SB-568849
SB-568849 Basic information
- Product Name:
- SB-568849
- Synonyms:
-
- SB-568849
- [1,1'-Biphenyl]-4-carboxamide, N-[4-[2-(diethylamino)ethoxy]-3-methoxyphenyl]-N-methyl-4'-(trifluoromethyl)-
- SB 568849,SB568849
- CAS:
- 395679-53-5
- MF:
- C28H31F3N2O3
- MW:
- 500.55
- Mol File:
- 395679-53-5.mol
SB-568849 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
SB-568849 Usage And Synthesis
Uses
SB-568849 is a melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pKi of 7.7.
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. DOI:10.1016/j.bmcl.2006.06.061
[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. DOI:10.1046/j.1365-2826.2003.00997.x
[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. DOI:10.1016/j.bmcl.2006.06.056
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