Crebanine是从云南厚朴(Stephania yunnanensis)草本植物中分离纯化的天然产物,能够将BaCl_2诱导的心律失常转变为窦性节律,减少CaCl_2诱导的VF和CA的发生,但对奎宁诱导的大鼠心律失常无保护作用。
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| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


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| 产品名称 | Akt ↓ ↑ | Akt1 ↓ ↑ | Akt2 ↓ ↑ | Akt3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Honokiol | ✔ | MEK | 98% | ||||||||||||||||
| PF-04691502 |
++++
P-Akt (S473), IC50: 3.8 nM P-Akt (T308), IC50: 7.5 nM |
98+% | |||||||||||||||||
| PHT-427 |
+
Akt, Ki: 2.7 μM |
99%+ | |||||||||||||||||
| Deguelin | ✔ | PI3K | 99%+ | ||||||||||||||||
| TIC10 isomer | ✔ | ERK | 98+% | ||||||||||||||||
| Perifosine |
+
Akt, IC50: 4.7 μM |
98% | |||||||||||||||||
| Miltefosine | ✔ | PI3K,PKC | 98% | ||||||||||||||||
| Triciribine |
+
Akt, IC50: 130 nM |
99%+ | |||||||||||||||||
| Uprosertib |
+
Akt1, IC50: 180 nM |
+
Akt2, IC50: 328 nM |
++
Akt3, IC50: 38 nM |
99%+ | |||||||||||||||
| Afuresertib |
++++
Akt1, Ki: 0.08 nM |
++++
Akt2, Ki: 2 nM |
++++
Akt3, Ki: 2.6 nM |
99%+ | |||||||||||||||
| Miransertib |
++++
Akt1, IC50: 5 nM |
++++
Akt2, IC50: 4.5 nM |
++
Akt3, IC50: 16 nM |
98+% | |||||||||||||||
| GSK-690693 |
++++
Akt1, IC50: 2 nM |
+++
Akt2, IC50: 13 nM |
+++
Akt3, IC50: 9 nM |
99%+ | |||||||||||||||
| AT7867 |
++
Akt1, IC50: 32 nM |
++
Akt2, IC50: 17 nM |
++
Akt3, IC50: 47 nM |
PKA | 99%+ | ||||||||||||||
| AKT inhibitor VIII |
++
Akt1, IC50: 58 nM |
+
Akt2, IC50: 210 nM |
+
Akt3, IC50: 2119 nM |
97% | |||||||||||||||
| MK-2206 2HCl |
+++
Akt1, IC50: 8 nM |
+++
Akt2, IC50: 12 nM |
+
Akt3, IC50: 65 nM |
99%+ | |||||||||||||||
| Ipatasertib |
++++
Akt1, IC50: 5 nM |
++
Akt2, IC50: 18 nM |
+++
Akt3, IC50: 8 nM |
99%+ | |||||||||||||||
| AT13148 |
++
Akt1, IC50: 38 nM |
+
Akt2, IC50: 402 nM |
++
Akt3, IC50: 50 nM |
PKA | 95% | ||||||||||||||
| Capivasertib |
++++
Akt1, IC50: 3 nM |
+++
Akt2, IC50: 8 nM |
+++
Akt3, IC50: 8 nM |
99%+ | |||||||||||||||
| A-674563 HCl |
+++
Akt1, Ki: 11 nM |
PKA | 99% | ||||||||||||||||
| CCT128930 |
+++
Akt2, IC50: 6 nM |
PKA | 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 | Crebanine, a natural product isolated and purified from the herbs of Stephania yunnanensis, can eonvert BaCl_2-induced arrhythmia into sinus rhythm in rats, decrease the incidence of VF and CA by CaCl_2 in rats and by chloroform in mice, but has no proteetive effects on ouahain-indueed arrhythmias in guinea pigs. Crebanine also has potential utility of crebanine in the development of neurodegenerative therapy, might be used as the starting point to develop a drug for Alzheimer's disease, can inhibit the proliferation of human leukemic cells (HL-60, U937 and K562), human fibrosarcoma cells (HT1080) and cervix cancer cell lines (KB-3-1 and KB-V1 and it mediates cell cycle arrest at G0/G1 phase and this was associated with down-regulation of cyclins A and D. |
| Concentration | Treated Time | Description | References | |
| U87MG cells | 0, 50, 100, 200 μM | 48 h | To evaluate the effect of CB on GBM cell viability, results showed that CB dose-dependently reduced cell viability | Front Pharmacol. 2024 Jun 4;15:1419044 |
| Osteoblast precursor cells (OPCs) | 5 μM | 48 h | To assess the cytotoxicity of CN on OPCs, results showed that CN did not exhibit significant cytotoxic effects on OPCs at concentrations below 5 μM. | J Cell Mol Med. 2024 Aug;28(16):e70044 |
