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  1. Membrane Transporter/Ion Channel Apoptosis
  2. Sodium Channel Ferroptosis
  3. Levobupivacaine hydrochloride

Levobupivacaine hydrochloride  (Synonyms: 鹽酸左布比卡因; (S)-(-)-Bupivacaine monohydrochloride)

目錄號(hào): HY-B0653A 純度: 99.98%
COA 產(chǎn)品使用指南 技術(shù)支持

Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) 是一種長效的酰胺類局部活性劑,可抑制或緩解疼痛。Levobupivacaine hydrochloride 通過可逆性阻斷神經(jīng)元鈉通道 (sodium channel) 發(fā)揮麻醉鎮(zhèn)痛作用。Levobupivacaine hydrochloride 可抑制心血管等組織的傳遞和傳導(dǎo)沖動(dòng),具有一定的心臟和中樞神經(jīng)毒性。Levobupivacaine hydrochloride 在體內(nèi)由細(xì)胞色素P450 (CYP450) 代謝。Levobupivacaine hydrochloride 也可通過 miR-489-3p/SLC7A11 信號(hào)通路誘導(dǎo)胃癌鐵死亡 (ferroptosis)。

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Levobupivacaine hydrochloride Chemical Structure

Levobupivacaine hydrochloride Chemical Structure

CAS No. : 27262-48-2

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10 mM * 1 mL in DMSO ¥500
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Customer Review

Other Forms of Levobupivacaine hydrochloride:

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

查看 Sodium Channel 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer[1][2][3].

IC50 & Target

Sodium channels, Ferroptosis[1]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
13 μM
Compound: Levo-(S)-bupivacaine
Inhibition of wild-type human ERG channel expressed in CHO cells by whole-cell patch clamp technique
Inhibition of wild-type human ERG channel expressed in CHO cells by whole-cell patch clamp technique
[PMID: 21624711]
CHO IC50
83 μM
Compound: Levo-(S)-bupivacaine
Inhibition of human ERG Y652A mutant channel expressed in CHO cells by whole-cell patch clamp technique
Inhibition of human ERG Y652A mutant channel expressed in CHO cells by whole-cell patch clamp technique
[PMID: 21624711]
HEK293 IC50
1013 μM
Compound: Levo-(S)-bupivacaine
Inhibition of human ERG F656A mutant channel expressed in HEK293 cells assessed as blockade of potassium tail current by whole-cell patch clamp technique
Inhibition of human ERG F656A mutant channel expressed in HEK293 cells assessed as blockade of potassium tail current by whole-cell patch clamp technique
[PMID: 21624711]
HEK293 IC50
13 μM
Compound: Levo-(S)-bupivacaine
Inhibition of wild-type human ERG channel expressed in HEK293 cells assessed as blockade of potassium tail current by whole-cell patch clamp technique
Inhibition of wild-type human ERG channel expressed in HEK293 cells assessed as blockade of potassium tail current by whole-cell patch clamp technique
[PMID: 21624711]
HEK293 IC50
278 μM
Compound: Levo-(S)-bupivacaine
Inhibition of human ERG Y652A mutant channel expressed in HEK293 cells assessed as blockade of potassium tail current by whole-cell patch clamp technique
Inhibition of human ERG Y652A mutant channel expressed in HEK293 cells assessed as blockade of potassium tail current by whole-cell patch clamp technique
[PMID: 21624711]
體外研究
(In Vitro)

Levobupivacaine (0-4 mM; 24 h) does not affect the viability of GES-1 cells but inhibits the viability of HGC27 and SGC7901 cells[2].
Levobupivacaine (2 mM; 24, 48 or 72 h) enhances Erastin-induced inhibitory impact on HGC27 and SGC7901 cell viabilities; induces the levels of Fe2+, iron, and lipid ROS[2].
Levobupivacaine (2 mM; 24 h) enhances the expression of miR-489-3p in HGC27 and SGC7901 cells, increases the levels of Fe2+ and iron[2].

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

Cell Viability Assay[2]

Cell Line: GES-1, HGC27 and SGC790
Concentration: 0, 0.5, 1, 2 and 4 mM
Incubation Time: 24 h
Result: Did not affect the viability of normal gastric epithelial GES-1 cell lines but inhibited the viability of HGC27 and SGC7901 cells in a dose-dependent manner.

