货号:A233637
同义名:
磷酸氯喹
/ Chloroquine(phosphate)(CRM); Chloroquine diphosphate
Chloroquine phosphate是一种广泛用于治疗疟疾和类风湿性关节炎的抗疟药和抗炎剂。它是一种自噬和 Toll 样受体 (TLR) 抑制剂,在体外控制 SARS-CoV-2 (COVID-19) 感染的效果非常显著 (EC50 = 1.13 μM)。


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| 产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| SBI-0206965 |
+++
ULK2, IC50: 711 nM ULK1, IC50: 108 nM |
95% | |||||||||||||||||
| Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
| Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
| PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
| MRT68921 HCl |
++++
ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 nM |
99%+ | |||||||||||||||||
| ROC-325 | ✔ | 99%+ | |||||||||||||||||
| Autophinib |
+++
Autophagy, IC50: 40 nM |
99% | |||||||||||||||||
| Lys05 | ✔ | 99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 产品名称 | ATM ↓ ↑ | ATR ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Wortmannin |
++
ATM, IC50: 150 nM |
MLCK,PI3K,DNA-PK | 99%+ | ||||||||||||||||
| CP-466722 |
+
ATM, IC50: 410 nM |
99%+ | |||||||||||||||||
| Torin 2 |
++
ATM, EC50: 28 nM |
++
ATR, EC50: 35 nM |
mTOR,DNA-PK | 99%+ | |||||||||||||||
| KU-55933 |
+++
ATM, IC50: 12.9 nM |
96% | |||||||||||||||||
| ETP-46464 |
+
ATM, IC50: 545 nM |
+++
ATR, IC50: 14 nM |
mTOR,DNA-PK | 98% | |||||||||||||||
| CGK733 |
++
ATM, IC50: 200 nM |
++
ATR, IC50: 200 nM |
99%+ | ||||||||||||||||
| AZD0156 | ✔ | 99%+ | |||||||||||||||||
| Dactolisib |
+++
ATR, IC50: 21 nM |
98+% | |||||||||||||||||
| Ceralasertib |
++++
ATR, IC50: 1 nM |
99%+ | |||||||||||||||||
| Berzosertib |
+++
ATR, IC50: 19 nM |
99%+ | |||||||||||||||||
| VE-821 |
+++
ATR, Ki: 13 nM |
99%+ | |||||||||||||||||
| AZ20 |
++++
ATR, IC50: 5 nM |
mTOR | 99%+ | ||||||||||||||||
| Schizandrin B |
+
ATR, IC50: 7.25 μM |
P-gp | 98% | ||||||||||||||||
| m-PEG25-NHS ester |
++++
ATR, IC50: 7 nM |
95% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | Chloroquine diphosphate (CQ), an autophagy inhibitor that may enhance the cytocidal effect of gefitinib against cSCC, was used in the present study. Suppression of autophagy by CQ, which was demonstrated by an alteration in microtubule associated protein 1 light chain 3-B in CQ pre-treated A431 cells, significantly enhanced cell apoptosis, which suggested that gefitinib-induced autophagy is cytoprotective. CQ was demonstrated to exhibit a synergistic apoptotic effect when used in combination with gefitinib during cSCC(cutaneous squamous cell carcinoma) therapy[2]. In vitro studies indicate that the antiviral effect of chloroquine diphosphate (CQ) requires a high concentration of the drug[3]. Chloroquine diphosphate (25mg/kg and 50mg/kg, respectively) significantly inhibited the growth of the implanted 4T1 tumor cells and induced apoptosis in the tumor microenvironment. Moreover, the metastasis of tumor cells to the lungs was inhibited significantly and the survival of the mice enhanced[4]. |
| Concentration | Treated Time | Description | References | |
| HK-2 cells | 10 μM | 24 h | CQ remarkably reversed the nilotinib-induced decrease in MMP and inhibited nilotinib-induced intracellular ROS accumulation. | Adv Sci (Weinh). 2023 Sep;10(26):e2302002. |
| HUVECs | 10 μM | 24 h | CQ remarkably reversed the nilotinib-induced decrease in MMP and inhibited nilotinib-induced intracellular ROS accumulation. | Adv Sci (Weinh). 2023 Sep;10(26):e2302002. |
| WS hMSCs | 0.2-100 μM | Chloroquine at low concentrations (0.2-5 μM) promoted cell self-renewal, while higher concentrations (20 μM and above) inhibited cell proliferation. Treatment with 1 μM CQ decreased the percentage of SA-β-gal-positive cells and increased the number of Ki67-positive cells, while also reducing IL-6 secretion. | Protein Cell. 2022 Jun;13(6):454-461. | |
| U2OS cells | 10, 20, 40 μM | 16 h | Induced eIF2α phosphorylation | Cell Death Dis. 2021 Jan 6;12(1):6. |
| U2OS-GFP-LC3 ATG5 knockout cells | 10, 20, 40 μM | 6 h | ATG5 knockout cells failed to accumulate autophagosomes | Cell Death Dis. 2021 Jan 6;12(1):6. |
| U2OS-GFP-LC3 wild type cells | 10, 20, 40 μM | 6 h | Induced GFP-LC3 dot formation, indicating autophagosome accumulation | Cell Death Dis. 2021 Jan 6;12(1):6. |
| Human glioma H4 cells | 10, 20, 40 μM | 6 h | Induced GFP-LC3 dot formation, indicating autophagosome accumulation | Cell Death Dis. 2021 Jan 6;12(1):6. |
