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Pilocarpine HCl.

(Synonyms: 盐酸毛果芸香碱)
目录号: PC16554 纯度: ≥98%
非选择性毒蕈碱乙酰胆碱受体激动剂。Pilocarpine Hydrochloride 是一种选择性的 M3 型毒蕈碱乙酰胆碱受体 (M3 muscarinic receptor) 激动剂。
CAS No. :54-71-7
商品编号 规格 价格 会员价 是否有货 数量
PC16554-100mg 100mg ¥535.00 请登录
PC16554-500mg 500mg ¥968.00 请登录
PC16554-10mM (in 1mL DMSO) 10mM (in 1mL DMSO) ¥637.00 请登录
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中文名称
Pilocarpine HCl.
中文别名
盐酸毛果芸香碱;( )-毛果芸香碱盐酸盐;(+)-毛果芸香碱盐酸盐;毛果芸香碱;毛果芸香碱盐酸盐;匹鲁卡品盐酸盐;盐酸毛果芸香碱 USP标准品;盐酸毛果芸香碱 标准品;盐酸匹罗卡品;盐酸匹罗卡品 EP标准品;(3S,4R)-4,5-二氢-3-乙基-4-(1-甲基-1H-咪唑-5-基甲基)-2(3H)-呋喃酮盐酸盐;氨噻唑;盐酸匹鲁卡品
英文名称
Pilocarpine HCl
英文别名
(+)-Pilocarpine hydrochloride;pilocarpine hcl;Pilocarpine Hydrochloride;(+)-Pilocarpine (hydrochloride);Pilocarpine (Hydrochloride);Pilocarpine Hydrochl;(3S,4R);(3S,4R)-3-ethyl-4-[(1-methyl-1H-imidazol-5-yl)-methyl]dihydrofuran-2(3H)one hydrochloride;Akarpine;ami-pilo;amisturap;pilocar;pilocarpine,2(3H)-furanone,3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)-methyl] monohydrochloride,(3S-cis);pilocel;pilovisc;Salagen;Sanpilo;(3S,4R)-4,5-Dihydro-3-ethyl-4-(1-methyl-1H-imidazol-5-ylmethyl)-2(3H)-furanone hydrochloride;Pilocarpal;Almocarpine;Pilocar SMP;Adsorbocarpine;Pilomiotin;Sno pilo;Mistura P;Pilocarpine muriate;Epicar;MI-Pilo Ophth Sol;Isopto-carpine;Isopto carpine;Amistura P;Pilocarpine, hydrochloride;Spersacarpine hydrochloride;Pilokarpin monohydrochloride;Pilocarpine monohydrochloride;PILOPINE HS;pilocarpine-hcl;Pilocarpine chloride;Pilopine HS Gel
Cas No.
54-71-7
分子式
C11H17ClN2O2
分子量
244.72
包装储存

4°C, sealed storage, away from moisture

*该产品在溶液状态不稳定,建议您现用现配,即刻使用。

生物活性

Pilocarpine Hydrochloride is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.

性状

Solid

IC50 & Target[1][2]

M3 muscarinic receptor

体外研究(In Vitro)

To evaluate the cytotoxicity of Pilocarpine, the morphology and viability of human corneal stromal (HCS) cells are examined by light microscopy and MTT assay, respectively. Morphological observations show that HCS cells exposed to Pilocarpine at a concentration from 0.625 to 20 g/L exhibit dose- and time-dependent proliferation retardation and morphological abnormality such as cellular shrinkage, cytoplasmic vacuolation, detachment from culture matrix, and eventually death, while no obvious difference is observed between those exposed to Pilocarpine below the concentration of 0.625 g/L and controls. Results of MTT assay reveal that the cell viability of HCS cells decrease with time and concentration after exposing to Pilocarpine above the concentration of 0.625 g/L (P<0.01 or 0.05), while that of HCS cells treated with Pilocarpine below the concentration of 0.625 g/L show no significant difference to controls. The partial muscarinic agonist, Pilocarpine, evokes concentration-dependent relaxation with an EC50 of 2.4 mM in isolated segments of rat tail artery that were constricted with Penylephrine (10 to 200 nM).

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

体内研究(In Vivo)

The Pilocarpine-induced saliva secretion of the control rats (CN) and exercised (EX) rats is examined. A significantly greater amount of saliva is induced by Pilocarpine in the EX rats than in the CN rats (P<0.01). Conversely, the Na concentration in the saliva of the EX rats is significantly lower than that of the CN rats (P<0.05).

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

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*该产品在溶液状态不稳定,建议您现用现配,即刻使用。

ClinicalTrial
结构分类
来源
参考文献
溶解度数据
体外研究: 

DMSO : 100 mg/mL (408.63 mM; Need ultrasonic)

H2O : ≥ 37 mg/mL (151.19 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.0863 mL 20.4315 mL 40.8630 mL
5 mM 0.8173 mL 4.0863 mL 8.1726 mL
10 mM 0.4086 mL 2.0432 mL 4.0863 mL
*

建议根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备溶液;该产品在溶液状态不稳定,建议您现用现配,即刻使用

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

    建议依照次序添加每种溶剂: PBS

    Solubility: 130 mg/mL (531.22 mM); Clear solution; Need ultrasonic

  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.50 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.50 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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 ddH?O 中,得到澄清透明的生理盐水溶液
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.50 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.50 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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
  • 4.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.50 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.50 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

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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