货号:A346669 同义名: Vincaleukoblastine sulfate salt;Vinblastine (sulfate)
Vinblastine Sulfate is a natural product targeting on microtubule formation, and also inhibits nAChR with IC50 value of 8.9 μM.
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产品名称 | AChE ↓ ↑ | AChR ↓ ↑ | mAChR ↓ ↑ | nAChR ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Donepezil |
+++
hAChE, IC50: 11.6 nM bAChE, IC50: 8.12 nM |
98% | |||||||||||||||||
Loganin |
++
AChE, IC50: 3.95 μM |
99%+ | |||||||||||||||||
topride HCl |
++
AChE, IC50: 2.04 μM |
98% | |||||||||||||||||
Dehydroevodiamine HCl | ✔ | 99%+ | |||||||||||||||||
Jatrorrhizine |
++
AChE, IC50: 872 nM |
99%+ | |||||||||||||||||
Palmatine |
++
AChE, IC50: 0.51 μM |
98% | |||||||||||||||||
(-)-Huperzine A |
++++
AChE (G4 form), Ki: 7 nM |
98% | |||||||||||||||||
Galanthamine HBr |
++
AChE, IC50: 0.35 μM |
98% | |||||||||||||||||
Trospium chloride | ✔ | 99% | |||||||||||||||||
Tiotropium Bromide Monohydrate | ✔ | 98+% | |||||||||||||||||
Gallamine Triethiodide |
+
AChR, IC50: 68.0 μM |
98% | |||||||||||||||||
Hexamethonium Bromide | ✔ | 99% | |||||||||||||||||
Pancuronium dibromide | ✔ | 98% | |||||||||||||||||
Neostigmine bromide | ✔ | 98% | |||||||||||||||||
Orphenadrine citrate | ✔ | 98% | |||||||||||||||||
Oxybutynin | ✔ | 98% | |||||||||||||||||
Irsogladine | ✔ | PDE | 98% | ||||||||||||||||
Pyridostigmine bromide | ✔ | 99+% | |||||||||||||||||
Rivastigmine |
+
AChR, IC50: 5.5 μM |
98% | |||||||||||||||||
Paroxetine hydrochloride | ✔ | 97% | |||||||||||||||||
Rocuronium Bromide | ✔ | 98% | |||||||||||||||||
Tropicamide |
+++
M4 mAChR, IC50: 8 nM |
98% | |||||||||||||||||
Diphenmanil methylsulfate | ✔ | 98% | |||||||||||||||||
Umeclidinium bromide | ✔ | 95% | |||||||||||||||||
Otilonium bromide | ✔ | 98% | |||||||||||||||||
Flavoxate HCl |
+
mAChR, IC50: 12.2 μM |
98% | |||||||||||||||||
Ipratropium bromide | ✔ | 98% | |||||||||||||||||
Diphenidol HCl | ✔ | 98% | |||||||||||||||||
Darifenacin hydrobromide |
++++
M3 mAChR, pKi: 8.9 |
98% | |||||||||||||||||
Aclidinium Bromide |
++++
M4 mAChR, Ki: 0.21 nM M2 mAChR, Ki: 0.1 nM |
98% | |||||||||||||||||
Oxybutynin chloride | ✔ | 99% | |||||||||||||||||
Pentoxyverine citrate | ✔ | 98% | |||||||||||||||||
Solifenacin | ✔ | 98% | |||||||||||||||||
Catharanthine | ✔ | 98% | |||||||||||||||||
Benzethonium chloride |
+++
α4β2 nAChRs, IC50: 49 nM α7 nAChRs, IC50: 122 nM |
99+% | |||||||||||||||||
Vinblastine sulfate |
+
nAChR, IC50: 8.9 μM |
99% | |||||||||||||||||
PNU-120596 |
++
α7 nAChR, EC50: 216 nM |
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。 |
靶点 |
|
描述 | Vinblastine, while not causing depolymerization of spindle microtubules, effectively blocks mitosis (e.g., IC50 0.8 nM in HeLa cells), leading to apoptotic cell death [2]. In NB4 cells, vinblastine induces alterations in p53 and DNA fragmentation. Its antiproliferative effect involves inducing apoptosis by disrupting the Bax/Bcl-2 balance. Vinblastine also suppresses NFκB expression and activity while activating JNK, resulting in apoptosis through a caspase-dependent pathway [3]. Vinblastine induces apoptosis, characterized by mitochondrial membrane potential loss, cytochrome c and apoptosis-inducing factor release, caspase-9 and caspase-3 activation, and Poly (ADP-ribose) Polymerase cleavage [4]. |
体内研究 | Vinblastine, an extensively utilized anticancer medication, is associated with undesirable side effects. Its conjugation with carrier molecules presents a potentially effective strategy for mitigating these adverse effects [5]. |
体外研究 | Vinblastine, while not causing depolymerization of spindle microtubules, effectively blocks mitosis (e.g., IC50 0.8 nM in HeLa cells), leading to apoptotic cell death [2]. In NB4 cells, vinblastine induces alterations in p53 and DNA fragmentation. Its antiproliferative effect involves inducing apoptosis by disrupting the Bax/Bcl-2 balance. Vinblastine also suppresses NFκB expression and activity while activating JNK, resulting in apoptosis through a caspase-dependent pathway [3]. Vinblastine induces apoptosis, characterized by mitochondrial membrane potential loss, cytochrome c and apoptosis-inducing factor release, caspase-9 and caspase-3 activation, and Poly (ADP-ribose) Polymerase cleavage [4]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
142BR cells | Cytotoxicity assay | 48 h | Cytotoxicity against human 142BR cells after 48 hrs by SRB assay, IC50=37.6 μM | 19467877 | |
A375 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human A375 cells after 48 hrs by SRB assay, IC50=7.2 μM | 19467877 | |
A549 cells | Proliferation assay | 48 h | Antiproliferative activity against human A549 cells after 48 hrs by MTS assay, IC50=2.36 μM | 22546674 | |
ACHN cells | Cytotoxicity assay | 48 h | Cytotoxicity against human ACHN cells after 48 hrs by SRB assay, IC50=22.7 μM | 19467877 | |
Dose | Mice: 10 mg/kg[3] (median lethal dose, i.v.) Rat: 2.9 mg/kg[3] (median lethal dose, i.v.); 2.9 mg/kg[3] (median lethal dose, p.o.) |
Administration | i.v., p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.10mL 0.22mL 0.11mL |
5.50mL 1.10mL 0.55mL |
11.00mL 2.20mL 1.10mL |
CAS号 | 143-67-9 |
分子式 | C46H60N4O13S |
分子量 | 909.053 |
别名 | Vincaleukoblastine sulfate salt;Vinblastine (sulfate);VLB;Vincaleukoblastinesulfate;Velsar;Velban®;Rozevinsulfate;Exal;Alkaban-AQ;29060-LE;Vincaleukoblastine;NSC-49842 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 45 mg/mL(49.5 mM),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 H2O: 50 mg/mL(55 mM),配合低频超声助溶 |
动物实验配方 |