OX2R-IN-1

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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。

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:

.......

Parameter	Units	Plasma	Brain tissuer
t_1/2,β(h)	t_1/2	min	9.63	14.85
t_max	min	5	40
C_max	μmol/L	29.40	0.199
AUC	μmol/L*min	1362.68	18.51
MRT	min	39.94	68.93

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.