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CAS No. :
MCE 国际站:HP661
产品活性:HP661 是一种具有口服活性的氧化磷酸化 (OXPHOS) 抑制剂,可有效阻断线粒体复合物 I 的活性,减少活性氧的产生。HP661 能够抑制高 OXPHOS 依赖性肿瘤的生长,克服高 OXPHOS 介导的耐药性,诱导凋亡 (apoptosis),可用于抗肿瘤研究。
研究领域:Metabolic Enzyme/Protease | NF-κB | Immunology/Inflammation | Apoptosis
作用靶点:Mitochondrial Metabolism | Reactive Oxygen Species | Apoptosis
In Vitro: HP661 (1 μM, 12 hours) inhibits the activity of complex I of oxidative phosphorylation (inhibition rate of 77.6%) and NAD +/NADH assay (inhibition rate of 87.5%).
HP661 (50 nM or 100 nM or 200 nM, 0-80min) potently selectively inhibits mitochondrial respiration capacity in high-OXPHOS lung cancer cells. Especially, HP661 suppresses the mitochondrial OCR with decreases basal OCR, maximal OCR and spare OCR capacity in a concentration-dependent manner in H460 andH441 cells.
HP661 (0-30 nM, 72 hours) selectively and dose-dependently inhibits the cell viability of the high OXPHOS lung cancer cell lines H460, H441, andA549/TR in the nanomolar range.
HP661 (25 nM or 50 nM or 100 nM, 7 days) selectively and dose-dependently inhibits the colony formation of the high OXPHOS lung cancer cell lines H460, H441, andA549/TR in the nanomolar range.
HP661 (30 μM, 48 hours) exhibits high selectivity toward high-OXPHOS lung cancer cells and Trametinib acquired resistant cells, leading to apoptosis.
In Vivo: HP661 (30 mg/kg, oral gavage twice daily for 18 days) achieves inhibition for tumor growth in high OXPHOS cancer cell xenograft mouse model by using H460 cells .
HP661 (1 mg.kg for i.v., 10 mg/kg for p.o.) shows a T1/2 of 2.3 h (i.v.) and 2.5 h (p.o.), and oral bioavailability (F%) of 64.3% in ICR mice.
Pharmacokinetic parameters for HP661 in ICR mice
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品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库,我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物;
• 50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领;
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Route |
Dose (mg/kg) |
Tmax (h) |
Cmax (ng/mL) |
AUC0-24 (h•ng/mL) |
AUC0-Ꝏ (h•ng/mL) |
VZ (mL/kg) |
CL (mL/h//kg) |
MRT0-24 |
T1/2 (h) |
F (%) |
i.v. |
1 |
0.08 |
425 |
337 |
359 |
9344 |
2794 |
1.5 |
2.3 |
/ |
p.o. |
10 |
1.00 |
618 |
2171 |
2304 |
/ |
/ |
3.0 |
2.5 |
64.3% |