SKF 96365 hydrochloride
(Synonyms: 1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑) 目录号 : GC14641
An inhibitor of voltage-gated calcium channels
Cas No.:130495-35-1
Sample solution is provided at 25 µL, 10mM.
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SKF 96365 hydrochloride is an inhibitor of store-operated calcium entry (SOCE). Also, it inhibits transient receptor potential cation channels (TRPCs) and voltage-gated sodium current [1] [2] [3].
Store-operated calcium entry (SOCE) increases cytosolic Ca2+ and induces the entry of extracellular calcium. TRPC channels are divided into store-operated and receptor-operated channels and play a critical role in brain development [1] [2].
SKF 96365 hydrochloride is a SOCE inhibitor. In MPP+ stressed PC12 cells, SKF-96365 (10, 50 μM) significantly prevented nuclear damage, decreased LDH release, increased cell viability and inhibited apoptosis. Also, SKF-96365 inhibited Homer1-mediated endoplasmic reticulum (ER) Ca2+ release and intracellular calcium overload induced by MPP+ injury [1]. In rat ventricular myocytes, SKF-96365 inhibited INa in a frequency-dependent and use-dependent way [3]. In Madin Darby canine kidney (MDCK) cells, SKF 96365 (25-100 μM) induced a robust [Ca2+]i transient in a dose-dependent way [4].
In rats, SKF-96365 significantly inhibited persistent spontaneous nociception induced by melittin and reduced hypersensitivity to both mechanical and thermal stimuli. These results suggested that SKF-96365-sensitive TRPC channels were involved in the processing of melittin-induced hypersensitivity and inflammatory pain [2].
References:
[1]. Chen T, Zhu J, Zhang C, et al. Protective effects of SKF-96365, a non-specific inhibitor of SOCE, against MPP+-induced cytotoxicity in PC12 cells: potential role of Homer1. PLoS One, 2013, 8(1): e55601.
[2]. Ding J, Zhang JR, Wang Y, et al. Effects of a non-selective TRPC channel blocker, SKF-96365, on melittin-induced spontaneous persistent nociception and inflammatory pain hypersensitivity. Neurosci Bull, 2012, 28(2): 173-181.
[3]. Chen KH, Liu H, Yang L, et al. SKF-96365 strongly inhibits voltage-gated sodium current in rat ventricular myocytes. Pflugers Arch, 2015, 467(6): 1227-1236.
[4]. Jan CR, Ho CM, Wu SN, et al. Multiple effects of 1-[beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole hydrochloride (SKF 96365) on Ca2+ signaling in MDCK cells: depletion of thapsigargin-sensitive Ca2+ store followed by capacitative Ca2+ entry, activation of a direct Ca2+ entry, and inhibition of thapsigargin-induced capacitative Ca2+ entry. Naunyn Schmiedebergs Arch Pharmacol, 1999, 359(2): 92-101.
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Animal experiment: |
Mice: Five to six-week-old female athymic BALB/c mice are inoculated into the right oxter with HCT116 cells. When the diameter of the subcutaneous tumor reaches approximately 0.5 cm, animals are randomLy assigned to the vehicle, SKF-96365 alone, HCQ alone or SKF-96365+HCQ. SKF-96365 is applied (20 mg/kg) and HCQ is applied (60 mg/kg) daily for 14 successive days by i.p. injection. Tumor sizes and volume are determined. Eight mice are included in each group. Mice are sacrificed 24 h after the last treatment. The tumors are weighed and processed for western blot analysis or paraffin embedding[2]. |
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References: [1]. Liu H, et al. SKF-96365 blocks human ether-à-go-go-related gene potassium channels stably expressed in HEK 293 cells. Pharmacological Research. Pharmacol Res, 2016 Feb, 104:61-9. |
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| Cas No. | 130495-35-1 | SDF | |
| 别名 | 1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑 | ||
| 化学名 | (S)-1-(2-(4-methoxyphenyl)-2-(3-(4-methoxyphenyl)propoxy)ethyl)-1H-imidazole hydrochloride | ||
| Canonical SMILES | COC1=CC=C(C=C1)[C@@H](CN2C=CN=C2)OCCCC(C=C3)=CC=C3OC.Cl | ||
| 分子式 | C22H26N2O3.HCl | 分子量 | 402.92 |
| 溶解度 | ≥ 40.3mg/mL in DMSO | 储存条件 | 4°C, protect from light, stored under nitrogen |
| 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 | 2.4819 mL | 12.4094 mL | 24.8188 mL |
| 5 mM | 0.4964 mL | 2.4819 mL | 4.9638 mL |
| 10 mM | 0.2482 mL | 1.2409 mL | 2.4819 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。
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet