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SB-568849

CAS No. : 395679-53-5

MCE 站：SB-568849

产品活性：SB-568849 是一种黑色素浓缩激素受体 1 (MCH R1) 拮抗剂，pK_i 值为 7.7。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：MCHR1 (GPR24)

In Vitro: SB-568849 is a selective SLC-1 antagonist with a pK_i of 7.7 as determined in radioligand binding displacement assays; coincubation of tissue with 1 μM SB-568849 for 45 min completely inhibits the MCH induced increase in corticotropin-releasing factor (CRF) release to basal levels without causing any effect on its own. The only reported MCH receptor in the rat is SLC-1, a G protein coupled receptor found throughout the brain and periphery.

In Vivo: SB-568849 (Compound 15h) possesses good receptor affinity and selectivity. SB-568849 proves to be an antagonist with stability in vivo, an acceptable brain–blood ratio and oral bioavailability. SB-568849 retains affinity, demonstrates greater in vivo stability (CL_b=16 mL/min/kg) and shows an acceptable brain-blood ratio of 1. SB-568849 also shows >30-fold selectivity over a wide range of monoamine receptors and is an antagonist in the FLIPR assay with a pK_b of 7.7.

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