EMD 66684 是 II 型血管紧张素 (AT1) 受体的拮抗剂。EMD 66684 对 AT1 亚型Ang II受体具有强亲和力，IC50为 0.7 nM。EMD 66684 也是一种抗缺血的细胞保护剂。
| 生物活性 | EMD 66684 is an antagonist ofAngiotensin II Type 1(AT1) receptor. EMD 66684 shows potent binding affinities for theAT1subtypeAng II receptorwith anIC50value of 0.7 nM. EMD 66684 also serves as an antiischemic cytoprotectant[1]-[5]. |
| IC50& Target | Angiotensin II Type 1 0.7 nM (IC50) |
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体外研究
(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 IC50value of 0.7 nM in rat adrenal cortical membranes, and inhibits Ang II-Induced contraction in rabbit aortic rings with an IC50value of 0.2 nM[3].
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. |
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体内研究
(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].
| 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. |
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| 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. |
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