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Catharanthine/长春质碱 {[allProObj[0].p_purity_real_show]}

货号:A247451 同义名: (+)-3,4-Didehydrocoronaridine

Catharanthine在10 μM时表现出对毒蕈碱受体的拮抗作用,并以IC50值59.6 μM完全抑制了烟碱受体介导的膈肌收缩。作为抗肿瘤药物长春花碱和长春新碱的前体,它也能抑制微管蛋白自组装成微管。

Catharanthine/长春质碱 化学结构 CAS号:2468-21-5
Catharanthine/长春质碱 化学结构
CAS号:2468-21-5
Catharanthine/长春质碱 3D分子结构
CAS号:2468-21-5
Catharanthine/长春质碱 化学结构 CAS号:2468-21-5
Catharanthine/长春质碱 3D分子结构 CAS号:2468-21-5
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Catharanthine/长春质碱 纯度/质量文件 产品仅供科研

货号:A247451 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AChE AChR mAChR nAChR 其他靶点 纯度
Donepezil +++

bAChE, IC50: 8.12 nM

hAChE, IC50: 11.6 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

95%
(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

98%
Galanthamine HBr ++

AChE, IC50: 0.35 μM

98%
Trospium chloride 99%
Tiotropium Bromide Monohydrate 97%
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

98%
Hexamethonium Bromide 99%
Pancuronium dibromide 98%
Neostigmine bromide 98%
Orphenadrine citrate 98%
Oxybutynin 98%
Irsogladine PDE 99%
Pyridostigmine bromide 99+%
Rivastigmine +

AChR, IC50: 5.5 μM

98%
Paroxetine HCl 99%
Rocuronium Bromide 98%
Tropicamide +++

M4 mAChR, IC50: 8 nM

98%
Diphenmanil methylsulfate 99%
Umeclidinium bromide 95%
Otilonium bromide 98%
Flavoxate HCl +

mAChR, IC50: 12.2 μM

99%
Ipratropium bromide 98%
Diphenidol HCl 98%
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

98%
Aclidinium Bromide ++++

M2 mAChR, Ki: 0.1 nM

M4 mAChR, Ki: 0.21 nM

98%
Oxybutynin chloride 99%
Pentoxyverine citrate 98%
Solifenacin 98%
Catharanthine 98%
Benzethonium chloride +++

α7 nAChRs, IC50: 122 nM

α4β2 nAChRs, IC50: 49 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。

Catharanthine/长春质碱 生物活性

靶点
  • nAChR

描述 Catharanthine is a constituent of anticancer vinca alkaloids. Catharanthine evoked concentration-dependent decreases (I(max) >98%) in endothelium-independent tonic responses of aortic rings to phenylephrine (PE) and KCl (IC50 = 28 µM for PE and IC50 = 34 µM for KCl) and of third-order branches of the small mesenteric artery (MA) (IC50 = 3 µM for PE and IC50 = 6 µM for KCl). Catharanthine also increased the inner vessel wall diameter (IC50 = 10 µM) and reduced intracellular free Ca2+ levels (IC50 = 16 µM) in PE-constricted MAs. Patch-clamp studies demonstrated that catharanthine inhibited voltage-operated L-type Ca2+ channel (VOCC) currents in cardiomyocytes and VSMCs (IC50 = 220 µM and IC50 = 8 µM, respectively) of MA[3].

Catharanthine/长春质碱 参考文献

[1]Pereira DM, Ferreres F, et al. Pharmacological effects of Catharanthus roseus root alkaloids in acetylcholinesterase inhibition and cholinergic neurotransmission. Phytomedicine. 2010 Jul;17(8-9):646-52.

[2]Prakash V, Timasheff SN. Mechanism of interaction of vinca alkaloids with tubulin: catharanthine and vindoline. Biochemistry. 1991 Jan 22;30(3):873-80.

[3]Jadhav A, Liang W, Papageorgiou PC, Shoker A, Kanthan SC, Balsevich J, Levy AS, Heximer S, Backx PH, Gopalakrishnan V. Catharanthine dilates small mesenteric arteries and decreases heart rate and cardiac contractility by inhibition of voltage-operated calcium channels on vascular smooth muscle cells and cardiomyocytes. J Pharmacol Exp Ther. 2013 Jun;345(3):383-92.

Catharanthine/长春质碱 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.97mL

0.59mL

0.30mL

14.86mL

2.97mL

1.49mL

29.72mL

5.94mL

2.97mL

Catharanthine/长春质碱 技术信息

CAS号2468-21-5
分子式C21H24N2O2
分子量 336.43
SMILES Code CCC1=C[C@@]2([H])C[C@]([C@]1([H])[N@@](C2)CC3)(C(OC)=O)C4=C3C5=CC=CC=C5N4
MDL No. MFCD01753356
别名 (+)-3,4-Didehydrocoronaridine
运输蓝冰
InChI Key CMKFQVZJOWHHDV-NQZBTDCJSA-N
Pubchem ID 5458190
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

DMSO: 105 mg/mL(312.1 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

请根据您的动物给药指南选择适当的溶解方案。
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
方案一
方案二
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