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

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.

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KR31173

KR31173 Chemical Structure

CAS No. : 260554-07-2

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Description

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)

In Vivo

[11C] KR31173 (19.1 MBq (517 μCi, 1.45 μg/kg), i.v., 5-90 min) selectively binds to organs known to contain a high density of AT1 angiotensin receptors[1].

MedChemExpress (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%).
Molecular Weight

546.62

Formula

C31H30N8O2

CAS No.
SMILES

[O-][N+]1=CC=CC=C1C2=C(COC)N=C(N(CC3=CC=C(C4=CC=CC=C4C5=NN=NN5)C=C3)C(CCCC)=N6)C6=C2

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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    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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Product Name:
KR31173
Cat. No.:
HY-165425
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