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  2. MAPK/ERK Pathway
  3. JNK
  4. SR-3306

SR-3306 是一種有效的可滲透腦的選擇性 JNK 抑制劑。

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SR-3306 Chemical Structure

SR-3306 Chemical Structure

CAS No. : 1128096-91-2

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1430
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1 mg ￥590
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5 mg ￥1300
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10 mg ￥2000
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50 mg 現(xiàn)貨 詢價
100 mg   詢價  
200 mg   詢價  

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查看 JNK 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

SR-3306 is a selective, potent, highly brain penetrant JNK inhibitor.

IC50 & Target

JNK

 

體外研究
(In Vitro)

The effect of SR-3306 or Tat-Sab on cell viability in response to oxidative stress is measured by an MTT assay. H9c2 cells treated with 100 μM H2O2/FeSO4 are ~40% viable, whereas the addition of 500 nM SR-3306 or 500 nM SR3562 to cells treated with 100 μM H2O2/FeSO4 increases viability to ~90%, and the addition of 10 μM Tat-Sab peptide to cells treated with 100 μM H2O2/FeSO4 increases viability to ~70% compared with 98% viability in untreated cells. Similar results are found for primary human cardiomyocytes [2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Administration of SR-3306 [10 mg/kg/day (s.c.) for 14 days] increases the number of tyrosine hydroxylase immunoreactive (TH+) neurons in the SNpc by 6-fold and reduces the loss of the TH+ terminals in the striatum relative to the corresponding side of 6-OHDA-lesioned rats that receive only vehicle (p<0.05). In addition, SR-3306 [10 mg/kg/day (s.c.) for 14 days] decreases d-amphetamine-induced circling by 87% compared to 6-hydroxydopamine (6-OHDA)-lesioned animals given vehicle. Steady-state brain levels of SR-3306 at day 14 are 347 nM, which is approximately 2-fold higher than the cell-based IC50 for this compound. Finally, immunohistochemical staining for phospho-c-jun (p-c-jun) reveals that SR-3306 [10 mg/kg/day (s.c.) for 14 days] produces a 2.3-fold reduction of the number of immunoreactive neurons in the substantia nigra pars compacta (SNpc) relative to vehicle treated rats[1]. In lean mice, intraperitoneal (i.p.) or intracerebroventricular (i.c.v.) administration of SR-3306 reduces food intake and body weight. Moreover, i.p. and i.c.v. administrations of SR11935 exert similar anorectic effects as SR3306, which suggests JNK2 or JNK3 mediates aspect of the anorectic effect by pan-JNK inhibition. Furthermore, daily i.p. injection of SR-3306 (7 days) prevents the increases in food intake and weight gain in lean mice upon high-fat diet feeding, and this injection paradigm reduced high-fat intake and obesity in diet-induced obese (DIO) mice[3].

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

490.56

Formula

C28H26N8O
CAS 號
性狀

固體

顏色

Off-white to light yellow

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)
細胞實驗： 

DMSO 中的溶解度 : 125 mg/mL (254.81 mM; 超聲助溶; 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)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.0385 mL 10.1924 mL 20.3849 mL
5 mM 0.4077 mL 2.0385 mL 4.0770 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?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，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
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: ≥ 2.08 mg/mL (4.24 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 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。
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: 99.0%

參考文獻
Cell Assay
[2]

H9c2 cells and primary human cardiomyocytes are grown under normal cell culture conditions (37 °C and 5% CO2) in DMEM supplemented with 10% fetal bovine serum and penicillin/streptomycin. To assure that the cells are actively growing, only cells at ~80% confluency and between passages 5 and 15 are used in our experiments. H9c2 cells and primary human cardiomyocytes are exposed to 500 nM SR-3306, 500 nM SR-3562, 0.01% DMSO vehicle control, 10 μM Tat-SabKIM1, and 10 μM Tat-scramble for 30 min prior to the addition of stress. To induce oxidative stress and mitochondrial dysfunction in H9c2 cells and primary human cardiomyocytes, 100 μM hydrogen peroxide (H2O2)/FeSO4 or 100 μM hydrogen peroxide (H2O2)/FeSO4 is added directly to the media of the cells. The cells are exposed to H2O2/FeSO4 for the times indicated in the experiments[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1][3]

Rats[1]
Four Sprague-Dawley rats are used. SR-3306 is dosed at 2.5 or 10 mg/kg in subcutaneous minipumps at a rate of 5 μL/h, and after 24 h on days 1, 2, 3, 4, 6, 7, 8, 9, 10, 13, and 14 blood, and day 14 brain are collected. Plasma is generated, and the samples are frozen at -80 °C. The plasma and brain are mixed with Acetonitrile (1:5 v/v or 1:5 w/v, respectively). The brain sample is sonicated with a probe tip sonicator to break up the tissue, and samples are analyzed for compound levels by LC-MS/MS. Plasma compound levels are determined against standards made in plasma and brain levels against standards made in blank brain matrix[1].
Mice[3]
Male, lean or DIO C57BL/6 mice are used. The mice are trained to scheduled, daily, 2-hour water access during the light for 2 weeks. On the first day of the conditioned taste aversion (CTA) test, the trained mice are given a novel 0.15% saccharin solution to drink for the first 50?minutes, and are then given an i.p. injection of SR-3306 (30?mg/kg or 60?mg/kg) or the vehicle. The injected mice are then provided water for the remaining 70?min. The next day, the mice are allowed to choose between water and 0.15% saccharin for 50?min. Fluid consumption is calculated[3].

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

SR-3306 相關(guān)分類

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 2.0385 mL 10.1924 mL 20.3849 mL 50.9622 mL
5 mM 0.4077 mL 2.0385 mL 4.0770 mL 10.1924 mL
10 mM 0.2038 mL 1.0192 mL 2.0385 mL 5.0962 mL
15 mM 0.1359 mL 0.6795 mL 1.3590 mL 3.3975 mL
20 mM 0.1019 mL 0.5096 mL 1.0192 mL 2.5481 mL
25 mM 0.0815 mL 0.4077 mL 0.8154 mL 2.0385 mL
30 mM 0.0679 mL 0.3397 mL 0.6795 mL 1.6987 mL
40 mM 0.0510 mL 0.2548 mL 0.5096 mL 1.2741 mL
50 mM 0.0408 mL 0.2038 mL 0.4077 mL 1.0192 mL
60 mM 0.0340 mL 0.1699 mL 0.3397 mL 0.8494 mL
80 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6370 mL
100 mM 0.0204 mL 0.1019 mL 0.2038 mL 0.5096 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.

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產(chǎn)品名稱：
SR-3306
目錄號：
HY-12829
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