S81420 |
GSK6853 |
源叶(MedMol) | 98% |
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- 产品描述: GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain
- 靶点: Epigenetic Reader Domain;EpigeneticReaderDomain
- 体外研究:
Screening GSK6853 against a panel of 48 unrelated assays reveals only off-target activities that are relatively weak compared to the BRPF1 potency. However, to minimize the chance of off-target effects , the recommended concentration is no higher than 1 μM in cell-based assays
- 体内研究:
In male CD1 mouse, following IV administration (1 mg/kg), GSK6853 demonstrates a high blood clearance of 107 mL/min/kg, a moderate volume of distribution (5.5 L/kg) and a moderate terminal half-life of 1.7 h. Oral administration (PO, 3 mg/kg) achieves a moderate systemic exposure, with a Cmax of 42 ng/mL and Tmax of 1.5 h, resulting in a bioavailability of 22%. The intraperitoneal route of administration (IP, 3 mg/kg) reaches a Cmax of 469 ng/mL and Tmax of 0.25 h, resulting in a bioavailability of 85%. The results indicate that the IP route of administration would be suitable for dosing this molecule in potential PKPD models
- 参考文献:
1. Bamborough P et al. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain. ACS Med Chem Lett. 2016 May 9;7(6):552-7.
- 溶解性: Soluble in DMSO、Ethanol
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.442 ml 12.211 ml 24.421 ml 5 mM 0.488 ml 2.442 ml 4.884 ml 10 mM 0.244 ml 1.221 ml 2.442 ml 50 mM 0.049 ml 0.244 ml 0.488 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)