SB-505124 hydrochloride
(Synonyms: SB 505124 hydrochloride;SB505124 hydrochloride) 目录号 : GC10421
Inhibitor of receptors ALK4, ALK5, and ALK7
Cas No.:356559-13-2
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
SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 value of 129 nM and 47 nM [1].
Anaplastic lymphoma kinase (ALK) gets involved in the development of the brain and influence specific neurons in the nervous system.
SB505124 is a reversible ATP competitive inhibitor of ALK4 and ALK5. Incubation of the ALK5 with high concentrations of SB505124, followed by dilution to a sub-IC50 concentration resulted in no effect of downstream Smad3 phosphorylation [2]. SB505124 was shown to have no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. Evidence showed that 100% drug will release within 12 h, and the gel showed no cytotoxicity to the cultured rabbit subconjunctival cells[2]. It was observed that ALK4 downstream effectors including pSmad2, CTGF, and α-SMA was inhibited by SB505124 in cultured fibroblasts [3].
In rabbit in glaucoma filtration surgery (GFS) model, the period of filtering blebs were reduced by TGFβ induced fibroblast. The filtering blebs in the GFS with SB505124 group were maintained for more than 10 days, and the period of bleb survival was significantly longer than that in controls, which suggested the significant inhibition of ALK4 and 5 by SB505124 [2]. It was observed that ALK4 downstream effectors CTGF and α-SMA were suppressed by SB-505124 in vivo[3].
References:
[1]. DaCosta B S et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol., 2004,65(3): 744-52.
[2]. Sutariya V, et al. Thermoreversible gel for delivery of activin receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. Pharm Dev Technol., 2013, 18(4): 957-962.
[3]. Sapitro J, et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor. Mol Vis., 2010, 16: 1880-1892.
| Cas No. | 356559-13-2 | SDF | |
| 别名 | SB 505124 hydrochloride;SB505124 hydrochloride | ||
| 化学名 | 2-[4-(1,3-benzodioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl]-6-methylpyridine | ||
| Canonical SMILES | CC1=CC=CC(=N1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4.Cl | ||
| 分子式 | C20H22ClN3O2 | 分子量 | 371.86 |
| 溶解度 | ≥ 9.3 mg/mL in DMSO, ≥ 87 mg/mL in EtOH | 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 | 2.6892 mL | 13.4459 mL | 26.8918 mL |
| 5 mM | 0.5378 mL | 2.6892 mL | 5.3784 mL |
| 10 mM | 0.2689 mL | 1.3446 mL | 2.6892 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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