BMS-248360
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- CAS号:
- 254737-87-6
- 英文名:
- BMS-248360
- 英文别名:
- BMS-248360;BMS 248360,BMS248360;BMS-248360 >=98% (HPLC);[1,1'-Biphenyl]-2-sulfonamide, 4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-N-(3,4-dimethyl-5-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-
- 中文名:
- BMS-248360
- 中文别名:
- 化合物 T14672
- CBNumber:
- CB04920739
- 分子式:
- C36H45N5O5S
- 分子量:
- 659.84
- MOL File:
- 254737-87-6.mol
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BMS-248360性质、用途与生产工艺
BMS-248360 是一种高效、有口服活性的血管紧张素 II 受体 (AT1) 和内皮素 A (ETA) 受体双拮抗剂，对 hAT1 和 hETA 受体作用的 Ki 值分别为 10 nM 和 1.9 nM。BMS-248360 具有抗高血压作用。
Ki: 10 nM (hAT1), 1.9 nM (hETA receptor), 6.0 nM (rAT1), 1.9 nM(r
ET
A
receptor)
BMS-248360 shows activity against rat AT1 and rat ET
A
receptor, with K
i
s of 6.0 nM and 1.9 nM, respectively.
BMS-248360 shows no activity against AT2 and ET
B
receptor subtypes.
BMS-248360 is found to be orally bioavailable in rats (%F=38) with excellent oral exposure (C
max
)=3.1 µM) and reasonable elimination profile (T
1/2
=5.5 hours).
BMS-248360 (30 µmol/kg, 100 µmol/kg; p.o.) blocks the hypertensive effects of intravenously administered AII.
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Animal Model:
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Male Rats
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Dosage:
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30 µM/kg, 100 µM/kg
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Administration:
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Oral administration
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Result:
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Blocked the hypertensive effects of intravenously administered AII.
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Animal Model:
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Male Rats
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Dosage:
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10 µM/kg
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Administration:
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Oral administration
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Result:
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T
1/2
= 5.5 hours
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BMS-248360
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254737-87-6, BMS-248360 相关搜索:
- 化合物 T14672
- 254737-87-6
- BMS 248360,BMS248360
- BMS-248360 >=98% (HPLC)
- [1,1'-Biphenyl]-2-sulfonamide, 4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-N-(3,4-dimethyl-5-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-
- BMS-248360