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  1. Apoptosis Immunology/Inflammation
  2. Apoptosis SOD Caspase Bcl-2 Family
  3. Pendimethalin

Pendimethalin  (Synonyms: 二甲戊靈)

目錄號(hào): HY-B0862 純度: 99.75%
COA 產(chǎn)品使用指南

Pendimethalin 是具有口服活性的除草劑,可控制一年生禾草和某些闊葉雜草。Pendimethalin 通過(guò)激活內(nèi)質(zhì)網(wǎng)應(yīng)激介導(dǎo)的線粒體功能障礙,誘導(dǎo)人臍靜脈內(nèi)皮細(xì)胞的凋亡 (Apoptotic) 細(xì)胞死亡。

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Pendimethalin Chemical Structure

Pendimethalin Chemical Structure

CAS No. : 40487-42-1

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10 mM * 1 mL in DMSO ¥385
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Other Forms of Pendimethalin:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Pendimethalin is an orally active herbicide that controls annual grasses and certain broadleaf weeds. Pendimethalin induces Apoptotic cell death through activating ER stress-mediated mitochondrial dysfunction in human umbilical vein endothelial cells[1][2][3][4].

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HFF IC50
0.26 μM
Compound: 11
Antimicrobial activity against Toxoplasma gondii RH infected in HFF cells by plaque assay
Antimicrobial activity against Toxoplasma gondii RH infected in HFF cells by plaque assay
[PMID: 20145086]
HFF IC50
0.34 μM
Compound: 11
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin I235V mutation infected in HFF cells by plaque assay
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin I235V mutation infected in HFF cells by plaque assay
[PMID: 20145086]
HFF IC50
0.71 μM
Compound: 11
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin I235T mutation infected in HFF cells by plaque assay
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin I235T mutation infected in HFF cells by plaque assay
[PMID: 20145086]
HFF IC50
0.75 μM
Compound: 11
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin S6I mutation infected in HFF cells by plaque assay
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin S6I mutation infected in HFF cells by plaque assay
[PMID: 20145086]
HFF IC50
1 μM
Compound: 11
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin I235L mutation infected in HFF cells by plaque assay
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin I235L mutation infected in HFF cells by plaque assay
[PMID: 20145086]
HFF IC50
1.1 μM
Compound: 11
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin R243C mutation infected in HFF cells by plaque assay
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin R243C mutation infected in HFF cells by plaque assay
[PMID: 20145086]
HFF IC50
12.2 μM
Compound: 11
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin T239I mutation infected in HFF cells by plaque assay
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin T239I mutation infected in HFF cells by plaque assay
[PMID: 20145086]
HFF IC50
13.2 μM
Compound: 11
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin L136F mutation infected in HFF cells by plaque assay
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin L136F mutation infected in HFF cells by plaque assay
[PMID: 20145086]
HFF IC50
2.5 μM
Compound: 11
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin H28Q mutation infected in HFF cells by plaque assay
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin H28Q mutation infected in HFF cells by plaque assay
[PMID: 20145086]
HFF IC50
3.2 μM
Compound: 11
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin V4L mutation infected in HFF cells by plaque assay
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin V4L mutation infected in HFF cells by plaque assay
[PMID: 20145086]
HFF IC50
3.2 μM
Compound: 11
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin F24H mutation infected in HFF cells by plaque assay
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin F24H mutation infected in HFF cells by plaque assay
[PMID: 20145086]
HFF IC50
9.7 μM
Compound: 11
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin R243S mutation infected in HFF cells by plaque assay
Antimicrobial activity against Toxoplasma gondii RH containing alpha1-tubulin R243S mutation infected in HFF cells by plaque assay
[PMID: 20145086]
體外研究
(In Vitro)

Pendimethalin (50 和 100 μM,24 小時(shí)) 顯著降低人類血管內(nèi)皮細(xì)胞 (HUVECs) 的細(xì)胞活力、導(dǎo)致細(xì)胞周期停滯、凋亡、內(nèi)質(zhì)網(wǎng)應(yīng)激、自噬以及線粒體功能障礙[2]。
Pendimethalin (25-100 μM,6 小時(shí)) 抑制 HUVECs 的遷移和管道形成[2]。
Pendimethalin (50-200 μM,3 小時(shí)) 在人類淋巴細(xì)胞中表現(xiàn)出 DNA 損傷[3]

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

Cell Viability Assay[2]

Cell Line: HUVECs
Concentration: 50 and 100 μM
Incubation Time: 24 h
Result: Decreased the cell viability of 57% and 73% at 50 and 100 μM in HUVECs.

