Stilbamidine (Ba 2652)
(Synonyms: 司替巴脒; Ba 2652; Stilbamidin) 目录号 : GC32268
Stilbamidine (Ba 2652) 是一种衍生自芪的二脒化合物，主要以其结晶羟乙基磺酸盐的形式用于治疗各种真菌感染。
Cas No.:122-06-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Stilbamidine is a diamidine compound derived from Stilbene and used chiefly in the form of its crystalline isethionate salt in treating various fungal infections.
The high-affinity pentamidine transporter (HAPT1) is inhibited by Propamidine but displays only low affinity to Stilbamidine. adenosine-sensitive pentamidine transporter (ASPT1), in contrast, is strongly inhibited by Stilbamidine, and Propamidine. [3H]pentamidine uptake is determined in the presence of various concentrations of adenosine (IC50=1.2 μM) or melarsen oxide (IC50=0.7 μM), as well as in the presence of 250 μM adenosine and increasing concentrations of hypoxanthine, Propamidine (IC50=6.1 μM) and Stilbamidine (IC50=110 μM)[1]. The two diamidine compounds, Stilbamidine and Pentamidine are used to treat in multiple myeloma, a disease in which increase of the globulin content of the serum is of frequent occurrence[2].
[1]. De Koning HP. Uptake of pentamidine in Trypanosoma brucei brucei is mediated by three distinct transporters: implications for cross-resistance with arsenicals. Mol Pharmacol. 2001 Mar;59(3):586-92. [2]. BREWER AE.et al. Multiple myeloma treated with stilbamidine and pentamidine. Br Med J. 1948 Dec 4;2(4587):978-82.
| Cas No. | 122-06-5 | SDF | |
| 别名 | 司替巴脒; Ba 2652; Stilbamidin | ||
| Canonical SMILES | N=C(C1=CC=C(/C=C/C2=CC=C(C(N)=N)C=C2)C=C1)N | ||
| 分子式 | C16H16N4 | 分子量 | 264.33 |
| 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 | 3.7831 mL | 18.9157 mL | 37.8315 mL |
| 5 mM | 0.7566 mL | 3.7831 mL | 7.5663 mL |
| 10 mM | 0.3783 mL | 1.8916 mL | 3.7831 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。
A theoretical study of the nonintercalative binding of berenil and Stilbamidine to double-stranded (dA-dT)n oligomers
Mol Pharmacol 1984 May;25(3):452-8.PMID:6727867doi
The nonintercalative binding of two diarylamidines , berenil and Stilbamidine , to the minor groove of double-stranded (dA-dT)n oligomers in the B-DNA conformation was investigated by performing theoretical computations of their intermolecular interaction energies with the groove. The method consists of an additive procedure developed previously in this laboratory using empirical formulae based on ab initio computations. The objective was to assess the extent to which the particular structure of each diarylamidine bears on its binding mode and affinity to the minor groove. The results show that the intrinsically preferred configurations of the two compounds are markedly different. Owing to its slightly curved shape, berenil interacts with the groove predominantly through its concave side, the binding occurring principally with sites (O2, O1) belonging to two thymidines on the opposite strands. The binding of Stilbamidine involves a more limited number of hydrogen-bonding interactions, although an appreciably large number of interatomic distances between its hydrogens and sites on the groove (O2, N3, O1) falls in the range 2.7-3.1 A. Each side of Stilbamidine with respect to its long axis faces a distinct strand of DNA. The importance of the electrostatic contribution of the binding energy of the two diarylamidines is underlined. Preferential binding of berenil rather than of Stilbamidine occurs only at the level of a complete helical turn of phosphates in (dA-dT)n. The energy difference increases significantly upon further buildup of phosphates. These results can be interpreted in terms of the molecular electrostatic potential in the grooves.
Tracer studies of the distribution and trypanocidal action of Stilbamidine in rats
Br J Pharmacol Chemother 1959 Mar;14(1):137-41.PMID:13651591DOI:10.1111/j.1476-5381.1959.tb00940.x.
[(14)C]Stilbamidine was used to study the distribution of the drug in the organs and tissues of rats following intravenous injection. The prophylactic action of Stilbamidine was shown to depend upon the unchanged drug retained in tissues, especially the liver. Only the parent drug was extracted from trypanosomes when an infection was treated during the acute phase, as shown by the use of the fluorescent properties of Stilbamidine in conjunction with scanning and chromatographic techniques. The action of Stilbamidine on trypanosomes is therefore a direct one. A method for the synthesis of [(14)C]Stilbamidine in much improved yield is also described.