CGP48369
目录号 : GC32561
CGP48369是血管紧张素II受体(angiotensinIIreceptor)拮抗剂，用于研究抗高血压疾病。
Cas No.:135689-23-5
Sample solution is provided at 25 µL, 10mM.
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CGP48369 is a nonpeptidic angiotensin II receptor antagonist, used for anti-hypertensive research.
CGP 48369 binds to the ATl receptor (IC50 1.8 nM in vascular smooth musc1e cells, VSMC) and inhibits AII-induced contraction in rabbit aorta (IC50 8.7 nM)[1].
CGP48369 (10 mg/kg/day p.o.) decreases BP in two-kidney/one-clip renal hypertensive rats for at least 24 h. In arteries with endothelium, contractions induced by AII 3×10-8 M do not differ in untreated spontaneously hypertensive rats (SHR) and WKY. All evoked significantly smaller contractions in SHR treated with CGP 48369 than in the other treated SHR. Antihypertensive treatment with benazepril or nifedipine, and to a lesser extent with CGP 48369, increases the sensitivity (pD2-va1ue) to intraluminal ACh. In arteries without endothelium, sensitivity to NE is identical in all groups, whereas maximal response in CGP 48369-treated SHR and in nifedipine treated SHR is slightly greater as compared with that in WKY[1]. In SHR, antihypertensive therapy with either benazepril HCl, CGP 48369, valsartan, or nifedipine (each 10 mg/kg/d for 8 weeks) significantly increase endothelium-dependent relaxations evoked by acetylcholine[2].
[1]. Dohi Y, et al. Angiotensin blockade or calcium antagonists improve endothelial dysfunction in hypertension: studies in perfused mesenteric resistance arteries. J Cardiovasc Pharmacol. 1994 Sep;24(3):372-9. [2]. Tschudi MR, et al. Antihypertensive therapy augments endothelium-dependent relaxations in coronary arteries of spontaneously hypertensive rats. Circulation. 1994 May;89(5):2212-8.
Animal experiment: | Male Wistar-Kyoto rats (WKY) and SHR aged 7 weeks are used in the assay. All rats are maintained on standard chow with free access to drinking water and used for experiments at age 15 weeks. SHR are randomly assigned 4 groups: All 4 groups are gavaged; in 3 of the 4, either CGP 48369, benazepril, or nifedipine (all 10 mg/kg/day p.o.) is administered for 8 weeks until the day ofthe experiment (age 15 weeks). All drugs are administered only once a day. Rats are studied in randomized order in a single-blinded design. BP is measured by the tail-cuff method 18-20 h after the last administration. Body weight and heart rate (HR) do not differ at the end of the treatment period in the four groups. On the day of the experiment, rats are anesthetized with pentobarbital (40 mg/kg intraperitoneally, i.p.) and the mesenterium is removed and placed in cold (40°C) Krebs-Ringer bicarbonate solution (in mM): NaCl 118.6, KCl 4.8, CaCl2 2.5, MgS04 1.2, KH2P04 1.2, NaHC03 25.1, edetate calcium disodium 0.026, glucose 10.1 (Krebs solution). |
References: [1]. Dohi Y, et al. Angiotensin blockade or calcium antagonists improve endothelial dysfunction in hypertension: studies in perfused mesenteric resistance arteries. J Cardiovasc Pharmacol. 1994 Sep;24(3):372-9. | |
| Cas No. | 135689-23-5 | SDF | |
| Canonical SMILES | O=C1NC(CCCC)=NC(CCCC)=C1CC2=CC=C(C3=CC=CC=C3C4=NN=NN4)C=C2 | ||
| 分子式 | C26H30N6O | 分子量 | 442.56 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2596 mL | 11.2979 mL | 22.5958 mL |
| 5 mM | 0.4519 mL | 2.2596 mL | 4.5192 mL |
| 10 mM | 0.226 mL | 1.1298 mL | 2.2596 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet