| Identification | Back Directory | [Name]
SB-568849 | [CAS]
395679-53-5 | [Synonyms]
SB-568849
[1,1'-Biphenyl]-4-carboxamide, N-[4-[2-(diethylamino)ethoxy]-3-methoxyphenyl]-N-methyl-4'-(trifluoromethyl)- | [Molecular Formula]
C28H31F3N2O3 | [MDL Number]
MFCD30533350 | [MOL File]
395679-53-5.mol | [Molecular Weight]
500.55 |
| Hazard Information | Back Directory | [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]. | [storage]
Store at -20°C | [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 |
|
| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
|