass ]:
539.074219

[ LogP ]:
3.91

[ Vapour Pressure ]:
0.0±2.5 mmHg at 25°C

[ Index of Refraction ]:
1.589


Related Compounds