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  1. Membrane Transporter/Ion Channel
  2. Na+/H+ Exchanger (NHE)
  3. FR183998 free base

FR183998 free base 是一種有效的 Na+/H+-exchange 抑制劑,通過測量在大鼠淋巴細胞、血小板及人血小板 pHi 值的變化中,得到 IC50 值分別為 0.3 nM,6.5 nM 和 3.1 nM。

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FR183998 free base Chemical Structure

FR183998 free base Chemical Structure

CAS No. : 239440-20-1

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規(guī)格 價格 是否有貨 數量
10 mM * 1 mL in DMSO ¥2968
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1 mg ¥1230
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5 mg ¥3150
In-stock
10 mg ¥4970
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50 mg 現貨 詢價
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Customer Review

  • 生物活性

  • 實驗參考方法

  • 純度 & 產品資料

  • 參考文獻

生物活性

FR183998 free base is a potent Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively.

IC50 & Target

IC50: 0.3 nM (Na+/H+-exchange, Rat lymphocytes), 3.1 nM (Na+/H+-exchange, Human platelet), 6.5 nM (Na+/H+-exchange, Rat platelet)[1]

體外研究
(In Vitro)

FR183998 free base is a Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 6.5 nM and 3.1 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively[1].

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

體內研究
(In Vivo)

FR183998 (0.1 and 1.0 mg/kg, i.v.) shows no effect hemodynamic parameters, and does not affect mean blood pressure and heart rate in conscious rats. Pretreatment of 0.01, 0.032, 0.10 mg/kg FR183998 or posttreament of 0.032 and 0.10 mg/kg FR183998 via intravenous administration, dose-dependently reuces reperfusion-induced ventricular fibrillation (VF) and mortality in reperfusion-induced arrhythmias in anesthetized rats, with ED50s against VF of 0.015 mg/kg and 0.070 mg/kg, respectively. FR183998 also reduces myocardial infarct sizes, and suppresses the arrhythmias in anesthetized rats[1]. FR183998 (1 mg/kg, i.v.) reduces the increase in serum levels of alanine transaminase, aspartate transaminase, and lactate dehydrogenase induced by hepatic I/R, and prevents the incidences of hepatic necrosis, apoptosis, and neutrophil infiltration. FR183998 blocks the I/R-induced activation of the NF-κB, reduces induction of iNOS and inhibits the production of nitric oxide. FR183998 also decreases the expression of the iNOS gene antisense transcript in the liver of hepatic I/R rats[2].

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

分子量

428.34

Formula

C17H19Cl2N5O2S

CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數據
細胞實驗: 

DMSO 中的溶解度 : 250 mg/mL (583.65 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質量 1 mg 5 mg 10 mg
1 mM 2.3346 mL 11.6730 mL 23.3459 mL
5 mM 0.4669 mL 2.3346 mL 4.6692 mL
查看完整儲備液配制表

* 請根據產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,避免反復凍融造成的產品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內使用,-20°C儲存時,請在1個月內使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
=
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

掃碼獲得
動物溶解方案

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

動物數量

由于實驗過程有損耗,建議您多配一只動物的量
純度 & 產品資料
參考文獻
Cell Assay
[1]

Intracellular pH of rats lymphocytes is measured at 37°C with a spectrofluorometer by using the ratio of the emission (530 nm) obtained at 490- and 440-nm excitation wavelengths. After addition of 10 μL of the BCECF- and acid-loaded cells to 460 μL of Na-free buffer with 5 μL of DMSO or FR183998, 25 μL of 2.0 M NaCl (final 100 mM) is applied to start the reaction. The pHi change of cells is measured for >2 min. The initial increase in pHi in response to the added NaCl is taken as an estimate of Na+/H+-exchange activity, and the inhibitory effect of the drug is evaluated as IC50 value. The BCECF fluorescence signals are calibrated by titration with stepwise addition of small volumes of 1 M MES after permeabilization of the cells with 0.5% Triton X-100[1].

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

Animal Administration
[1]

Male Sprague-Dawley rats age 9-10 weeks are anesthetized with sodium pentobarbital (50 mg/kg, i.p.), intubated, and ventilated with room air at a stroke volume of 4.5 mL with a frequency of 50 strokes/min. Saline or FR183998 is injected into the left femoral vein (bolus i.v.) 5 min before occlusion. Thoracotomy for coronary artery ligation is performed at the left side of the thorax above the heart, and the origin of the left anterior descending coronary artery is occluded by applying negative tension by aspiration through polyethylene tubing connected to the vacuum system, which can achieve regional ischemia. Successful occlusion is confirmed by ischemia-induced alteration of electrocardiogram (ECG). After 5-min ischemia, reperfusion is performed, and the incidence of ventricular tachycardia (VT) and ventricular fibrillation (VF) of >5 s is observed intermittently over a 5-min period of reperfusion[1].

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

參考文獻

完整儲備液配制表

* 請根據產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,避免反復凍融造成的產品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內使用,-20°C儲存時,請在1個月內使用。

可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3346 mL 11.6730 mL 23.3459 mL 58.3649 mL
5 mM 0.4669 mL 2.3346 mL 4.6692 mL 11.6730 mL
10 mM 0.2335 mL 1.1673 mL 2.3346 mL 5.8365 mL
15 mM 0.1556 mL 0.7782 mL 1.5564 mL 3.8910 mL
20 mM 0.1167 mL 0.5836 mL 1.1673 mL 2.9182 mL
25 mM 0.0934 mL 0.4669 mL 0.9338 mL 2.3346 mL
30 mM 0.0778 mL 0.3891 mL 0.7782 mL 1.9455 mL
40 mM 0.0584 mL 0.2918 mL 0.5836 mL 1.4591 mL
50 mM 0.0467 mL 0.2335 mL 0.4669 mL 1.1673 mL
60 mM 0.0389 mL 0.1945 mL 0.3891 mL 0.9727 mL
80 mM 0.0292 mL 0.1459 mL 0.2918 mL 0.7296 mL
100 mM 0.0233 mL 0.1167 mL 0.2335 mL 0.5836 mL

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產品名稱:
FR183998 free base
目錄號:
HY-100302
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