GSK 4112
(Synonyms: SR6452) 目录号 : GC10715An agonist of the heme-dependent nuclear receptor REV-ERBα
Cas No.:1216744-19-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 2.3 μM
GSK4112 is a synthetic antagonist of the Nuclear Heme Receptor REV-ERB.
Rev-erbα and Rev-erbβ are heme sensors and atypical members of the nuclear receptor superfamily. As a member of the nuclear receptor superfamily, REV-ERBR functions as a receptor for the porphoryin heme. REV-ERBR can suppress the transcription of its target genes in a heme-dependent manner.
In vitro: Previous study showed that GSK4112 addition to either the REV-ERBR or REV-ERBβ assay led to enhanced repression. Cells were treated the with GSK4112 and similar pattern in GAL4 chimeric receptor assay was observed. In addition, GSK4112 suppressed reporter gene expression. GSK4112 also suppressed transcription driven by the Bmal1 promoter dose-dependently. GSK4112 activity was found to be associated with REV-ERBR [1].
In vivo: GSK4112 was found to display poor pharmacokinetic properties (rat liver microsomal Cint > 1.0 mL/min/mg protein; lack of oral bioavailability (F < 1% in mice)), which likely limited its use to biochemical and cell-based assays. As a result, GSK4112 was unlikely to be suitable for in vivo studies [1].
Clinical trial: N/A
Reference:
[1] Daniel Grant,Lei Yin,Jon L. Collins et al. GSK4112, a small molecule chemical probe for the cell biology of the nuclear Heme receptor Rev-erbα. ACS CHEMICAL BIOLOGY5(10):925-32.
Cas No. | 1216744-19-2 | SDF | |
别名 | SR6452 | ||
分子式 | C18H21ClN2O4S | 分子量 | 396.89 |
溶解度 | ≥ 11.9mg/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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.5196 mL | 12.5979 mL | 25.1959 mL |
5 mM | 0.5039 mL | 2.5196 mL | 5.0392 mL |
10 mM | 0.252 mL | 1.2598 mL | 2.5196 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 | |||
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% 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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