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Apamin

小电导Ca2+激活K+通道（KCa2，SK）抑制剂,Apamin 是一种在蜂毒中发现的18个氨基酸的肽神经毒素，可阻断Ca 2+激活的K+通道，且预防肝纤维化。

目录号: PC12228 纯度: ≥98%

CAS No. :24345-16-2

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中文名称

Apamin

中文别名

蜂毒明肽;蜂毒明肽(蜜蜂由来);蜂毒明肽<电离质谱校准物>;蜂针液明肽

英文名称

Apamin

英文别名

Apamin;CYS-ASN-CYS-LYS-ALA-PRO-GLU-THR-ALA-LEU-CYS-ALA-ARG- ARG-CYS-GLN-GLN-HIS-NH2(DISULFIDE BRIDGE:CYS1-CYS11, CYS3-CYS15);CYS-ASN-CYS-LYS-ALA-PRO-GLU-THR-ALA-LEU-CYS-ALA-ARG-ARG-CYS-GLN-GLN-HIS-NH2;APAMIN FROM BEE VENOM;APAMIN FROM HONEY BEE VENOM;APAMIN,BEE VENOM;apamine;CNCKAPETALCARRCQQH-NH2;M.W. 2027.34 C79H131N31O24S4;32,15-(Iminoethaniminopropanodithiomethano)-31H-pyrrolo[2,1-e1][1,2,5,8,11,14,17,20,23,26,29,32,35,38]dithiadodecaazacyclohentetracontine,cyclic peptide deriv.;Apamin (reduced), cyclic (1®11),(3®15)-bis(disulfide);L-Histidinamide,L-cysteinyl-L-asparaginyl-L-cysteinyl-L-lysyl-L-alanyl-L-prolyl-L-a-glutamyl-L-threonyl-L-alanyl-L-leucyl-L-cysteinyl-L-alanyl-L-arginyl-L-arginyl-L-cysteinyl-L-glutaminyl-L-glutaminyl-,cyclic (1®11),(3®15)-bis(disulfide);Ro 23-6721;66: PN: WO2008088422 FIGURE: 8 claimed protein;68: PN:WO2006116156 SEQID: 68 claimed protein;L-Cysteinyl-L-asparaginyl-L-cysteinyl-L-lysyl-L-alanyl-L-prolyl-L-alpha-glutamyl-L-threonyl-L-alanyl-L-leucyl-L-cysteinyl-L-alanyl-L-arginyl-L-arginyl-L-cysteinyl-L-glutaminyl-L-glutaminyl-L-histidinamide cyclic (1-11) (3-15)-bis(disulfide) = Cys-Asn-Cys-Lys-Ala-Pro-Glu-Thr-Ala-leu-Cyc-Ala-Arg-Arg-Cys-Gln-Gln-His-NH2

Cas No.

24345-16-2

分子式

C₇₉N₃₁O₂₄S₄H₁₃₁

分子量

2027.34

包装储存

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca-activated K (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.

性状

Solid

IC50 & Target[1][2]

K channel

体外研究(In Vitro)

Apamin (0.5-2 μg/mL; 24 hours; HSC-T6 cells) treatment markedly reduces the expression of α-SMA in the TGF-β1-induced HSC-T6 cells. Apamin treatment abrogats the activation of p-Smad2/3 and Smad4 induced by TGF-β1.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	HSC-T6 cells
Concentration:	0.5 μg/mL, 1 μg/mL and 2 μg/mL
Incubation Time:	24 hours
Result:	Markedly reduced the expression of α-SMA in the TGF-β1-induced HSC-T6 cells. Abrogated the activation of p-Smad2/3 and Smad4 induced by TGF-β1.

体内研究(In Vivo)

Apamin (0.1 mg/kg; intraperitoneal injection; twice a week; for 4 weeks; C57BL/6 male mice) treatment results in decreased liver injury and proinflammatory cytokine levels. Apamin suppresses the deposition of collagen, proliferation of BECs and expression of fibrogenic genes in the 3,5-diethoxycarbonyl-1,4-dihydrocollidine (DDC)-fed mice.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	8-week-old C57BL/6 male mice (20-25 g) with DDC feeding
Dosage:	0.1 mg/kg
Administration:	Intraperitoneal injection; twice a week; for 4 weeks
Result:	Resulted in decreased liver injury and proinflammatory cytokine levels. Suppressed the deposition of collagen, proliferation of BECs and expression of fibrogenic genes in the DDC-fed mice.

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

SequenceShortening

CNCKAPETALCARRCQQH-NH2 (Disulfide bridge: Cys1-Cys11;Cys3-Cys15)

Sequence

Cys-Asn-Cys-Lys-Ala-Pro-Glu-Thr-Ala-Leu-Cys-Ala-Arg-Arg-Cys-Gln-Gln-His-NH2 (Disulfide bridge: Cys1-Cys11;Cys3-Cys15)

参考文献

[1]. Kim JY, et al. Apamin suppresses biliary fibrosis and activation of hepatic stellate cells. Int J Mol Med. 2017 May;39(5):1188-1194. [Information]

溶解度数据

体外研究:

H₂O : 100 mg/mL (49.33 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.4933 mL	2.4663 mL	4.9326 mL
5 mM	0.0987 mL	0.4933 mL	0.9865 mL
10 mM	0.0493 mL	0.2466 mL	0.4933 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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