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SCH-336

Catalog No. T24771 CAS 447459-51-0

SCH-336 is a CB2 receptor agonist (Ki-1.8 nM, EC50-2 nM) with effective, selective, and oral activity. SCH-336 is also bioactive against CB1 receptor, and is 100 times more selective to CB2 receptor than CB1. SCH-336 reduced the binding of guanosine 5' -3-o -(sulfur) triphosphate to the membrane containing hCB, inhibited BaF3/CB2 cell migration, inhibited leukocyte migration in mouse delayed hypersensitivity models, and inhibited antigen-induced pulmonary eosinophilia in mouse allergy models.

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SCH-336, CAS 447459-51-0

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SCH-336 is a CB2 receptor agonist (Ki-1.8 nM, EC50-2 nM) with effective, selective, and oral activity. SCH-336 is also bioactive against CB1 receptor, and is 100 times more selective to CB2 receptor than CB1. SCH-336 reduced the binding of guanosine 5' -3-o -(sulfur) triphosphate to the membrane containing hCB, inhibited BaF3/CB2 cell migration, inhibited leukocyte migration in mouse delayed hypersensitivity models, and inhibited antigen-induced pulmonary eosinophilia in mouse allergy models.
Targets&IC50	human CB2:2nM(EC50), BaF3/CB2:34nM, human CB1:200nM(EC50)
In vitro	SCH 336 (also known as Sch.336) exhibits competitive binding with [3H]CP55,940 to human CB2 receptors on Sf9 cell membranes, with a Ki value of 1.8 nM. It reduces GTPγS binding on membranes containing human CB2 receptors, with an EC50 of 2 nM. However, its potency decreases on membranes containing CB1 receptors, with an EC50 of 200 nM [1]. Moreover, SCH 336 inhibits the migration of BaF3/CB2 cells towards 100 nM 2-AG, with an IC50 of 34 nM [1].
In vivo	In in vivo studies, when administered intraperitoneally (i.p.) at doses of 0.02-2.0 mg/kg, SCH 336 significantly inhibits leukocyte migration [1].

Molecular Weight	539.64
Formula	C23H25NO8S3
CAS No.	447459-51-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 90.0 mg/mL (48.6 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Lunn CA, et al. A novel cannabinoid peripheral cannabinoid receptor-selective inverse agonist blocks leukocyte recruitment in vivo. J Pharmacol Exp Ther. 2006;316(2):780-788.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SCH-336 447459-51-0 GPCR/G Protein Cannabinoid Receptor SCH-225336 Inhibitor inhibitor inhibit

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