1. GPCR/G Protein Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. OX2R-IN-1

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,活性分子半衰期短。

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OX2R-IN-1 Chemical Structure

OX2R-IN-1 Chemical Structure

CAS No. : 2639148-08-4

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查看 Orexin Receptor (OX Receptor) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life[1].

IC50 & Target

OX2 Receptor

 

体外研究
(In Vitro)

OX2R-IN-1 (compound 15) has low cytotoxic withIC50 values 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1].

Cell Line: CHO-K1 cell line
Concentration: 100-1000 µM
Incubation Time: 24h
Result: Exhibited low cytotoxic with IC50values of 484 μM
体内研究
(In Vivo)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
t1/2,β (h)t1/2 min 9.63 14.85
tmax min 5 40
Cmax 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
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
OX2R-IN-1
目录号:
HY-149014
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