NBI-74330|855527-92-3|-陌孚医药/Medlife

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NBI-74330

目录号: PL04414 纯度: ≥99%

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。

CAS No. :855527-92-3

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中文名称	NBI-74330
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;NBI-74330
英文名称	NBI-74330
英文别名	N-{1-[3-(4-Ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin- 2-yl]ethyl}-2-[4-fluoro-3-(trifluoromethyl)phenyl]-N-(3-pyridinyl methyl)acetamide;NBI 74330;N-[1-[3-(4-ethoxyphenyl)-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-2-[4-fluoro-3-(trifluoromethyl)phenyl]-N-(pyridin-3-ylmethyl)acetamide;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;N-1-[(3-4(-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)be
Cas No.	855527-92-3
分子式	C₃₂H₂₇F₄N₅O₃
分子量	605.58
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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，K_i 值分别为 1.5 和 3.2 nM。
生物活性	NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (I)CXCL10 and (I)CXCL11 specific binding with K i of 1.5 and 3.2 nM, respectively.
性状	Solid
IC50 & Target[1][2]	[I]CXCL10-CXCR3 1.5 nM (Ki, in CXCR3-CHO cell membranes) [I]CXCL11-CXCR3
体外研究(In Vitro)	BI-74330 demonstrates potent inhibition of [I]CXCL11 specific binding to membranes prepared from transfected CHO cells expressing CXCR3 (CXCR3-CHO) (Ki=3.6 nM). NBI-74330 is 12- and 3.5-fold more potent than CXCL9 (Ki=45.2 nM) and CXCL10 (Ki=12.5 nM), respectively, at inhibiting [I]CXCL11 binding to CXCR3-CHO cell membranes. NBI-74330 inhibits calcium mobilization in response to CXCL11 and CXCL10 with an IC50 value of 7 nM for both ligands used at their EC80 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 [S]GTPγS binding in membranes of cells endogenously expressing CXCR3 (H9 cells, IC50 value 5.5 nM). BI-74330 inhibits CXCL11-induced chemotaxis in these cells with an IC50
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Heise CE, et al. Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. J Pharmacol Exp Ther. 2005 Jun;313(3):1263-71. [2]. Jopling LA, et al. Analysis of the pharmacokinetic/pharmacodynamic relationship of a small molecule CXCR3 antagonist, NBI-74330, using a murine CXCR3 internalization assay. Br J Pharmacol. 2007 Dec;152(8):1260-71.

溶解度数据	In Vitro: DMSO : 100 mg/mL (165.13 mM; Need ultrasonic)配制储备液

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