New Products for August 2007

Highly selective CB₂ agonist
Gp 1a
CB₂ receptor agonist that displays > 9800-fold selectivity over CB₁ receptors. Increases P-ERK1/2 expression in HL-60 cells in vitro.
CB₂ Related Products: L-759,633 L-759,656 CB 65

Potent and selective CXCR2 antagonist
SB 225002
CXCR2 chemokine receptor antagonist (IC₅₀ = 22 nM) that displays > 150-fold selectivity over CXCR1 receptors. Causes inhibition of IL-8 and GROα-mediated calcium mobilisation in HL60 cells (IC₅₀ values are 8 and 10 nM respectively). CXCR2 Related Products: ZK 756326 RS 504393 DAPTA

Potent and selective P2Y₆ agonist
3-Phenacyl UDP disodium salt
Potent and selective P2Y₆ receptor agonist (EC₅₀ values are 7, > 1000 and > 10000 nM for P2Y₆, P2Y₂ and P2Y₄ receptors respectively).
P2Y₆ Related Products: MRS 2578

Selective AMPA antagonist
YM 90K hydrochloride
Displays 26-fold and > 440-fold selectivity over kainate and NMDA receptors respectively. Neuroprotective; delays neuronal death in a global ischaemia model and cerebral infarction in a focal ischaemia model.
AMPA Related Products: ZK 200775 GYKI 52466

Potent and selective VPAC₂ agonist
Bay 55-9837
Selective VPAC₂ receptor agonist (IC₅₀ values are 60, 8700 and > 10000 nM for VPAC₂, VPAC₁ and PAC₁ receptors respectively). Stimulates glucose-dependent insulin secretion in isolated human pancreatic islets.
VPAC₂ Related Products: [Ala^11,22,28]VIP

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