BAY 11-7082

别名: BAY 11-7821

BAY 11-7082 (BAY 11-7821)是一种 NF-κB 抑制剂,抑制TNFα诱导的 IκBα 磷酸化,在肿瘤细胞中IC50为10 μM。BAY 11-7082 可抑制 ubiquitin-specific protease USP7USP21,对应的IC50值分别为0.19 μM和0.96 μM。BAY 11-7082 在胃癌细胞中可诱导凋亡和S期阻滞。

BAY 11-7082 Chemical Structure

BAY 11-7082 Chemical Structure

CAS: 19542-67-7

规格 价格 库存 购买数量
10mg 738.58 现货
50mg 2223.41 现货
1g 16298.1 现货
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BAY 11-7082相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
SP6.5 Growth Inhibition Assay 2.5-20 μM 24 h  IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner 23443086
OM431 Function Assay 5 μM 2 h decreases translocation of p65 in the nucleus  23443086
OCM1 Function Assay 5 μM 2 h decreases translocation of p65 in the nucleus  23443086
VUP Function Assay 5 μM 2 h decreases translocation of p65 in the nucleus  23443086
SP6.5 Function Assay 5 μM 2 h decreases translocation of p65 in the nucleus  23443086
BAFs Function Assay 0.5/1 μM 24 h inhibits TNFα/DEX induced CYP19A1 transcripts 23485457
KMS-12-BM Apoptosis Assay 30 µM 3 h induces MM cell death involves necrosis 23527154
MM.1S Apoptosis Assay 30 µM 3 h induces MM cell death involves necrosis 23527154
HT29 Function Assay 10/30/100 μM 1 h inhibits TNF-induced phosphorylation and degradation of IκBα 23527154
HT29 Function Assay 10/30/100 μM 1 h inhibites both TWEAK-induced p100 processing 23527154
HUVEC Function Assay 10 μM 0.5 h counteractes the loss of Tie2 mRNA 23563632
RAW 264  Function Assay 0.2-5 µM 30/60/90 min inhibits the phosphatase activity of PTP1B  23578302
AM Growth Inhibition Assay 5 µM 4/8 d reduces the viability of intracellular MTB 23634218
MDM Growth Inhibition Assay 5 µM 4/8 d reduces the viability of intracellular MTB 23634218
THP-1  Growth Inhibition Assay 5 µM 4/8 d reduces the viability of intracellular MTB 23634218
THP-1 Function Assay 5 µM 1 h inhibits MTB-induced NFκB activation 23634218
HepG2 Function Assay 0.3/1/3 μM 48 h reduces IL6-induced PON1 expression 23791833
HBE  Function Assay 10μM 3h abolishes the increases of IL-6 expression induced by CSE 23824089
HGC-27  Apoptosis Assay 7.5/15/30 μM 6 h induces apoptosis in a time- and dose-dependent manner 23846545
MGC80-3 Function Assay 7.5/15/30 μM 6 h induces the dephosphorylation and up-regulation of IκBα 23846545
HGC-27  Function Assay 7.5/15/30 μM 6 h induces the dephosphorylation and up-regulation of IκBα 23846545
MGC80-3 Growth Inhibition Assay 10/20/30 μM 6/24 h suppresses cell viability significantly 23846545
AGS Growth Inhibition Assay 10/20/30 μM 6/24 h suppresses cell viability significantly 23846545
NCI-N87 Growth Inhibition Assay 10/20/30 μM 6/24 h suppresses cell viability significantly 23846545
A549 Apoptosis Assay 1 μM 48 h reduces the cell death induced by combined stimulation 23900080
A549 Function Assay 1 μM 48 h enhances the up-regulation of IκB and subsequent decrease in Bax expression induced by combined stimulation 23900080
THP-1  Function Assay 10 μM 1 h abolishes the effect of rHSP27 on SR-A mRNA 23939398
PC-3 Function Assay 2.5/5/10 μM 0.5 h blocks IGF-II-induced STS mRNA expression  24055520
iNKT Function Assay 10/100 μM 0.5 h inhibits the induction of A2AR mRNA and other factor 24124453
IVD  Function Assay 10 μM 3 d abrogates TNF-α–induced up-regulation of ADAMTS-4 and ADAMTS-5  24176808
IVD  Function Assay 10 μM 3 d reverses TNF-α–mediated suppression of the disc matrix macromolecules aggrecan and collagen II 24176808
A549RT-eto Function Assay 10 μM 24 h decreases the expression levels of NF-κB and P-gp  24220725
A549RT-eto Apoptosis Assay 10 μM 24 h accelerates F14 extract-mediated apoptosis combined treatment with F14 24220725
WPs Function Assay 25 μM 5 min suppresses ATP and vWF secretion 24331207
