395679-53-5

395679-53-5 structure

395679-53-5 structure

Name: SB-568849
Chemical Name: SB-568849
CAS Number: 395679-53-5
Molecular Formula: C₂₈H₃₁F₃N₂O₃
Molecular Weight: 500.55
Catalog: Signaling Pathways GPCR/G Protein MCHR1 (GPR24)
Create Date: 2018-04-17 17:29:26
Modify Date: 2024-01-23 18:37:02
SB-568849 is a melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pKi of 7.7.

Name	SB-568849

Description	SB-568849 is a melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pKi of 7.7.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> MCHR1 (GPR24) Research Areas >> Metabolic Disease
Target	MCH R1 receptor[1]
In Vitro	SB-568849 is a selective SLC-1 antagonist with a pKi 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[2].
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 (CLb=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 pKb of 7.7[3].
References	[1]. Witty DR, et al. Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4872-8. [2]. Kennedy AR, et al. Effect of direct injection of melanin-concentrating hormone into the paraventricular nucleus: further evidence for a stimulatory role in the adrenal axis via SLC-1. J Neuroendocrinol. 2003 Mar;15(3):268-72. [3]. Witty DR, et al. SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4865-71.

Molecular Formula	C₂₈H₃₁F₃N₂O₃
Molecular Weight	500.55
Storage condition	2-8℃