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GRP-60367 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GRP-60367 hydrochloride图片
CAS NO:1309241-34-6 (free base)
包装:5mg, 10mg, 25mg, 50mg
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品名称
GRP-60367 HCl
GRP60367
产品介绍

生物活性

GRP-60367 hydrochloride is a first-in-class potent and selective inhibitor of rabies virus (RABV) entry that specifically targets the RABV G protein. GRP-60367 inhibits entry of a subset of RABV strains. Resistance profiling of the chemotype revealed hot spots in conserved hydrophobic positions of the RABV G protein fusion loop that were confirmed in transient cell-to-cell fusion assays. Transfer of RABV G genes with signature resistance mutations into a recombinant VSV backbone resulted in the recovery of replication-competent virions with low susceptibility to the inhibitor.


化学数据

分子量389.92
分子式C21H27N3O2.HCl
CAS号1309241-34-6 (free base)
纯度>99%
溶解性(25°C)DMSO ≥ 100 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系Mouse neuronal N2a cells
方法Virus yield reduction assays. Mouse neuronal N2a cells (1.5 × 104 cells/well) were seeded in a 96-well plate format and incubated for 24 h. GRP-60367 was added in 3-fold serial dilutions, followed by infection of 6,000 focus-forming units (FFU) (MOI, 0.2 FFU/cell) of virus. Control wells without compound were infected in parallel with the same amount of inoculum. After 60 min, the inoculum was removed and replaced with 100 μl fresh DMEM with (treated) or without (controls) compound. Culture supernatants were collected after 48 h incubation at 34°C, and progeny virus titers were determined on N2a cells.
浓度100 nM, 1 uM, 10 uM, 100 uM, 1000 uM
处理时间48 h

动物实验
动物模型
配制
剂量
给药处理

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM2.5646 mL12.8231 mL25.6463 mL
5 mM0.5129 mL2.5646 mL5.1293 mL
10 mM0.2565 mL1.2823 mL2.5646 mL