SB-505124 hydrochloride (Synonyms: SB 505124 hydrochloride;SB505124 hydrochloride) |
| رقم الكتالوجGC10421 |
مثبط لمستقبلات ALK4 وALK5 وALK7
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 356559-13-2
Sample solution is provided at 25 µL, 10mM.
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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 | |
| المرادفات | SB 505124 hydrochloride;SB505124 hydrochloride | ||
| Chemical Name | 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 | ||
| Formula | C20H22ClN3O2 | M.Wt | 371.86 |
| الذوبان | ≥ 9.3 mg/mL in DMSO, ≥ 87 mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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