Cell Viability Assay[2]

Cell Line: HGC27 and SGC7901 (incubated with 5 μM erastin)
Concentration: 2 mM
Incubation Time: 24, 48 or 72 h
Result: Enhanced erastin-induced inhibitory impact on HGC27 and SGC7901 cell viabilities; induced the levels of Fe2+, iron, and lipid ROS.

RT-PCR[2]

Cell Line: HGC27 and SGC7901 (incubated with 5 μM erastin)
Concentration: 2 mM
Incubation Time: 24 h
Result: Enhanced the expression of miR-489-3p in HGC27 and SGC7901 cells, increased the levels of Fe2+ and iron.
體內(nèi)研究
(In Vivo)

Levobupivacaine (40 μmol/kg; IP; once daily for 25 days) significantly inhibits SGC7901 cell growth, and enhances the lipid ROS accumulation[2].
Levobupivacaine (5 or 36 mg/kg; IP; single dosage) increases the latency to partial seizures and prevents the occurrence of generalized seizures at low dosage; reduces the latency to N-methyl-d-aspartate (NMDA)-induced seizures and increased seizure severity at high dosage[3].

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

Animal Model: CD1 mice (30-35 g; induced epileptic seizures by injecting with NMDA)[3]
Dosage: 5 or 36 mg/kg
Administration: IP; single dosage
Result: Increased the latency to partial seizures and prevented the occurrence of generalized seizures at 5 mg/kg; reduced the latency to NMDA-induced seizures and increased seizure severity at 36 mg/kg.
Animal Model: SCID nude mice (6-8 weeks; subcutaneously injected with 5×106 SGC7901 cells)[2]
Dosage: 40 μmol/kg
Administration: IP; once daily for 25 days
Result: Significantly inhibited SGC7901 cell growth, and enhanced the lipid ROS accumulation.
Clinical Trial
分子量

324.89

Formula

C18H29ClN2O

CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

鹽酸左布比卡因

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

4°C, sealed storage, away from moisture

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 100 mg/mL (307.80 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

H2O 中的溶解度 : ≥ 50 mg/mL (153.90 mM)

* "≥" 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 3.0780 mL 15.3898 mL 30.7796 mL
5 mM 0.6156 mL 3.0780 mL 6.1559 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 (sealed storage, away from moisture)。-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。

* 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

  • 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;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/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: ≥ 3 mg/mL (9.23 mM); 澄清溶液

    此方案可獲得 ≥ 3 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 30.0 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: ≥ 3 mg/mL (9.23 mM); 澄清溶液

    此方案可獲得 ≥ 3 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 30.0 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)過程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
該產(chǎn)品水溶性佳,請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度,如有需要,請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
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 (sealed storage, away from moisture)。-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
H2O / DMSO 1 mM 3.0780 mL 15.3898 mL 30.7796 mL 76.9491 mL
5 mM 0.6156 mL 3.0780 mL 6.1559 mL 15.3898 mL
10 mM 0.3078 mL 1.5390 mL 3.0780 mL 7.6949 mL
15 mM 0.2052 mL 1.0260 mL 2.0520 mL 5.1299 mL
20 mM 0.1539 mL 0.7695 mL 1.5390 mL 3.8475 mL
25 mM 0.1231 mL 0.6156 mL 1.2312 mL 3.0780 mL
30 mM 0.1026 mL 0.5130 mL 1.0260 mL 2.5650 mL
40 mM 0.0769 mL 0.3847 mL 0.7695 mL 1.9237 mL
50 mM 0.0616 mL 0.3078 mL 0.6156 mL 1.5390 mL
60 mM 0.0513 mL 0.2565 mL 0.5130 mL 1.2825 mL
80 mM 0.0385 mL 0.1924 mL 0.3847 mL 0.9619 mL
100 mM 0.0308 mL 0.1539 mL 0.3078 mL 0.7695 mL

* 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

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產(chǎn)品名稱:
Levobupivacaine hydrochloride
目錄號(hào):
HY-B0653A
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