DSCs  Function Assay 2.5 μM 0.5 h reverses the enhancement of CCL2/CCR2 expression of DSCs induced by IL-33 24344240
OVCXCR2 Function Assay 2 µM 48 h blocks the CXCL1-induced cell invasion 24376747
SKCXCR2  Function Assay 2 µM 48 h blocks the CXCL1-induced cell invasion 24376747
SKCXCR2  Growth Inhibition Assay 2 µM 48 h decreases cell proliferation significantly 24376747
THP-1  Function Assay 0.1/1 μM 0.5 h abrogates TNF-α secretion as well as the increased secretion of IL-6 and IL-1β 24378536
A549RT-eto Apoptosis Assay 10 μM 24 h accelerates FERO-mediated apoptosis 24535083
HUVEC Function Assay 20 µM 0.5 h prevents the induction of EAM expression 24551209
A549 Function Assay 10 μM 1 h inhibits the increase of phospho-IκBα in PA103-infected cultures  24612488
HeLa  Function Assay 5 μM 24 h reduces the activity of TNF-α promoter  24657783
HUVECs Function Assay 3-30 μM 1 h reduces the expression of miR-146a in a dose-dependent manner 24863965
macrophages Function Assay 5 µM 3 h partially blocks YPFS-induced expression of iNOS and COX-2  24967898
RAW 264.7 Function Assay 5 μM 1 h inhibits TNF-α and IL-12 p40 production 25019567
A549  Function Assay 10 µM 12 h suppresses Dvl-3 induced activation of p65 25156800
HMECs Function Assay 5 μM 2 h abolishes TNF-α-induced VCAM-1 expression  25193116
HCT116 Function Assay 5 μM 2 h attenuates silymarin-induced downregulation of cyclin D1 25479723
ARPE-19 Function Assay 1 μM 0.5 h suppresses TG-induced IL-8 promoter activation 25593029
SiHa  Function Assay 10 μM 1.5 h abolishes BPA induced up regulation of FN and MMP-9  25797437
HeLa Function Assay 10 μM 1.5 h abolishes BPA induced up regulation of FN and MMP-9  25797437
VUP Growth Inhibition Assay 2.5-20 μM 24 h  IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner 23443086
OCM1 Growth Inhibition Assay 2.5-20 μM 24 h  IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner 23443086
OM431 Growth Inhibition Assay 2.5-20 μM 24 h  IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner 23443086
SP6.5 Apoptosis Assay 5 μM 24 h  induces apoptosis  23443086
VUP Apoptosis Assay 5 μM 24 h  induces apoptosis  23443086
OCM1 Apoptosis Assay 5 μM 24 h  induces apoptosis  23443086
OM431 Apoptosis Assay 5 μM 24 h  induces apoptosis  23443086
SP6.5 Function Assay 5 μM 12 h reduces the migration  23443086
VUP Function Assay 5 μM 12 h reduces the migration  23443086
OCM1 Function Assay 5 μM 12 h reduces the migration  23443086
OM431 Function Assay 5 μM 12 h reduces the migration  23443086
HBL-1  Growth Inhibition Assay 3 μM 24/48/72 h slows cell growth modestly 23441730
RAW 264.7 Function Assay 2-15 μM 1 h suppresses the activation of IKK family members 23441730
IL-1R  Function Assay 2-15 μM 1 h suppresses the activation of IKK family members 23441730
RAW 264.7 Function Assay 15 μM 1 h suppresses the activation of and JNK 23441730
IL-1R  Function Assay 15 μM 1 h suppresses the activation of and JNK 23441730
U2OS Function Assay 15 μM 1 h prevents the LPS- or IL-1-stimulated formation of K63-pUb chains  23441730
MT‐1  Function Assay 8 µm 3 h decreases the levels of p‐STAT3 and p‐4EBP1 23278479
MT‐2  Function Assay 8 µm 3 h decreases the levels of p‐STAT3 and p‐4EBP1 23278479
MT‐1  Function Assay 8 µm 3 h decreases the levels of the p65 subunit of NF‐κB  23278479
MT‐2  Function Assay 8 µm 3 h decreases the levels of the p65 subunit of NF‐κB  23278479
MCF-7  Function Assay 2.5-15 μM 0.5 h causes the gradual loss of cell adhesion 23093227
HaCaT  Function Assay 5.0 μM 1 h  attenuates the TCOH-induced production of IL-6  23041168
OA chondrocytes  Function Assay 10 μM 1 h blocks the AGE-BSA-induced gene/protein expression of GRP78 or COX-2 (p<0.05) 22982228
