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  1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel
  3. Cilnidipine

Cilnidipine  (Synonyms: 西尼地平; FRC-8653)

目錄號(hào): HY-17404 純度: 99.92%
COA 產(chǎn)品使用指南

Cilnidipine 是一種長(zhǎng)效的第二代二氫吡啶類 Ca2+ 通道阻斷劑,可有效作用于 L 和 N 型 Ca2+ 通道[1]。具有抗高血壓作用。

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Cilnidipine Chemical Structure

Cilnidipine Chemical Structure

CAS No. : 132203-70-4

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10 mM * 1 mL in DMSO ¥385
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5 mg ¥218
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10 mg ¥350
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Other Forms of Cilnidipine:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Cilnidipine is a long-acting, second-generation dihydropyridine Ca2+-channel blocker on L and N-type Ca2+ channel[1][2][3][4]. Antihypertensive effects[5].

體外研究
(In Vitro)

Cilnidipine inhibits the L-type current with an IC50 of 100 nM in neurons pretreated with omegaCgTx plus omegaAgTx[1].
The IC50 for Cilnidipine in respect of the N-type current is 200 nM[1].
Cilnidipine dose- and time-dependently inhibits Ba2+ currents in A7r5 cells with the IC50 at 10 nM after 10 min[2].
Cilnidipine dose-dependently inhibits depolarization- and Ca2+-induced contractions of rat aortic rings, with an IC50 of 10 nM at 10 min[2].
The viability of nPC12 cells show no significant change up to 150?μM Cilnidipine, but it decreases slightly in the cells treated with greater than 200?μM Cilnidipine[3].
Cilnidipine (100 μM, 2 hours) treatment increases the expression of p85aPI3K p-Akt, p-GSK-3β, and heat shock transcription factor (HSTF-1), and decreases levels of cytosolic cytochrome c, activated caspase 3, and cleaved PARP[3].

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

Cell Viability Assay

Cell Line: Neuronally differentiated PC12 (nPC12) cells
Concentration: 0, 1, 5, 10, 25, 50, 100, 150, and 200 μM
Incubation Time: Treated for 2 hours; cell viability was measured after 24 hours
Result: Cell viability was not affected by low concentrations up to 150 μM, but it was slightly decreased at 200 μM.

Western Blot Analysis

Cell Line: nPC12 cells
Concentration: 100 μM
Incubation Time: 2 hours
Result: Increased the IRs of p58a PI3K, p-Akt, p-GSK-3β, and HSTF-1 and decreased the Immunoreactivities (IRs) of cytosolic cytochrome c, activated caspase 3 (17 kDa), and cleaved PARP (85 kDa).
體內(nèi)研究
(In Vivo)

Cilnidipine has potent inhibitory actions on N-type as well as L-type voltage-dependent Ca2+-channel in rat dorsal root ganglion neurons[1].
Administration of Cilnidipine (10 mg/kg) and Nimodipine (10 mg/kg) significantly attenuates the immobilized stress-induced behavioral changes and restored memory deficits along with normalization of the corticosterone levels[4].
Cilnidipine and Nimodipine produce comparable beneficial effects in restoring immobilization stress subjected mice[4].
Oral administration of Cilnidipine (3 mg/kg) markedly lowers both systolic and diastolic blood pressure 1 hr after administration in 2K1C renal hypertensive dogs[5].

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

Animal Model: Swiss albino mice weighing 25±5 g[4]
Dosage: 5 and 10 mg/kg
Administration: administered i.p. 30 min prior to immobilization stress
Result: Cilnidipine (10 mg/kg, i.p.) and nimodipine (10 mg/kg, i.p.) 30 min prior to subjecting immobilization stress resulted in significant attenuation of immobilization stress-induced decrease in locomotor activity.
Administration with Cilnidipine (5 mg/kg, i.p.) and Nimodipine (5 mg/kg, i.p.) did not show any significant effect on the stressed mice.
Administration of Cilnidipine (10 mg/kg, i.p.) and Nimodipine (10 mg/kg, i.p.) in the non-stressed mice, and vehicle in the stressed mice did not modulate locomotor activity in a significant manner.
Clinical Trial
分子量

492.52

Formula

C27H28N2O7

CAS 號(hào)
性狀

固體

顏色

Light yellow to green yellow

中文名稱

西尼地平

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : ≥ 100 mg/mL (203.04 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.0304 mL 10.1519 mL 20.3037 mL
5 mM 0.4061 mL 2.0304 mL 4.0607 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.08 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.08 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中,混合均勻。

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0304 mL 10.1519 mL 20.3037 mL 50.7594 mL
5 mM 0.4061 mL 2.0304 mL 4.0607 mL 10.1519 mL
10 mM 0.2030 mL 1.0152 mL 2.0304 mL 5.0759 mL
15 mM 0.1354 mL 0.6768 mL 1.3536 mL 3.3840 mL
20 mM 0.1015 mL 0.5076 mL 1.0152 mL 2.5380 mL
25 mM 0.0812 mL 0.4061 mL 0.8121 mL 2.0304 mL
30 mM 0.0677 mL 0.3384 mL 0.6768 mL 1.6920 mL
40 mM 0.0508 mL 0.2538 mL 0.5076 mL 1.2690 mL
50 mM 0.0406 mL 0.2030 mL 0.4061 mL 1.0152 mL
60 mM 0.0338 mL 0.1692 mL 0.3384 mL 0.8460 mL
80 mM 0.0254 mL 0.1269 mL 0.2538 mL 0.6345 mL
100 mM 0.0203 mL 0.1015 mL 0.2030 mL 0.5076 mL
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產(chǎn)品名稱:
Cilnidipine
目錄號(hào):
HY-17404
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