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
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
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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. Further protocols information, click here.
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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.
In Vivo
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.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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