RAW264.7 Function Assay 15 μM 15-120 min blocks the production of NO, PGE2, and TNF-α 22745523
RAW264.7 Growth Inhibition Assay 5-30 μM 24 h inhibits cell growth in a dose-dependent manner 22745523
HBL6 Apoptosis Assay 0.5/5/25 μM 6/24 h decreases cell viability and leeads to apoptosis in a dose-dependent manner  22074820
HT29  Function Assay 1-10 μM 10 h increases HO-1 mRNA and protein expression 21620964
Ca9–22 Apoptosis Assay 10 μM  1 h completely inhibits ALA-PDT-induced apoptosis 21138480
Ca9–22 Function Assay 10 μM  1 h completely abrogates the ALA-PDT-induced JNK activation 21138480
A-549 Growth Inhibition Assay 10 μM  24/48 h inhibits cell growth in a time-dependent manner 20866043
AP Function Assay 5/10 μM 48 h downregulates the BAD protein level a dose-dependent manner 20596645
AQ1 Function Assay 5/10 μM 48 h downregulates the BAD protein level a dose-dependent manner 20596645
AP Function Assay 20 μM 4/8 h downregulates the BAD protein level a time-dependent manner 20596645
AQ1 Function Assay 20 μM 4/8 h downregulates the BAD protein level a time-dependent manner 20596645
THP-1 Function Assay 5 μM  0.5 h attenuates the LPS-induced p-IκBα protein by 72% 20309718
K562 Growth Inhibition Assay 2-30 μM 24 h IC50=8 μM,inhibits cell growth in a dose-dependent manner 19646807
Jurket Growth Inhibition Assay 2-30 μM 24 h IC50=7.1 μM, inhibits cell growth in a dose-dependent manner 19646807
U937 Growth Inhibition Assay 2-30 μM 24 h IC50=10.5 μM, inhibits cell growth in a dose-dependent manner 19646807
PBMC Growth Inhibition Assay 2-30 μM 24 h IC50=40.2 μM, inhibits cell growth in a dose-dependent manner 19646807
K562 Apoptosis Assay 2-20 μM  24 h induces a dose-dependent apoptosis 19646807
HEK293 Function assay 20 uM 24 hrs Inhibition of TNF-alpha stimulated NFkappaB transactivation in HEK293 cells at 20 uM measured after 24 hrs by dual luciferase reporter gene assay 27736063
RAW264.7 Function assay 20 uM 1 hr Inhibition of LPS-induced NFkB activation in mouse RAW264.7 cells assessed as reduction in nuclear translocation of p65 at 20 uM preincubated for 1 hr followed by LPS stimulation measured after 3 hrs by Western blot method 28667873
RAW264.7 Function assay 20 uM 6 hrs Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells at 20 uM treated 30 mins before LPS challenge measured after 6 hrs by luciferase reporter gene assay 24315191
RAW264.7 Antinflammatory assay 20 uM 18 hrs Antinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 20 uM treated 30 mins before LPS challenge measured after 18 hrs by Griess assay 24315191
THP1 Antinflammatory assay 5 uM 24 hrs Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced extracellular IL-1beta level at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA 24400858
THP1 Antinflammatory assay 5 uM 24 hrs Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced extracellular TNF-alpha production at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA 24400858
THP1 Antinflammatory assay 5 uM 24 hrs Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced intracellular proIL-1beta level at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA 24400858
THP1 Antinflammatory assay 5 uM 24 hrs Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced intracellular IL-1beta level at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA 24400858
RAW264.7 Function assay 0.3 ug/ml 12 hrs Inhibition of LPS-induced NF-kB p65 phosphorylation in mouse RAW264.7 cells at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by Western blot method 28284806
RAW264.7 Function assay 0.3 ug/ml 12 hrs Inhibition of LPS-induced NF-kB p65 activation in mouse RAW264.7 cells at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by DAPI staining based inverted fluorescence microscopic method 28284806
