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  1. Stem Cell/Wnt MAPK/ERK Pathway Autophagy
  2. Organoid p38 MAPK Autophagy Mitophagy
  3. Adezmapimod hydrochloride

Adezmapimod hydrochloride  (Synonyms: SB 203580 hydrochloride; RWJ 64809 hydrochloride)

目錄號: HY-10256A 純度: 99.37%
COA 產(chǎn)品使用指南 技術(shù)支持

Adezmapimod (SB 203580; RWJ 64809) hydrochloride 是一種選擇性的,ATP 競爭性的 p38 MAPK 抑制劑,對 SAPK2a/p38SAPK2b/p38β2IC50 分別為 50 nM 和 500 nM。Adezmapimod hydrochloride 抑制 LCK,GSK3β 和 PKBα,IC50 比 SAPK2a/p38 高 100-500 倍。Adezmapimod hydrochloride 不抑制 JNK 活性,是一種自噬 (autophagy) 和線粒體自噬 (mitophagy) 激活劑。

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

Adezmapimod hydrochloride Chemical Structure

Adezmapimod hydrochloride Chemical Structure

CAS No. : 869185-85-3

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     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

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10 mM * 1 mL in DMSO ¥363
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5 mg ¥330
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10 mg ¥600
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50 mg ¥1400
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100 mg ¥2100
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Customer Review

Other Forms of Adezmapimod hydrochloride:

MCE 顧客使用本產(chǎn)品發(fā)表的 467 篇科研文獻

WB
IF
IHC

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomaterials. 2018 Aug;175:19-29.  [Abstract]

    Western blotting analysis showing the related protein expression (MHC, MyoD, p38α, phospho-p38α) of C2C12 myoblasts after incubated for 6 days in DM containing 40?μg/mL AuNPs and Au-AgNPs in the presence or absence of SB203580 (SB).

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: PLoS Biol. 2018 May 11;16(5):e2004225.  [Abstract]

    Representative western blots of p-CREB (Ser133) and UCP-1 in iWAT from C57BL/6J mice after 4 wk of SB203580 treatment. These mice are exposed to cold for 2 d before analysis.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Jun 15;15(1):184.  [Abstract]

    Representative immunoblots of total lysates from BV2 cells treated with MPP+or/and U0126 (10 μM), SP600125 (SP, 10 μM) and SB203580 (SB, 10 μM) using the antibodies against DICER.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Phytomedicine. 2018 Mar 15;42:152-163.  [Abstract]

    Cells are pretreated with SP600125 (20 μM), SB203580 (20 μM) or U0126 (20 μM) in presence or absence of KLA, then incubated with LPS (1 μg/mL) for certain time. Cell lysates are subjected to western blot.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Br J Pharmacol. 2018 Dec;175(23):4338-4352.  [Abstract]

    Treatment of macrophages with inhibitor of p38 (SB203580) or JNK (SP600125) inhibits the synthesis of pro-IL-1β in ZFP91-overexpressing THP-1 cells.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-JNK1&JNK1 is downregulated by inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    The protein level of MMP-9 is downregulated by inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-p38&p38 is downregulated by inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    The protein levels of IL-1β and TNF-α are sharply downregulated by the addition of inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-ERK1/2/ERK1/2 is notably reduced by inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Acta Physiol (Oxf). 2018 Feb;222(2).  [Abstract]

    P38 inhibitor SB203580 pretreatment also decreases p-HSP27 and MMP9 levels induced by MICAL2-overexpression.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Jun 27;66(25):6317-6325.  [Abstract]

    HepG2 cells are pre-incubated with 20 μM SB203580, SP600125 and PD98059 for 1 h and then treated with tangeretin(20μM) for 24 h.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Front Immunol. 2018 Dec 7;9:2854.  [Abstract]

    Neutrophils are pretreated with inhibitor of p38 MAPK (SB203580) and ERK1/2 (U0126), and the cells are then incubated with either SS2 ZY05719 or PMA for 3 h. Immunofluorescence is performed.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Am J Physiol Cell Physiol. 2018 Aug 1;315(2):C225-C235.  [Abstract]

    Western blot analysis shows that inhibiting MAPK cannot completely reverse increased expression of RNF2 and CDDP resistance of OC cells.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Cell Mol Med. 2018 Nov;22(11):5450-5467.  [Abstract]

    Treatment with SB203580 significantly abolishes siPlectin-stimulated p38 activation.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: FASEB J. 2019 Feb;33(2):2435-2450.  [Abstract]

