网站主页 >> CAS数据库列表 >> N-[(1R)-1-[3-(4-乙氧基苯基)-3,4-二氢-4-氧代吡啶并[2,3-D]嘧啶-2-基]乙基]-4-氟-N-(3-吡啶基甲基)-3-(三氟甲基)苯乙酰胺
N-[(1R)-1-[3-(4-乙氧基苯基)-3,4-二氢-4-氧代吡啶并[2,3-D]嘧啶-2-基]乙基]-4-氟-N-(3-吡啶基甲基)-3-(三氟甲基)苯乙酰胺
|
|
- CAS号:
- 855527-92-3
- 英文名:
- NBI-74330
- 英文别名:
- NBI-74330;N-[(1R)-1-[3-(4-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)benzeneacetamide;(R)-N-(1-(3-(4-Ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl)ethyl)-2-(4-fluoro-3-(trifluoromethyl)phenyl)-N-(pyridin-3-ylmethyl)acetamide;Benzeneacetamide, N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)-
- 中文名:
- N-[(1R)-1-[3-(4-乙氧基苯基)-3,4-二氢-4-氧代吡啶并[2,3-D]嘧啶-2-基]乙基]-4-氟-N-(3-吡啶基甲基)-3-(三氟甲基)苯乙酰胺
- 中文别名:
- N-[(1R)-1-[3-(4-乙氧基苯基)-3,4-二氢-4-氧代吡啶并[2,3-D]嘧啶-2-基]乙基]-4-氟-N-(3-吡啶基甲基)-3-(三氟甲基)苯乙酰胺;(R)-N-(1-(3-(4-乙氧基苯基)-4-氧代-3,4-二氢吡啶并[2,3-D]嘧啶-2-基)乙基)-2-(4-氟-3-(三氟甲基)苯基)-N-(吡啶-3-基甲基)乙酰胺
- CBNumber:
- CB62628189
- 分子式:
- C32H27F4N5O3
- 分子量:
- 605.58
- MOL File:
- 855527-92-3.mol
|
|
|
N-[(1R)-1-[3-(4-乙氧基苯基)-3,4-二氢-4-氧代吡啶并[2,3-D]嘧啶-2-基]乙基]-4-氟-N-(3-吡啶基甲基)-3-(三氟甲基)苯乙酰胺化学性质
-
沸点:
-
752.5±70.0 °C(Predicted)
-
|
-
密度:
-
1.32±0.1 g/cm3(Predicted)
-
|
-
储存条件:
-
Store at -20°C
-
|
-
溶解度:
-
DMSO:100.0(Max Conc. mg/mL);165.1(Max Conc. mM)
-
|
-
酸度系数(pKa):
-
4?+-.0.11(Predicted)
-
|
-
形态:
-
Powder
-
|
-
颜色:
-
Light yellow to yellow
-
|
N-[(1R)-1-[3-(4-乙氧基苯基)-3,4-二氢-4-氧代吡啶并[2,3-D]嘧啶-2-基]乙基]-4-氟-N-(3-吡啶基甲基)-3-(三氟甲基)苯乙酰胺性质、用途与生产工艺
NBI-74330 是一种有效的 CXCR3 拮抗剂,能够抑制 (125I)CXCL10 和 (125I)CXCL11 的特异性结合,Ki 值分别为 1.5 和 3.2 nM。
[
125
I]CXCL10-CXCR3
1.5 nM (Ki, in CXCR3-CHO cell membranes)
|
[
125
I]CXCL11-CXCR3
3.2 nM (Ki, in CXCR3-CHO cell membranes)
|
BI-74330 demonstrates potent inhibition of [
125
I]CXCL11 specific binding to membranes prepared from transfected CHO cells expressing CXCR3 (CXCR3-CHO) (K
i
=3.6 nM). NBI-74330 is 12- and 3.5-fold more potent than CXCL9 (K
i
=45.2 nM) and CXCL10 (K
i
=12.5 nM), respectively, at inhibiting [
125
I]CXCL11 binding to CXCR3-CHO cell membranes. NBI-74330 inhibits calcium mobilization in response to CXCL11 and CXCL10 with an IC
50
value of 7 nM for both ligands used at their EC
80
concentrations (1 nM for CXCL11 and 30 nM for CXCL10). NBI-74330 specifically inhibits CXCR3-mediated calcium mobilization. NBI-74330 also dose-dependently inhibits CXCL11-induced [
35
S]GTPγS binding in membranes of cells endogenously expressing CXCR3 (H9 cells, IC
50
value 5.5 nM). BI-74330 inhibits CXCL11-induced chemotaxis in these cells with an IC
50
of 3.9 nM. NBI-74330 (30-300 nm, 1-10 μM) produces concentration-dependent, parallel rightward shifts of the CXCL11 E/[A] curve with no significant change in the E/[A] curve maximal response.
NBI-74330 (100 mg/kg) results in the formation of an N-oxide metabolite, also an antagonist of CXCR3, in mice. Mice treated with 100 mg/kg NBI-74330 (in 1% Na Doc in 0.5% 400Cp Methylcellulose) result in serum concentrations of approximately 1 μM. This concentration is sufficient to fully block the CXCR3 receptor in vivo.
N-[(1R)-1-[3-(4-乙氧基苯基)-3,4-二氢-4-氧代吡啶并[2,3-D]嘧啶-2-基]乙基]-4-氟-N-(3-吡啶基甲基)-3-(三氟甲基)苯乙酰胺
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/04/30 | HY-15320 | NBI-74330 | | 1 mg | 681元 |
2024/04/30 | HY-15320 | N-[(1R)-1-[3-(4-乙氧基苯基)-3,4-二氢-4-氧代吡啶并[2,3-D]嘧啶-2-基]乙基]-4-氟-N-(3-吡啶基甲基)-3-(三氟甲基)苯乙酰胺 NBI-74330 | 855527-92-3 | 5mg | 1500元 |
N-[(1R)-1-[3-(4-乙氧基苯基)-3,4-二氢-4-氧代吡啶并[2,3-D]嘧啶-2-基]乙基]-4-氟-N-(3-吡啶基甲基)-3-(三氟甲基)苯乙酰胺
生产厂家
855527-92-3, N-[(1R)-1-[3-(4-乙氧基苯基)-3,4-二氢-4-氧代吡啶并[2,3-D]嘧啶-2-基]乙基]-4-氟-N-(3-吡啶基甲基)-3-(三氟甲基)苯乙酰胺 相关搜索:
- C32H27F4N5O3
- (R)-N-(1-(3-(4-乙氧基苯基)-4-氧代-3,4-二氢吡啶并[2,3-D]嘧啶-2-基)乙基)-2-(4-氟-3-(三氟甲基)苯基)-N-(吡啶-3-基甲基)乙酰胺
- N-[(1R)-1-[3-(4-乙氧基苯基)-3,4-二氢-4-氧代吡啶并[2,3-D]嘧啶-2-基]乙基]-4-氟-N-(3-吡啶基甲基)-3-(三氟甲基)苯乙酰胺
- 855527-92-3
- (R)-N-(1-(3-(4-Ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl)ethyl)-2-(4-fluoro-3-(trifluoromethyl)phenyl)-N-(pyridin-3-ylmethyl)acetamide
- Benzeneacetamide, N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)-
- N-[(1R)-1-[3-(4-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)benzeneacetamide
- NBI-74330