RAW264.7 Function assay 0.3 ug/ml 12 hrs Inhibition of NF-kB p65 in mouse RAW264.7 cells assessed as reduction in LPS-induced iNOS expression at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by Western blot method 28284806
RAW264.7 Function assay 0.3 ug/ml 12 hrs Inhibition of NF-kB p65 in mouse RAW264.7 cells assessed as reduction in LPS-induced COX2 expression at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by Western blot method 28284806
HEK293 Function assay 20 uM 24 hrs Inhibition of TNFalpha-induced NFkappaB activation in HEK293 cells at 20 uM after 24 hrs by dual luciferase reporter gene assay 28873303
RAW264.7 Function assay 20 uM 2 hrs Inhibition of NFkappaB nuclear translocation in LPS-stimulated mouse RAW264.7 cells at 20 uM pretreated for 2 hrs followed by LPS-induction by DAPI-staining based immunofluorescence microscopic method 29759725
BGC823 Function assay 5 uM 12 hrs Inhibition of colony formation in human BGC823 cells at 5 uM treated for 12 hrs followed by incubation in drug free medium for 14 days by crystal violet staining based assay 28881286
SGC7901 Function assay 5 uM 12 hrs Inhibition of colony formation in human SGC7901 cells at 5 uM treated for 12 hrs followed by incubation in drug free medium for 14 days by crystal violet staining based assay 28881286
RAW264.7 Function assay 10 uM 2 hrs Inhibition of LPS-induced IL-6 mRNA expression in mouse RAW264.7 cells at 10 uM pre-incubated for 2 hrs before LPS stimulation for 24 hrs by qRT-PCR method 27038497
RAW264.7 Function assay 10 uM 2 hrs Inhibition of LPS-induced IL-1beta mRNA expression in mouse RAW264.7 cells at 10 uM pre-incubated for 2 hrs before LPS stimulation for 24 hrs by qRT-PCR method 27038497
RAW264.7 Function assay 10 uM 2 hrs Inhibition of LPS-induced iNOS mRNA expression in mouse RAW264.7 cells at 10 uM pre-incubated for 2 hrs before LPS stimulation for 24 hrs by qRT-PCR method 27038497
FaDu Function Assay 2 h inhibits p65 expression and blocks TNFα-induced TWIST expression 24220622
A549  Function Assay 1 h inhibits LTA-induced SP-A mRNA production significantly 23031213
THP1 Cytotoxicity assay 72 hrs Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 72 hrs by MTT assay, TC50 = 1.5 μM. 28410442
RAW264.7 Function assay 6 hrs Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells treated 30 mins before LPS challenge measured after 6 hrs by luciferase reporter gene assay, IC50 = 1.72 μM. 24315191
HEK293 Function assay 6 hrs Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM. 24533857
HEK293 Function assay 6 hrs Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM. 24992702
HEK293 Function assay 6 hrs Inhibition of TNFalpha-induced NF-kappaB activity (unknown origin) transfected in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM. 26343828
HEK293 Function assay 6 hrs Inhibition of TNFalpha-induced NF-kappaB activity expressed in human HEK 293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM. 22850207
HEK293 Function assay 6 hrs Inhibition of TNFalpha-induced human NFkappaB activity in HEK293 cells incubated for 6 hrs followed by compound wash out measured after 5 mins by by luciferase assay, IC50 = 2.01 μM. 22712432
HEK293 Function assay 6 hrs Inhibition of TNFalpha-induced NFkappaB (unknown origin) activation expressed in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 5 μM. 23316950
HEK293 Cytotoxicity assay Cytotoxicity against HEK293 cells, IC50 = 3.8 μM. 24533857
HEK293 Function assay Effect on Cdc2 expressed in HEK293 cells assessed as effect on Cdc2:Cdc25C interaction complexes in presence of camptothecin by EYFP and/or YFP Venus fragment based reporter gene assay 16680159
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生物活性

