成人免费xx,国产又黄又湿又刺激不卡网站,成人性视频app菠萝网站,色天天天天

  2. Membrane Transporter/Ion Channel Immunology/Inflammation GPCR/G Protein Neuronal Signaling Apoptosis
  3. Potassium Channel Histamine Receptor Na+/Ca2+ Exchanger Caspase Apoptosis
  4. Terfenadine

Terfenadine  (Synonyms: 特非那定; (±)-Terfenadine; MDL-991)

目錄號: HY-B1193 純度: 99.91%
COA 產(chǎn)品使用指南

Terfenadine ((±)-Terfenadine) 是一種有效的 hERG 開放通道抑制劑, IC50為 204 nM。Terfenadine 也是一種 H1 組胺受體 (histamine receptor) 拮抗劑，通過調(diào)節(jié) Ca2+ 穩(wěn)態(tài)在黑素瘤細(xì)胞中起到有效的細(xì)胞凋亡誘導(dǎo)作用。 Terfenadine 誘導(dǎo) ROS 依賴性細(xì)胞凋亡，同時激活 Caspase-4，-2，-9。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)

Terfenadine Chemical Structure

Terfenadine Chemical Structure

CAS No. : 50679-08-8

1.  客戶無需承擔(dān)相應(yīng)的運輸費用。

2.  同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥550
In-stock
100 mg ￥500
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Terfenadine:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM[1]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].

IC50 & Target

H1 Receptor

 

Caspase-4

 

Caspase-2

 

Caspase-9

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
0.93 μM
Compound: terfenadine
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
[PMID: 23812503]
HEK293 IC50
0.022 μM
Compound: Terfenadine
Inhibition of human ERG expressed in HEK293 cells by patch clamp method
Inhibition of human ERG expressed in HEK293 cells by patch clamp method
[PMID: 28481112]
HEK293 IC50
0.03 μM
Compound: Terfenadine
Inhibition of wild-type human ERG expressed in HEK293 cells by whole cell patch clamp method
Inhibition of wild-type human ERG expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
HEK293 IC50
0.03 μM
Compound: Terfenadine
Inhibition of human ERG td[wt:Y652A] mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG td[wt:Y652A] mutant expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
HEK293 IC50
0.03 μM
Compound: Terfenadine
Inhibition of human ERG td[wt:F656A] mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG td[wt:F656A] mutant expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
HEK293 IC50
0.03 μM
Compound: Terfenadine
Inhibition of human ERG S624A mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG S624A mutant expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
HEK293 IC50
0.056 μM
Compound: figure 2, R2C1
Inhibition of human Erg expressed in HEK293 cells assessed as rubidium efflux after 4 hrs by atomic absorbance spectrometric analysis
Inhibition of human Erg expressed in HEK293 cells assessed as rubidium efflux after 4 hrs by atomic absorbance spectrometric analysis
[PMID: 22542010]
HEK293 IC50
0.086 μM
Compound: Terfenadine
Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual patch clamp assay
Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual patch clamp assay
[PMID: 30624934]
HEK293 IC50
0.35 μM
Compound: Terfenadine
Inhibition of human ERG Y652A mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG Y652A mutant expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
HEK293 IC50
0.96 μM
Compound: Terfenadine
Inhibition of human ERG F656A mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG F656A mutant expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
HEK293 IC50
1.2 μM
Compound: Terfenadine
Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay
Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay
[PMID: 32392053]
HEK293 IC50
1.32 μM
Compound: Terfenadine
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
[PMID: 22761000]
HEK293 IC50
130 nM
Compound: 1a, terfenadine
Displacement of [3H]astemizole from human ERG expressed in HEK293 cells by scintillation counting method
Displacement of [3H]astemizole from human ERG expressed in HEK293 cells by scintillation counting method
[PMID: 25238555]
HEK293 IC50
56 μM
Compound: 41, Terfenadine
Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay
Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay
[PMID: 16931010]
HEK293 IC50
971 nM
Compound: Terfenadine
Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA
Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA
[PMID: 21300721]
L929 IC50
312 nM
Compound: rac-1
Inhibition of human ERG in L929 cells by whole cell patch-clamp assay
Inhibition of human ERG in L929 cells by whole cell patch-clamp assay
[PMID: 19660947]
L929 IC50
312 nM
Compound: rac-1
Inhibition of human ERG in L929 cells at 10 uM by whole cell patch-clamp assay
Inhibition of human ERG in L929 cells at 10 uM by whole cell patch-clamp assay
[PMID: 19660947]
LLC-PK1 IC50
1.4 μM
Compound: Terfenadine
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
2 μM
Compound: Terfenadine
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
23 μM
Compound: Terfenadine
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
Ventricular myocyte IC50
0.142 μM
Compound: Terfenadine
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
0.25 μM
Compound: Terfenadine
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
0.375 μM
Compound: Terfenadine
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
375 nM
Compound: Terfenadine
Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes
Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes
[PMID: 21300721]
體外研究
(In Vitro)