| bone marrow-derived monocytes (BMMs) | 10 μM | 48 h | To assess the cytotoxicity of CN on BMMs, results showed that CN did not exhibit significant cytotoxic effects on BMMs at concentrations below 15 μM. | J Cell Mol Med. 2024 Aug;28(16):e70044 |
| HepG2 cells | 35, 105, 175 µM | 24 h | To detect the effect of Crebanine on the apoptosis of HepG2 cells, the results showed that Crebanine induced apoptosis by activating ROS and the mitochondrial pathway. | Front Pharmacol. 2023 Feb 16;14:1069093 |
| HepG2 cells | 35, 105, 175 µM | 24 h | To observe the effect of Crebanine on the migration and invasion ability of HepG2 cells, the results showed that Crebanine significantly inhibited cell migration and invasion. | Front Pharmacol. 2023 Feb 16;14:1069093 |
| HepG2 cells | 35, 70, 105, 140, 175, 280 µM | 24, 48, 72 h | To evaluate the inhibitory effect of Crebanine on the proliferation of HepG2 cells, the results showed that Crebanine significantly inhibited cell proliferation in a dose- and time-dependent manner. | Front Pharmacol. 2023 Feb 16;14:1069093 |
| H22 cells | 50-300 μg/mL | 24 and 48 h | To evaluate the inhibitory effect of Crebanine and FA-Cre@PEG-PLGA NPs on the proliferation of H22 cells. The results showed that FA-Cre@PEG-PLGA NPs significantly enhanced the inhibitory effect on H22 cell proliferation under ultrasonic irradiation. | Int J Nanomedicine. 2024 Oct 17;19:10513-10536 |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Xylene-induced ear edema model | Tail vein injection | 5 mg/kg | Single administration | Cre inhibited xylene-induced ear edema in mice. | Front Pharmacol. 2023 Jan 4;13:1092583 |
| C57BL/6J male mice | GC-induced femoral head necrosis model | Intramuscular injection | 5 mg/kg | Three times per week for 3 weeks | To evaluate the therapeutic effect of CN on glucocorticoid-induced femoral head necrosis, results showed that CN significantly improved the trabecular structure of the femoral head. | J Cell Mol Med. 2024 Aug;28(16):e70044 |
| Mice | CHCl3-induced ventricular fibrillation model | Caudal vein injection | 5 mg/kg | Single dose | Evaluate the antiarrhythmic effects of Crebanine and its derivatives. Results showed that Crebanine at 5 mg/kg significantly reduced the incidence of ventricular fibrillation. | Molecules. 2016 Nov 28;21(12):1555 |
| Sprague-Dawley rats and Kunming mice | Orthotopic hepatocellular carcinoma transplantation model | Tail vein injection | 3 mg/kg | Administered every other day for 10 doses | To evaluate the tumor targeting and anti-tumor efficacy of FA-Cre@PEG-PLGA NPs under ultrasonic irradiation. The results demonstrated that FA-Cre@PEG-PLGA NPs significantly prolonged the retention time of the drug at the tumor site and exhibited superior anti-tumor effects under ultrasonic irradiation. | Int J Nanomedicine. 2024 Oct 17;19:10513-10536 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.95mL 0.59mL 0.29mL |
14.73mL 2.95mL 1.47mL |
29.46mL 5.89mL 2.95mL |
|
| CAS号 | 25127-29-1 |
| 分子式 | C20H21NO4 |
| 分子量 | 339.39 |
| SMILES Code | CN1CCC(C2=C3C4=CC=C(OC)C(OC)=C4C[C@@]12[H])=CC5=C3OCO5 |
| MDL No. | MFCD01658977 |
| 别名 | |
| 运输 | 蓝冰 |
| 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 |
DMSO: 105 mg/mL(309.38 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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