395679-53-5
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- CAS号:
- 395679-53-5
- 英文名:
- SB-568849
- 英文别名:
- SB-568849;SB 568849,SB568849;[1,1'-Biphenyl]-4-carboxamide, N-[4-[2-(diethylamino)ethoxy]-3-methoxyphenyl]-N-methyl-4'-(trifluoromethyl)-
- 中文名:
- 395679-53-5
- 中文别名:
- 化合物 T16852
- CBNumber:
- CB23384785
- 分子式:
- C28H31F3N2O3
- 分子量:
- 500.55
- MOL File:
- 395679-53-5.mol
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395679-53-5化学性质
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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395679-53-5性质、用途与生产工艺
SB-568849 是一种黑色素浓缩激素受体 1 (MCH R1) 拮抗剂，pKi 值为 7.7。
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.
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.
395679-53-5
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395679-53-5, 395679-53-5 相关搜索:
- 化合物 T16852
- 395679-53-5
- SB 568849,SB568849
- [1,1'-Biphenyl]-4-carboxamide, N-[4-[2-(diethylamino)ethoxy]-3-methoxyphenyl]-N-methyl-4'-(trifluoromethyl)-
- SB-568849