New Products for September 2009

Potent and selective CB₂ agonist
3088 l HU 308
K_i values are 22.7 nM and > 10 μM for CB₂ and CB₁ receptors respectively, EC₅₀ = 5.57 nM. Displays antiallodynic activity in the rat hindpaw incision model of postoperative pain.
Related Products: JTE 907 GP 1a AM 630

Potent, orally active DPP-IV inhibitor
3506 l NVP DPP 728
K_i = 11 nM, IC₅₀ = 14 nM. Displays > 15 000-fold selectivity over DPP-II and a range of proline-cleaving proteases. Exhibits antidiabetic activity in vivo.
Related Products: DPPI 1c K 579

Diacyl glycerolacyltransferase 1 (DGAT-1) inhibitor
3587 l A 922500
IC₅₀ values are 7 and 24 nM at human and mouse DGAT-1 respectively. Devoid of activity at DGAT-2, ACAT1 or ACAT2. Induces significant weight loss without altering food intake, and decreases liver and plasma triglyceride levels in vivo. Orally active.

Potent Raf kinase inhibitor
3572 l L-779,450
IC₅₀ = 10 nM. Ddisplays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively. Suppresses DNA synthesis and induces apoptosis in cells that proliferate in response to Raf-1 and A-Raf but not B-Raf.
Related Products: GW 5074 ZM 336372

Selective FAAH inhibitor
3307 l PF 750
IC₅₀ = 16.2 nM. Displays no activity at a range of other serine hydrolases. Selectively inhibits FAAH within the central nervous system. Orally active.
Related Products: JNJ 1661010 MAFP AACOCF₃

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