Terfenadine ((±)-Terfenadine) (4-20 μM; 24 hours) induces dose and time-dependent apoptosis on A375 melanoma cells. The IC50 after 24 h of TEF treatment in complete medium was 10.4 μM for A375 cells, 9.9 μM for Hs294T cells and 9.6 for HT144 cells[2].
? Terfenadine (2-10 μM; 8 hours) induces dose-dependent cytotoxicity[2].
? Terfenadine (10 μM; 8 hours) causes a massive vacuolization of the cytoplasm and autophagic vacuoles of both double and multiple membranes and at various stages. Terfenadine induces autophagy by ROS-dependent and -independent mechanisms[2].

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

Apoptosis Analysis[2]

Cell Line: A375, HT144 and Hs294T cells
Concentration: 4, 8, 12, 16, 20 μM
Incubation Time: 24 hours
Result: Induced dose and time-dependent apoptosis.

Cell Cytotoxicity Assay[2]

Cell Line: A375 melanoma cells
Concentration: 2, 4, 6, 8, 10 μM
Incubation Time: 8 hours
Result: Induces dose-dependent cytotoxicity.

Cell Autophagy Assay[2]

Cell Line: A375 cells
Concentration: 10 μM
Incubation Time: 8 hours
Result: Caused a massive vacuolization of the cytoplasm and autophagic vacuoles of both double and multiple membranes and at various stages.
體內(nèi)研究
(In Vivo)

Terfenadine (p.o.; 40 mg/kg; for 16 days) produces a significant inhibition of tumour growth rate and enhances the anti-cancer effect of EPI in chemo-resistant NSCLC xenograft models[3].

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

Animal Model: 6-week-old male BALB/cA-nu mice[3]
Dosage: 40 mg/kg
Administration: P.o.; for 16 days
Result: Produced a significant inhibition of tumour growth rate.
分子量

471.67

Formula

C32H41NO2
CAS 號
性狀

固體

顏色

White to off-white

中文名稱

特非那定；特非那丁；叔哌丁醇
運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
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)胞實驗： 

DMSO 中的溶解度 : ≥ 50 mg/mL (106.01 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.1201 mL 10.6006 mL 21.2013 mL
5 mM 0.4240 mL 2.1201 mL 4.2403 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，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

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.30 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。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 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

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.30 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。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 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。
動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動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 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲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: 99.91%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1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 2.1201 mL 10.6006 mL 21.2013 mL 53.0032 mL
5 mM 0.4240 mL 2.1201 mL 4.2403 mL 10.6006 mL
10 mM 0.2120 mL 1.0601 mL 2.1201 mL 5.3003 mL
15 mM 0.1413 mL 0.7067 mL 1.4134 mL 3.5335 mL
20 mM 0.1060 mL 0.5300 mL 1.0601 mL 2.6502 mL
25 mM 0.0848 mL 0.4240 mL 0.8481 mL 2.1201 mL
30 mM 0.0707 mL 0.3534 mL 0.7067 mL 1.7668 mL
40 mM 0.0530 mL 0.2650 mL 0.5300 mL 1.3251 mL
50 mM 0.0424 mL 0.2120 mL 0.4240 mL 1.0601 mL
60 mM 0.0353 mL 0.1767 mL 0.3534 mL 0.8834 mL
80 mM 0.0265 mL 0.1325 mL 0.2650 mL 0.6625 mL
100 mM 0.0212 mL 0.1060 mL 0.2120 mL 0.5300 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

您最近查看的產(chǎn)品:

Your information is safe with us. * Required Fields.

   產(chǎn)品名稱：

  

* 需求量：

* 客戶姓名：

 

* Email：

* 電話：

 

* 公司或機構(gòu)名稱：

   留言給我們：

Bulk Inquiry

Inquiry Information

產(chǎn)品名稱：
Terfenadine
目錄號：
HY-B1193
需求量：