Deserpidine
(Synonyms: 地舍平; Harmonyl) 目录号 : GC38768
Deserpidine (Harmonyl), an alkaloid isolated from the roots of Rauwolfia canescens, is a competitive angiotensin converting enzyme (ACE) inhibitor, also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex.
Cas No.:131-01-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Deserpidine (Harmonyl), an alkaloid isolated from the roots of Rauwolfia canescens, is a competitive angiotensin converting enzyme (ACE) inhibitor, also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex.
[1] Varchi G, et al. J Nat Prod. 2005 Nov;68(11):1629-31. [2] Zhang H, et al. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Oct 1;877(27):3221-5. [3] Fulton SC, et al. Fed Proc. 1976 Dec;35(14):2558-62.
| Cas No. | 131-01-1 | SDF | |
| 别名 | 地舍平; Harmonyl | ||
| Canonical SMILES | COC([C@H]1[C@@]2([H])C[C@]3([H])C4=C(CCN3C[C@@]2([H])C[C@@H](OC(C5=CC(OC)=C(OC)C(OC)=C5)=O)[C@@H]1OC)C6=CC=CC=C6N4)=O | ||
| 分子式 | C32H38N2O8 | 分子量 | 578.65 |
| 溶解度 | DMSO: 100 mg/mL (172.82 mM) | 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 | 1.7282 mL | 8.6408 mL | 17.2816 mL |
| 5 mM | 0.3456 mL | 1.7282 mL | 3.4563 mL |
| 10 mM | 0.1728 mL | 0.8641 mL | 1.7282 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。
Synthesis of Deserpidine from reserpine
J Nat Prod 2005 Nov;68(11):1629-31.PMID:16309312DOI:10.1021/np050179x.
The Rauwolfia alkaloids reserpine (1) and Deserpidine (2), two alkaloids from Rauwolfia species, have been widely used for their antihypertensive action. Deserpidine (2) is a compound with limited availability from natural sources, and its synthesis from 1 in six steps (41% overall yield) is reported here.
Liquid chromatography/tandem mass spectrometry method for the quantification of Deserpidine in human plasma: Application to a pharmacokinetic study
J Chromatogr B Analyt Technol Biomed Life Sci 2009 Oct 1;877(27):3221-5.PMID:19620026DOI:10.1016/j.jchromb.2009.06.005.
A sensitive and rapid liquid chromatography/tandem mass spectrometric (LC/MS/MS) method was developed and validated for the determination of Deserpidine in human plasma. The plasma samples were prepared using liquid-liquid extraction (LLE) with ethyl ether-dichloromethane (3:2, v/v). Chromatographic separation was accomplished on an Ultimate XB-C18 column. The mobile phase consisted of methanol-5mM ammonium acetate-formic acid (72:28:0.036, v/v/v). Detection of Deserpidine and the internal standard tropisetron was achieved by tandem mass spectrometry with an electrospray ionization interface in positive ion mode. The lower limit of quantification was 4.0pg/ml. The linear range of the method was from 4.0 to 2000pg/ml. The intra- and inter-day precisions were lower than 14.7% in terms of relative standard deviation (RSD), and the accuracy was within +/-8.7% in terms of relative error (RE). This validated method was successfully applied for the evaluation of pharmacokinetics of Deserpidine after a single oral administration dose of 0.25mg Deserpidine to 22 healthy volunteers.
Antibody specificity studies for reserpine, its metabolites, and synthetic reserpine congeners: radioimmunoassay
J Pharm Sci 1979 Nov;68(11):1433-5.PMID:574544DOI:10.1002/jps.2600681126.
Progress in the development of radioimmunoassay techniques for reserpine and related compounds is reported. A conjugate of reserpine with human serum albumin was prepared, involving linkage at the indole nitrogen atom of reserpine. Injection of the purified conjugate into sheep elicited antibodies of high titer, which bound reserpine selectively. Tritiated reserpine was employed in the procedure, and dextran-coated charcoal was utilized to separate free and bound forms of the drug. Antibodies exhibited a selectivity for reserpine and did not cross-react significantly with major human metabolites. Cross-reactivity of antibodies with other reserpine derivatives (i.e., syrosingopine, Deserpidine, and rescinnamine) also was investigated. A stable tritiated or radioiodinated reserpine derivative of high specific activity is being sought to improve assay sensitivity for use in bioequivalence and bioavailability studies. In the absence of any extraction or concentration procedures, at least a 10-fold increase in immunoassay sensitivity would be required to follow reserpine levels in humans given normal doses of the drug. The methods show promise also for the assay of reserpine derivatives such as Deserpidine, which exhibits cross-reactivity to reserpine antibodies.