New Products for October 2009

Potent, competitive NPY Y₁ antagonist
3242 l BMS 193885
K_i = 3.3 nM, IC₅₀ = 5.9 nM. Displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over σ₁, α₁, Y₂, Y₄ and Y₅ receptors respectively. Reduces food intake and body weight via central Y₁ inhibition and is brain penetrant.
Related Products: BIBO 3304 BIBP 3226 [Leu³¹,Pro³⁴]-Neuropeptide Y (human, rat)

Peptide cleaved from PAR₁ upon receptor activation
3554 l Parstatin (mouse)
Cell-permeable peptide cleaved from protease-activated receptor 1 (PAR₁) upon receptor activation. Attenuates endothelial cell migration and proliferation (IC₅₀ ~ 20 μM), and induces cell cycle arrest.
Related Products: TFLLR-NH₂ TRAP-6 SCH 79797

Selective σ₁ antagonist
3133 l NE 100
K_i = 0.86 nM. Displays > 55-fold selectivity over σ₂ receptors and > 6000-fold selectivity over D₁, D₂, 5-HT_1A, 5-HT₂ and PCP receptors. Exhibits reversible binding (K_d = 1.2 nM) and displays antipsychotic activity in vivo. Orally active.
Related Products: BD 1047 (+)-SK&F 10047 PRE-084

Reverse transcriptase inhibitor
3666 l Tenofovir
Selectively inhibits HIV reverse transcriptase (RNA-dependent DNA polymerase). Prevents cytotoxicity in SIV-infected C-8166 cells in vitro (IC₅₀ = 1.5 μM). Used clinically as an antiviral agent.
Related Products: Acyclovir DAPTA

Potent and selective NPY Y₅ antagonist
3432 l S 25585
IC₅₀ values are 5.4, > 1000, > 10 000 and > 10 000 nM at Y₅, Y₁, Y₂ and Y₄ receptors respectively. Significantly inhibits NPY-induced feeding but not through blockade of Y₅ receptors.
Related Products: L-152,804 [cPP^1-7,NPY^19-23,Ala³¹,Aib³²,Gln³⁴] - hPancreatic Polypeptide CGP 71683

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