1. GPCR/G Protein
  2. Angiotensin Receptor
  3. KR31173

KR31173 是一种 AT1 拮抗剂,其 IC50 为 3.27 nM。KR31173 经 11C 同位素标记后可用作正电子发射断层扫描 (PET) 示踪剂。KR31173 在小鼠体内表现出良好的生物分布和药理特性。KR31173 选择性地与 CD-1 小鼠中已知含有高密度 AT1 血管紧张素受体的器官结合。

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KR31173 Chemical Structure

KR31173 Chemical Structure

CAS No. : 260554-07-2

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生物活性

KR31173 is an AT1 antagonist with an IC50 of 3.27  nM. KR31173 can be used as a positron emission tomography (PET) tracer after being labeled with 11C isotope. KR31173 shows promising biodistribution and pharmacological properties in mice. KR31173 selectively binds to organs known to contain a high density of AT1 angiotensin receptors in CD-1 mice[1].

IC50 & Target

AT1 Receptor

3.27 nM (IC50)

体内研究
(In Vivo)

[11C] KR31173 (19.1 MBq (517 μCi, 1.45 μg/kg), 静脉注射, 5-90 分钟) 选择性地与已知含有高密度 AT1 血管紧张素受体的器官结合[1]

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

Animal Model: Male CD-1 mice were injected via the tail vein with 19.1 MBq (517 μCi, 1.45 μg/kg) of [11C] KR31173 10 min after KR31173 administration[1].
Dosage: 1 mg/kg
Administration: i.v., once and then collected blood sample, and measured organs weight and their radioactivity 60 min after [11C] KR31173 administration.
Result: Had high initial liver uptake which rapidly washes out over 30 minutes following by subsequent accumulation in adrenal glands and kidneys after 30 minutes, with tissue-to-blood ratios generally exceeding 10:1.
Significantly inhibited the uptake of [11C] KR31173 in the adrenal glands (91%), kidneys (90%), lungs (88%), heart (92%) and livers (50%).
分子量

546.62

Formula

C31H30N8O2

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
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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:
KR31173
目录号:
HY-165425
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