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OX2R-IN-1
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。
OX2R-IN-1图片
CAS NO:2639148-08-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
OX2R-IN-1(compound 15) 是一种 OX2R 拮抗剂(一种潜在的 OX2R 结合剂) ,具有低细胞毒性,IC50值为 484 μM。OX2R-IN-1 可穿过血脑屏障,药物半衰期短。
生物活性

OX2R-IN-1 (compound 15) is a low cytotoxicity profileOX2R-IN-1antagonist (a potential OX2R binder) with anIC50value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life[1].

IC50& Target

IC50: 484 μM (OX2R)

体外研究
(In Vitro)

OX2R-IN-1 (compound 15) has low cytotoxic withIC50values of 484 μM. OX2R-IN-1 (compound 15) is significant and dose-dependently reduce the signal of orexin A-evoked response (0.2 μM) in CHO-K1 cell line. OX2R-IN-1 (compound 15) has uncertain permeation through the BBB, since the PAMPA assay is limited by several drawbacks[1].

Cell Cytotoxicity Assay[1].

Cell Line:CHO-K1 cell line
Concentration:100-1000 μM
Incubation Time:24h
Result:Exhibited low cytotoxic withIC50values of 484 μM
体内研究
(In Vivo)

OX2R-IN-1 (compound 15) has a short half-life and poor bioavailability.

Animal Model:Albino male Wistar rats[1]
Dosage:75 mg/kg
Administration:OX2R-IN-1 (75 mg/kg; intraperitoneal injection) blood samples are collected at 0, 5, 10, 20, 30, 40, 60, 90, 120 and 240 min with a short half-life and poor bioavailability
Result:.......
ParameterUnitsPlasmaBrain tissuer
t1/2,β(h)t1/2min9.6314.85
tmaxmin540
Cmaxμmol/L29.400.199
AUCμmol/L*min1362.6818.51
MRTmin39.9468.93
分子量

457.97

Formula

C20H28ClN3O5S

CAS 号

2639148-08-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.