    Bile acids (BAs) cause nuclear translocation of NF-kB p65, an effect that is abolished by SB203580.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Endod. 2018 May;44(5):751-758.  [Abstract]

    p38 MAPK inhibition enhances DPC-Exos–induced tube formation. (A) p38 MAPK activity is measured by detecting Phospho-p38 MAPK. The ratio between Phospho-p38 MAPK and the p38 MAPK band is used for quantification. (B) The effects of VEGF-A and KDR expression after p38 MAPK inhibitor SB203580 treatment on DPC-Exos-stimulated HUVECs.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Dec 2.  [Abstract]

    Western analysis of protein expression in the treatment of miR-543 and SB 203580.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Nov;119(10):8450-8459.  [Abstract]

    Western blot results show a reduction in phosphorylated p38 MAPK in ADSCs after treatment with 20 μM SB203580, 20 μM SP600125, or 20 μM PD98059 for 1 hour.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: BMC Pulm Med. 2018 Nov 27;18(1):178.  [Abstract]

    P-p38 and P-Hsp27 are detected by western blotting with the treatment of LPS, SB203580 and SB203580+ LPS.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: BMC Pulm Med. 2018 Nov 27;18(1):178.  [Abstract]

    P-p38 and P-Hsp27 are detected by western blotting with the treatment of LPS, SB203580 and SB203580+ LPS.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;46(5):1779-1792.  [Abstract]

    Western blot bands of p38, phospho-p38, ZO-1, Clau-din-1, and Occludin. JNK inhibitor SP600125 and p38 inhibitor SB203580 are used.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Cell Death Differ. 2017 Mar;24(3):492-499.  [Abstract]

    LPS stimulates ICER expression via p38-CREB pathway. Effect of MAPK and IKK inhibitors on LPS-induced CREB phosphorylation in peritoneal macrophages.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Cancer Lett. 2017 Feb 16;393:22-32.  [Abstract]

    Effects of p38 MAPK inhibitor (SB203580), ERK inhibitor (U0126), JNK inhibitor (SP600125), caspase inhibitor (Z-VAD-FMK) and NAC on SGC-7901 and MGC-803 treated with DOX/VCPA combination treatment. VCPA pretreatment strategy is the same as above. SB203580 (20 μM), U0126 (10 μM), SP600125 (20 μM), Z-VAD-FMK (10 μM) and NAC (5 mM) are treated 2 h before DOX (2 μg/mL) added into the culture, respectively. MAPK pathway protein levels are determined.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Free Radic Biol Med. 2017 Nov;112:49-59.  [Abstract]

    Cells are pre-treated with ERK (U1026) and p38 (SB203580) inhibitors, followed by GL-V9 treatment for 24 h. Western blot is performed to analyze NAG-1 expression.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563.  [Abstract]

    Immunofluorescence analysis for expression of the I-cell marker ΔNP63 on proximal sections of ureters explanted from E12.5 wildtype (control) embryos and cultured for 6 d in the presence of solvent (DMSO) (A), the AKT inhibitor (AKT-i) MK2206 (B), the P38 inhibitor (P38-i) SB203580 (C), the ERK1/2 inhibitor (ERK1/2-i) PD98059 (D) or combinations as indicated (E and F).

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biochem Cell Biol. 2017 Feb;95(1):64-68.  [Abstract]

    The involvement of the p38 MAPK signaling pathways in lactoferrin-induced differentiation of HaCaT keratinocytes. HaCaT cells are differentiated in the presence or absence of 10 μM bovine Lactoferrin for 5 days. PD98059 (40 μM), SB203580 (10 μM), or LY294002 (10 μM) are added at the same time. Cell differentiation is evaluated by the expression levels of Involucrin and Filaggrin. GAPDH is used as a loading control.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Res. 2017; 28 (8): 3383-3386

    Effects of various protease inhibitors on HO-1 and P-gp protein expressions.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2017;10(9):13542-13549.

    SB203580 decreases the expression ratio of p-p38 and p38 to inhibit activation of p38 MARK pathway.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: China Biotechnology. 2017, 37(12): 40-48.

    The Western blot analysis of HOG1 and Phospho-HOG1.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2017 Oct 19;8(60):101965-101983.  [Abstract]

    Representative western blot analysis of P-gp, p38 MAPK and phospho-p38 MAPK expression in MCF-7/MDR and K562/MDR cells treated with 10 μM SB203580 for 48 hr.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:6175841.  [Abstract]

    Involvements of MAPK signaling pathway in CPS-induced apoptosis in ALI cultures of sheep bronchial epithelial cells. Cells are pretreated with SB203580 (a P38 inhibitor, 20?μM) for 1?h, followed by exposure to CPS (100?ng/mL) or MO (MOI = 30) for 48?h. Cell lysates are subjected to Western blotting analysis using indicated antibodies.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Chin Arch Otolaryngol Head Neck Surg. 2016,23(01):49-52.