| Human U2OS osteosarcoma cells | 10, 20, 40 μM | 6 h | Induced GFP-LC3 dot formation, indicating autophagosome accumulation | Cell Death Dis. 2021 Jan 6;12(1):6. |
| lymphoblastoid cells | 100 μM | Chloroquine induced phosphorylation of KAP1 at S824 and ZEBRA expression, and the EBV lytic cycle reached completion, releasing substantial numbers of viral particles. | PLoS Pathog. 2017 Mar 1;13(3):e1006249. | |
| Jijoye and Raji Burkitt lymphoma cells | 200 μM | Chloroquine induced the expression of ZEBRA in both cell lines, although with different temporal patterns. | PLoS Pathog. 2017 Mar 1;13(3):e1006249. | |
| Calu-3 cells | 64.7 µM | Inhibit SARS-CoV-2 infection | J Mol Cell Biol. 2021 Jul 6;13(3):175-184. | |
| Vero E6 cells | 6.5 µM | Inhibit SARS-CoV-2 infection | J Mol Cell Biol. 2021 Jul 6;13(3):175-184. | |
| HH514-16 Burkitt lymphoma cells | 200 μM | 24 h | Chloroquine induced phosphorylation of KAP1 at S824 and activated the EBV lytic cycle. | PLoS Pathog. 2017 Mar 1;13(3):e1006249. |
| MiaPaca-2 | 100 μM | 72 h | To evaluate the cytotoxicity of CQ-HES, results showed that CQ-HES had similar cytotoxicity to HCQ. | Biomacromolecules. 2017 Aug 14;18(8):2247-2257. |
| MiaPaca-1 | 100 μM | 72 h | To evaluate the cytotoxicity of CQ-HES, results showed that CQ-HES had similar cytotoxicity to HCQ. | Biomacromolecules. 2017 Aug 14;18(8):2247-2257. |
| AsPC-1 | 100 μM | 72 h | To evaluate the cytotoxicity of CQ-HES, results showed that CQ-HES had similar cytotoxicity to HCQ. | Biomacromolecules. 2017 Aug 14;18(8):2247-2257. |
| Administration | Dosage | Frequency | Description | References | ||
| C57BL/6J mice | Nilotinib-induced nephrotoxicity model | Oral | 30 mg/kg | Daily for 30 days | HCQ significantly reversed the nilotinib-induced elevation of BUN and Scr and ameliorated kidney cell apoptosis and oxidative stress induced by nilotinib. | Adv Sci (Weinh). 2023 Sep;10(26):e2302002. |
| Sprague Dawley (SD) rats | Physiologically aged rat model | Oral | 0.1 mg/kg | Twice a week for 5 months | Low-dose CQ treatment extended the lifespan of rats, repressed systemic inflammation, and inhibited fibrosis across multiple tissues. Furthermore, CQ treatment mitigated age-related molecular changes and repressed genes linked to fibrosis and the inflammatory response. | Protein Cell. 2022 Jun;13(6):454-461. |
| Mice | C57Bl/6j mice | Intraperitoneal injection | 50 mg/kg | Once daily for 10 days | Induced eIF2α phosphorylation | Cell Death Dis. 2021 Jan 6;12(1):6. |
| Mice | HCoV-OC43 infection model | 15 mg/kg | Prevent HCoV-OC43 infection | J Mol Cell Biol. 2021 Jul 6;13(3):175-184. |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02563496 | Malaria, Vivax | Phase 2 | Recruiting | November 30, 2019 | Colombia ... 展开 >> GSK Investigational Site Recruiting Monteria, Colombia Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com Thailand GSK Investigational Site Not yet recruiting Tak, Thailand, 63110 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com Vietnam GSK Investigational Site Recruiting Hanoi, Vietnam, 100000 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Ho Chi Minh City, Vietnam, 700000 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Ho Chi Minh, Vietnam Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com 收起 << |
| NCT01136850 | Malaria in Pregnancy ... 展开 >> Sexually Transmitted Infections Anaemia 收起 << | Phase 3 | Completed | - | Papua New Guinea ... 展开 >> Papua New Guinea Institute of Medical Research Madang, Madang Province, Papua New Guinea 收起 << |
| NCT00157859 | Falciparum Malaria ... 展开 >> Vivax Malaria 收起 << | Not Applicable | Completed | - | Indonesia ... 展开 >> SP9 & SP12 Public Health- Malaria control clinics Timika, Papua, Indonesia 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.94mL 0.39mL 0.19mL |
9.69mL 1.94mL 0.97mL |
19.39mL 3.88mL 1.94mL |
|
| CAS号 | 50-63-5 |
| 分子式 | C18H32ClN3O8P2 |
| 分子量 | 515.86 |
| SMILES Code | CC(NC1=CC=NC2=CC(Cl)=CC=C12)CCCN(CC)CC.O=P(O)(O)O.O=P(O)(O)O |
| MDL No. | MFCD00069852 |
| 别名 | 磷酸氯喹 ;Chloroquine(phosphate)(CRM); Chloroquine diphosphate; NSC 14050; DL-Chloroquine |
| 运输 | 蓝冰 |
| InChI Key | QKICWELGRMTQCR-UHFFFAOYSA-N |
| Pubchem ID | 64927 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place,Sealed in dry,2-8°C |
| 溶解方案 |
H2O: 30 mg/mL(58.16 mM)
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