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Dalcetrapib (RO4607381) 是rhCETP 抑制剂(IC50:0.2 μM),具有增加血浆中HDL 胆固醇含量的作用。
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Dalcetrapib (RO4607381) 是rhCETP 抑制剂(IC50:0.2 μM),具有增加血浆中HDL 胆固醇含量的作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 253 | 现货 | |
2 mg | ¥ 362 | 现货 | |
5 mg | ¥ 589 | 现货 | |
10 mg | ¥ 841 | 现货 | |
25 mg | ¥ 1,420 | 现货 | |
50 mg | ¥ 2,160 | 现货 | |
100 mg | ¥ 3,730 | 现货 | |
500 mg | ¥ 8,380 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,450 | 现货 |
产品描述 | Dalcetrapib (RO4607381), a rhCETP inhibitor (IC50=0.2 μM), increases the plasma HDL cholesterol. |
靶点活性 | CETP (recombinant human):0.2 μM |
体外活性 | Dalcetrapib 通过调节 CETP 活性发挥作用。当加入人类血浆中时,Dalcetrapib 诱导 CETP 发生构象变化。在 Dalcetrapib ≤3 μM 的条件下,CETP 诱导的人类血浆中 pre-β-HDL 形成保持不变,而在 10 μM 时增加。Dalcetrapib 统计学上显著增加 pre-β-HDL 形成。[1] 在人类血浆中,Dalcetrapib 以 9 μM 的浓度实现对 CETP 活性的 50% 抑制。[2] Dalcetrapib 以剂量依赖性方式抑制 HepG2 中介质的 CETP 活性。[3] |
体内活性 | Dalcetrapib处理显著提高了HDL-C水平。在注射了[3H]胆固醇标记的自体巨噬细胞的仓鼠体内,Dalcetrapib显著增加了[3H]中性甾醇和[3H]胆汁酸的粪便排泄。Dalcetrapib提高了血浆中HDL-[3H]胆固醇水平。[1] 在口服剂量为30 mg/kg时,Dalcetrapib在日本白兔雄性动物身上抑制CETP活性达到95%。Dalcetrapib通过每天一次,连续3天口服30 mg/kg或100 mg/kg的剂量,分别将血浆HDL胆固醇水平提高了27%和54%。[2] Dalcetrapib处理显著提升了血清HDL-C水平。在5个月和7个月时,接受Dalcetrapib处理的兔子与对照组兔子相比,HDL2-C与HDL3-C的比率显著更高,表明Dalcetrapib通过抑制CETP活性改变了HDL亚类分布,并优先提高了HDL2-C水平。Dalcetrapib治疗增加了血清中的多巴酚醌酶活性和与HDL相关的血小板活化因子乙酰水解酶活性,但降低了血浆中的溶血磷脂酰胆碱浓度。[4] |
激酶实验 | Inhibition of rhCETP and C13S CETP-mediated transfer of CE from HDL to LDL: The inhibitory potency (IC50) of Dalcetrapib to decrease CE transfer from HDL to LDL by rhCETP and C13S CETP is measured using a scintillation proximity assay kit. Briefly, [3H]CE-labeled HDL donor particles are incubated in the presence of purified CETP proteins (final concentration 0.5 μg/mL) and biotinylated LDL acceptor particles for 3 hours at 37 °C. Subsequently, streptavidin-coupled polyvinyltoluene beads containing liquid scintillation cocktail binding selectively to biotinylated LDL are added, and the amount of [3H]CE molecules transferred to LDL is measured by β counting. |
细胞实验 | The HepG2 cells are seeded in 6-well plates and cultured to 70–80% confluence. After being washed with PBS, the cells are incubated with growth medium and a different concentration (0 μM–30 μM) of chemical inhibitor Dalcetrapib and dissolved in 2% DMSO for 24 hours. Total RNA is used for RT-PCR.(Only for Reference) |
别名 | JTT-705, 达塞曲匹, RO4607381 |
分子量 | 389.59 |
分子式 | C23H35NO2S |
CAS No. | 211513-37-0 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 72 mg/mL (184.8 mM) Ethanol: 72 mg/mL (184.8 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
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