    Effect of p38MAPK inhibitor on the soft palate reconstruction of the rats with chronic intermittent hypoxia.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Mol Cell Cardiol. 2015 Dec;89(Pt B):268-79.  [Abstract]

    Dose response of MAPK and Akt inhibitors on cardiac fibroblast-derived exosomes (Exo)-induced activation of MAPKs and Akt. Neonatal rat cardiomyocytes are treated with or without Exo (50 μg/mL), U0126, SP600125, MK-2206, and SB023580 for 20 min and subjected to Western blot analysis. The results are from 4 separate experiments.

    查看 p38 MAPK 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    Adezmapimod (SB 203580; RWJ 64809) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride does not disrupt JNK activity and is an autophagy and mitophagy activator[1].

    IC50 & Target[1]

    p38

    50 nM (IC50)

    p38β2

    500 nM (IC50)

    體外研究
    (In Vitro)

    Adezmapimod hydrochloride (用 0-30 μM 預(yù)孵育 1 小時并在 20 ng/mL IL-2 存在下培養(yǎng) 24 小時) 可防止 IL-2 誘導(dǎo)的原代人 T 細胞、鼠 CT6 T 細胞或 BAF 增殖 F7 B 細胞的 IC50 為 3-5 μM[1]。
    Adezmapimod hydrochloride 阻斷 PKB 磷酸化 (IC50 3-5 μM)。Adezmapimod hydrochloride 在 CT6 和活化的人 T 細胞以及 IL-2 反應(yīng)性 BA/F3 F7 B 細胞中以劑量依賴性方式抑制 Ser473 的磷酸化[1]。

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

    Cell Proliferation Assay[1]

    Cell Line: CT6, BA/F3 cell line F7, and PBMC/T cells
    Concentration: 0-30 μM
    Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
    Result: Prevented the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3-5 μM.

    Western Blot Analysis[1]

    Cell Line: CT6 cells, activated human T cells, and BA/F3 F7 cells
    Concentration: 0-30 μM
    Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min
    Result: Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.
    體內(nèi)研究
    (In Vivo)

    Adezmapimod hydrochloride (5 mg/kg/day; 連續(xù)16天每天腹膜內(nèi)注射; 雌性無胸腺 Nu/Nu 小鼠) 處理與平行處理的 p38TM 腫瘤相比,p38WT 腫瘤的腫瘤負荷明顯更小[1]。

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

    Animal Model: Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors[1]
    Dosage: 5 mg/kg/day
    Administration: Intra peritoneal injected daily for 16 consecutive days
    Result: After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10). ?
    分子量

    413.90

    Formula

    C21H17ClFN3OS

    CAS 號
    性狀

    固體

    顏色

    Light yellow to yellow

    運輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    溶解性數(shù)據(jù)
    細胞實驗: 

    DMSO 中的溶解度 : 100 mg/mL (241.60 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)

    H2O 中的溶解度 : 5 mg/mL (12.08 mM; 超聲助溶)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.4160 mL 12.0802 mL 24.1604 mL
    5 mM 0.4832 mL 2.4160 mL 4.8321 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 (sealed storage, away from moisture)。-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。

    * 備注:如您選擇水作為儲備液,請稀釋至工作液后,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: ≥ 2.5 mg/mL (6.04 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 (6.04 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

    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)。

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    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: 99.71%

    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 (sealed storage, away from moisture)。-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
    H2O / DMSO 1 mM 2.4160 mL 12.0802 mL 24.1604 mL 60.4011 mL
    5 mM 0.4832 mL 2.4160 mL 4.8321 mL 12.0802 mL
    10 mM 0.2416 mL 1.2080 mL 2.4160 mL 6.0401 mL
    DMSO 15 mM 0.1611 mL 0.8053 mL 1.6107 mL 4.0267 mL
    20 mM 0.1208 mL 0.6040 mL 1.2080 mL 3.0201 mL
    25 mM 0.0966 mL 0.4832 mL 0.9664 mL 2.4160 mL
    30 mM 0.0805 mL 0.4027 mL 0.8053 mL 2.0134 mL
    40 mM 0.0604 mL 0.3020 mL 0.6040 mL 1.5100 mL
    50 mM 0.0483 mL 0.2416 mL 0.4832 mL 1.2080 mL
    60 mM 0.0403 mL 0.2013 mL 0.4027 mL 1.0067 mL
    80 mM 0.0302 mL 0.1510 mL 0.3020 mL 0.7550 mL
    100 mM 0.0242 mL 0.1208 mL 0.2416 mL 0.6040 mL

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

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    • 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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