Cell Cycle Analysis[2]

Cell Line: HUVECs
Concentration: 50 and 100 μM
Incubation Time: 24 h
Result: Increased the proportion of cells in the G1 phase in HUVECs.

Apoptosis Analysis[2]

Cell Line: HUVECs
Concentration: 50 and 100 μM
Incubation Time: 24 h
Result: Significantly increased proportions of necrotic cells in HUVECs.
體內(nèi)研究
(In Vivo)

Pendimethalin (12.5-50 mg/kg,口服強(qiáng)飼,每天一次,持續(xù) 14 天) 在大鼠骨髓細(xì)胞中表現(xiàn)出 DNA 損傷,并降低了 GSH 和 CAT 的水平,同時(shí)增加了 LPO 的水平[3]。
Pendimethalin (62.5-250 mg/kg,口服一次,持續(xù) 14 天) 在大鼠的肝臟和腎臟中引起氧化應(yīng)激,這表現(xiàn)在超氧化物歧化酶 (SOD)、過(guò)氧化氫酶 (CAT)、谷胱甘肽 (GSH) 和谷胱甘肽 S-轉(zhuǎn)移酶 (GST) 水平明顯下降,同時(shí) TBARS 和羰基含量升高,導(dǎo)致肝臟和腎臟損傷,表現(xiàn)出庫(kù)普弗細(xì)胞活化和白細(xì)胞浸潤(rùn),以及細(xì)胞質(zhì)大內(nèi)泡化和血竇擴(kuò)張[4]。
Pendimethalin (62.5-250 mg/kg,口服一次,持續(xù) 14 天) 明顯上調(diào)了抗炎和凋亡標(biāo)志物,如腫瘤壞死因子 α (TNF-α)、干擾素 γ (IFN-γ)、Bax 和半胱氨酸蛋白酶-3 的表達(dá),并下調(diào)了 Bcl-2,同時(shí) TNF-α 基因的 mRNA 表達(dá)顯著上調(diào)[4]。

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

Animal Model: Male Wistar rats (140±10 g), 8–9 weeks[2]
Dosage: 12.5-50 mg/kg
Administration: oral gavage, daily for 14 days
Result: Induced 1.6, 4.9, and 10.5-fold (p<0.05) increase in comet OTM value at 12.5, 25, and 50 mg/kg b w/day.
分子量

281.31

Formula

C13H19N3O4

CAS 號(hào)
性狀

固體

顏色

Orange to red

中文名稱

二甲戊靈;二甲戊樂(lè)靈

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 50 mg/mL (177.74 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(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.5548 mL 17.7740 mL 35.5480 mL
5 mM 0.7110 mL 3.5548 mL 7.1096 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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(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 (8.89 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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (8.89 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

    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 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
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)。
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

純度: 99.75%

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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(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 3.5548 mL 17.7740 mL 35.5480 mL 88.8699 mL
5 mM 0.7110 mL 3.5548 mL 7.1096 mL 17.7740 mL
10 mM 0.3555 mL 1.7774 mL 3.5548 mL 8.8870 mL
15 mM 0.2370 mL 1.1849 mL 2.3699 mL 5.9247 mL
20 mM 0.1777 mL 0.8887 mL 1.7774 mL 4.4435 mL
25 mM 0.1422 mL 0.7110 mL 1.4219 mL 3.5548 mL
30 mM 0.1185 mL 0.5925 mL 1.1849 mL 2.9623 mL
40 mM 0.0889 mL 0.4443 mL 0.8887 mL 2.2217 mL
50 mM 0.0711 mL 0.3555 mL 0.7110 mL 1.7774 mL
60 mM 0.0592 mL 0.2962 mL 0.5925 mL 1.4812 mL
80 mM 0.0444 mL 0.2222 mL 0.4443 mL 1.1109 mL
100 mM 0.0355 mL 0.1777 mL 0.3555 mL 0.8887 mL
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產(chǎn)品名稱:
Pendimethalin
目錄號(hào):
HY-B0862
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