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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- CAS No.: 1216884-39-7
- 화학식: C28H31ClN8O2
- 분자량:547.05
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Angiotensin Receptor Isoforms
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Biological Activity
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Angiotensin II Type 1 0.7 nM (IC50) |
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.
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Cell Line:Hep G2 cells (liver hepatocellular carcinoma cell line)
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Concentration:1 nM
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Incubation Time:1 hour
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Result:Completely blocked the Ang II responses Ang II-induced response.
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.
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Animal Model:Conscious furosemide-treated SHR (Spontaneous Hypertension Rat)[3]
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Dosage:0.1, 0.3, 1 mg/kg
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Administration:Intravenous injection; once; as potassium salts to conscious furosemide-treated SHR
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Result:Showed a long lasting fall in blood pressure, resulted mean arterial pressure (MAP) decreased in a dose-dependent manner.
Chemical Information
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CAS No. 1216884-39-7
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분자량 547.05
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화학식 C28H31ClN8O2
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Westfall TC, et al. Interactions of neuropeptide y, catecholamines, and angiotensin at the vascular neuroeffector junction. Adv Pharmacol. 2013;68:115-39. [Content Brief]
[2]. Qu L, et al. Systematic characterization of AT1 receptor antagonists with label-free dynamic mass redistribution assays. J Pharmacol Toxicol Methods. 2020 Mar-Apr;102:106682. [Content Brief]
[3]. Mederski WW, et al. Non-peptide angiotensin II receptor antagonists: synthesis and biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine derivatives. J Med Chem. 1994 May 27;37(11):1632-45. [Content Brief]
[4]. Byku M, et al. Nerve stimulation induced overflow of neuropeptide Y and modulation by angiotensin II in spontaneously hypertensive rats. Am J Physiol Heart Circ Physiol. 2008 Nov;295(5):H2188-97. [Content Brief]
[5]. Avkran M, et al. Treatment of ischemia with an angiotensin II antagonist: UK, GB2337701. 1999-12-01.
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EMD 66684 Related Classifications
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