SKF 525A (hydrochloride)
(Synonyms: 盐酸丙基解痉素,RP 5171|U 5446) 目录号 : GC16259
A nonspecific CYP450 inhibitor
Cas No.:62-68-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: in the μM range when tested using human liver microsomes
SKF 525A is a cytochrome P (CYP)450 inhibitor.
Cytochromes P450 (CYPs) use various molecules as substrates in enzymatic reactions. CYPs are the metabolic oxidase enzymes in electron transfer chains, categorized as P450-containing systems.
In vitro: Previous study found that when incubated with human liver microsomes, SKF525A could undergo CYP-dependent oxidative N-deethylation to its secondary amine metabolite SKF8742. In addition, SKF525A and its metabolite and primary amine analog all inhibited CYP2B6-, CYP2C9-, CYP2C19-, CYP2D6-, as well as CYP3A-selective reactions to various degrees but had little effect on CYP1A2, CYP2A6, and CYP2E1 reactions [1].
In vivo: Animal study found that SKF 525A at 1.5-9 mg/kg could reduce or abolish the hypertensive effect of McN-A-343, DMPP and nicotine, but could neither noticeably affect the hypertensive effect of tyramine, adrenaline and noradrenaline, nor the hypotensive effect of acetylcholine and orciprenaline. Thus, SKF 525A was able to block the rat sympathetic ganglia and the adrenal medulla and such blockade was non-specific. Moreover, the blockade might result from the stabilizing effect of SKF 525A on postsynaptic membranes of the sympathetic ganglia and the adrenal medulla [2].
Clinical trial: Up to now, SKF 525A is still in the preclinical development stage.
References:
[1] M. R. Franklin and L. B. Hathaway. 2-Diethylaminoethyl-2,2-diphenylvalerate-HCl (SKF525A) revisited: Comparative cytochrome P450 inhibition in human liver microsomes by SKF525A, its metabolites, and SKF-acid and SKF-alcohol. Drug Metabolism and Disposition 36(12), 2539-2546 (2008).
[2] Krsti MK. Blockade by SKF 525A of the rat sympathetic ganglia and the adrenal medulla. Arch Int Pharmacodyn Ther. 1976 Sep;223(1):64-70.
| Cas No. | 62-68-0 | SDF | |
| 别名 | 盐酸丙基解痉素,RP 5171|U 5446 | ||
| 化学名 | α-phenyl-α-propyl-benzeneacetic acid, 2-(diethylamino)ethyl ester, monohydrochloride | ||
| Canonical SMILES | O=C(OCCN(CC)CC)C(C1=CC=CC=C1)(CCC)C2=CC=CC=C2.Cl | ||
| 分子式 | C23H31NO2 • HCl | 分子量 | 390.0 |
| 溶解度 | ≥ 20.2mg/mL 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 | 2.5641 mL | 12.8205 mL | 25.641 mL |
| 5 mM | 0.5128 mL | 2.5641 mL | 5.1282 mL |
| 10 mM | 0.2564 mL | 1.2821 mL | 2.5641 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。