产品说明书
GP130 receptor agonist-1
 |
同义名 : | Ucla gp130 2 |
| CAS号 : | 339303-87-6 | |
| 货号 : | A670924 | |
| 分子式 : | C15H11FN2S | |
| 纯度 : | 99%+ | |
| 分子量 : | 270.325 | |
| MDL号 : | MFCD00784992 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 105 mg/mL(388.42 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | P-glycoprotein (P-gp) is an efflux transporter that influences the pharmacokinetics (PK) of various compounds[1]. P-glycoprotein is a well-identified membrane transporter with capability to efflux drug molecules out of the cancer cell leading to reduced efficiency of chemotherapy. Cancer cells upregulate P-gp expression as an adaptive response to evade chemotherapy mediated cell death[2]. Permeability glycoprotein (P-gp) mediates the export of drugs from cells located in the small intestine, blood-brain barrier, hepatocytes, and kidney proximal tubule, serving a protective function for the body against foreign substances[3]. N-(4-Fluorophenyl)-4-phenyl-2-thiazolami (UCLA GP130 2) is a potent, brain-penetrant and orally active GP130 receptor agonist. UCLA GP130 2 treatment showed a 2-fold increase in phosphorylation of STAT3 within 10 min at its regulatory Tyr705 site in SH-SY5Y cells. UCLA GP130 2 treatment increases phosphorylation of AKT at its regulatory Thr308 site and phosphorylation of ERK1/2 at its regulatory Thr202/Tyr204 site in the serum free media condition in SH-SY5Y cells, and in primary cortical neurons. For UCLA GP130 2, mice are dosed orally at 10 or 30 mg/kg, or injected subcutaneously at 10 mg/kg, and euthanized after 1, 2, 4, 6, and 8 h post dose. At 2 h after SQ delivery at 10 mg/kg the brain Cmax is 161 ng/g while dosing at 30 mg/kg orally, results in the brain Cmax of 156 ng/g (0.57 μM). The brain to plasma ratio for 2 is ∼4:1 for oral 30 mg/kg and ∼7.5:1 for 10 mg/kg SQ injection[4]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
3.70mL 0.74mL 0.37mL |
18.50mL 3.70mL 1.85mL |
36.99mL 7.40mL 3.70mL |
| 参考文献 |
|---|