1. GPCR/G Protein
  2. Angiotensin Receptor
  3. EMD 66684

EMD 66684 is an antagonist of Angiotensin II Type 1 (AT1) receptor. EMD 66684 shows potent binding affinities for the AT1 subtype Ang II receptor with an IC50 value of 0.7 nM. EMD 66684 also serves as an antiischemic cytoprotectant -.

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EMD 66684 Chemical Structure

EMD 66684 Chemical Structure

CAS No. : 1216884-39-7

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Description

EMD 66684 is an antagonist of Angiotensin II Type 1 (AT1) receptor. EMD 66684 shows potent binding affinities for the AT1 subtype Ang II receptor with an IC50 value of 0.7 nM. EMD 66684 also serves as an antiischemic cytoprotectant [1]-[5].

IC50 & Target

Angiotensin II Type 1

0.7 nM (IC50)

In Vitro

Ang II is known to activate at least two receptor subtypes, namely, AT1 and AT2 receptors[1].
EMD 66684 (0.1 μM) decreases Ang II (0.1 mM)-induced in basal and NS-induced NPY overflow, attenuates the NS-induced stimulation of both NE and NPY release[1].
EMD 66684 (0.01 nM-1 μM; 0, 30, 60 min) exhibits a time-dependent inhibition against Ang II in DMR (dynamic mass redistribution) responses, with IC50s of 181.97 nM (0 min), 0.22 nM (30 min), 0.17 nM (60 min), respectively[2].
EMD 66684 exhibits binding affinities for the AT1 subtype Ang II receptor with an IC50 value of 0.7 nM in rat adrenal cortical membranes, and inhibits Ang II-Induced contraction in rabbit aortic rings with an IC50 value of 0.2 nM[3].

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

Cell Viability Assay[1]

Cell Line: Hep G2 cells (liver hepatocellular carcinoma cell line)
Concentration: 1 nM
Incubation Time: 1 hour
Result: Completely blocked the Ang II responses Ang II-induced response.
In Vivo

EMD 66684 (0.1, 0.3, 1 mg/kg; i.v.; once) results in a long lasting fall in blood pressure[3].
EMD 66684 (0.1 μM; 45 min) decreases the NS-induced overflow of NE and NPY from preparations from SHRs at 10-12 weeks old[4].

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

Animal Model: Conscious furosemide-treated SHR (Spontaneous Hypertension Rat)[3]
Dosage: 0.1, 0.3, 1 mg/kg
Administration: Intravenous injection; once; as potassium salts to conscious furosemide-treated SHR
Result: Showed a long lasting fall in blood pressure, resulted mean arterial pressure (MAP) decreased in a dose-dependent manner.
Molecular Weight

547.05

Formula

C28H31ClN8O2

CAS No.
SMILES

O=C1C2=C(C=CN1CC(N(C)C)=O)N=C(CCCC)N2CC3=CC=C(C4=C(C5=NN=NN5)C=CC=C4)C=C3.Cl

Shipping

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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EMD 66684 Related Classifications

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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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Product Name:
EMD 66684
Cat. No.:
HY-103247
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