Ziconotide acetate(Synonyms: SNX-111 acetate)

发表于由

Ziconotide acetate;(Synonyms: SNX-111 acetate) 纯度: 99.64%

Ziconotide acetate (SNX-111 acetate) 是一种肽，是一种有效且选择性的 N 型钙通道 (N-type calcium channels) 拮抗剂阻断剂。Ziconotide acetate 减少突触传递，并可用于慢性疼痛研究。

Ziconotide acetateamp;;(Synonyms: SNX-111 acetate)

Ziconotide acetate Chemical Structure

CAS No. : 914454-03-8

规格 价格 是否有货 数量
5 mg ￥5800 In-stock
10 mg ￥9000 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

Ziconotide acetate 相关产品

bull;相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library
  • Peptide Library

生物活性

Ziconotide acetate (SNX-111 acetate), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide acetate reduces synaptic transmission, and can be used for chronic pain research[1].

IC50 Target[1]

N-Type Ca2+ Channel

;

体外研究
(In Vitro)

Most native cells express a variety of different calcium channels and as a result, Ziconotide acetate only partially reduces high-voltage-activated calcium currents in differentiated human neuroblastoma IMR32 cells, rat superior cervical ganglion neurons, and rat hippocampal neurons. Ziconotide acetate also reduces calcium currents that result from expression of the α1B subunit in HEK cells, tsa-201 cells, and Xenopus laevis oocytes[1].
Ziconotide acetate delivers its antinociceptive efficacy by reducing the release of pronociceptive neurotransmitters in the dorsal horn of the spinal cord, thereby inhibiting pain signal transmission[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Ziconotide (i.t.; 25-100 pmol/site; 5 μL; on the 4 th, 10 th, 15 th, 20 th, and 24 th days) acetate reduces the levels of IL-1β and IL-23 in the CNS, as well as IL-17 production in the spleen, 25 days after MOG35-55-elicited EAE, in the mouse model of experimental autoimmune encephalomyelitis (EAE)[2].

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

Animal Model: Female C57BL/6mice (18-22 g, 6-8 weeks old) injected with myelin oligodendrocytes glycoprotein[2]
Dosage: 25 pmol/site, 50 pmol/site, 100 pmol/site
Administration: Intrathecal injection; on the 4 th, 10 th, 15 th, 20 th, and 24 th days
Result: Significantly reduced the mechanical hypersensitivity in animals with EAE.

Formula

C102H172N36O32S7.xC2H4O2
CAS 号

914454-03-8
Sequence

Cys-Lys-Gly-Lys-Gly-Ala-Lys-Cys-Ser-Arg-Leu-Met-Tyr-Asp-Cys-Cys-Thr-Gly-Ser-Cys-Arg-Ser-Gly-Lys-Cys-NH2 (Disulfide bridge:Cys1-Cys16;Cys8-Cys20;Cys15-Cys25)
Sequence Shortening

CKGKGAKCSRLMYDCCTGSCRSGKC-NH2 (Disulfide bridge:Cys1-Cys16;Cys8-Cys20;Cys15-Cys25)
中文名称

醋酸齐考诺肽
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Protect from light, stored under nitrogen

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:;

H2O : 100 mg/mL (Need ultrasonic)

DMSO : 25 mg/mL (Need ultrasonic)

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (Infinity mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (Infinity mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (Infinity mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (Infinity mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (Infinity mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (Infinity mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Joseph G McGivern, et al. Ziconotide: a review of its pharmacology and use in the treatment of pain. Neuropsychiatr Dis Treat. 2007 Feb;3(1):69-85.

    [2]. Rodrigo B M Silva, et al. Beneficial Effects of the Calcium Channel Blocker CTK 01512-2 in a Mouse Model of Multiple Sclerosis. Mol Neurobiol. 2018 Dec;55(12):9307-9327.