产品描述 BAY 11-7082 (BAY 11-7821)是一种 NF-κB 抑制剂,抑制TNFα诱导的 IκBα 磷酸化,在肿瘤细胞中IC50为10 μM。BAY 11-7082 可抑制 ubiquitin-specific protease USP7USP21,对应的IC50值分别为0.19 μM和0.96 μM。BAY 11-7082 在胃癌细胞中可诱导凋亡和S期阻滞。
靶点
E2-conjugating enzymes [6]
(Cell-free assay)
USP7 [7]
(Cell-free assay)
USP21 [7]
(Cell-free assay)
USP6 [7]
(Cell-free assay)
IκBα phosphorylation [1]
(Tumor cells)
0.19 μM 0.96 μM 1.7 μM 10 μM
体外研究(In Vitro)
体外研究活性

BAY 11-7082完全且特异性地废除 NF-κB DNA结合, 下调NF-κB-诱导的细胞因子IL-6,且诱导细胞凋亡。[1]

BAY 11-7082 (< 8 μM) 有效抑制原有的和TNFα 刺激的NF-κB荧光素酶活性,这种作用存在剂量依赖性。BAY 11-7082 (8 μM) 强抑制NCI-H1703 细胞增殖。 [2]

Bay 11-7082 (5 μM)作用于感染HTLV-I的T细胞系,快速且有效的降低NF-κB的DNA结合力,且下调抗凋亡基因Bcl-x(L)的表达,而对另一种转录因子AP-1与DNA结合没有作用效果。Bay 11-7082诱导原代ATL细胞发生凋亡比正常的外周血单核细胞更明显,而诱导的这些细胞凋亡也与NF-κB活性的下调相关。Bay 11-7082 (5 μM) 选择性诱导感染HTLV-I的T细胞系发生细胞凋亡,且下调 cyclin D1, cyclin D2, 和 Bcl-xL的表达。 [3]

BAY 11-7082 (100 μM)作用于小鼠海马脑片区,抑制NMDA引起的p65发生 核易位,也抑制NMDA诱导的NF-κB结合力的增强。BAY 11-7082抑制NMDA毒性发生在海马脑片区的CA1区,20 μM时,对40%神经有保护作用,100 μM时,对70%神经有保护作用。[4]

作用于脂肪组织,实验中所有浓度的BAY 11-7082都显著抑制 NF-κB p65 DNA结合活性,而作用于骨骼肌,只有50 μM 和 100 μM 的BAY 11-7082显著抑制NF-κB p65 DNA结合活性。BAY 11-7082 (100 μM) 作用于人体脂肪组织和骨骼肌,降低IKK-β蛋白。BAY 11-7082 (100 μM) 显著降低TNF-α从动物脂肪组织中释放,而 IL-6 和 IL-8 的释放显著抑制实验中BAY 11-7082的所有浓度。 BAY 11-7082 (50 μM)作用于骨骼肌,显著降低 TNF-α, IL-6, 和IL-8 的释放。[5]

此外,BAY 11-7082还被发现抑制了 E2-conjugating酶和E3 ligase酶的活性,从而诱导了B-淋巴癌细胞和T淋巴癌细胞的死亡。 [6]

细胞实验 细胞系 NCI-H1703 细胞
浓度 ~8 μM
孵育时间 12 小时
方法

细胞在96孔板中转染siRNA,然后在完全NSCLC 培养基中培养72小时,再使用BAY 11-7082 处理12小时。细胞与[3H]胸甘温育3小时。使用自动细胞收集器将细胞收集到过滤器上,然后通过β-闪烁计数法测量放射性。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot NF-κB p-IKKβ/ IκBα p-IRAK4 / IRAK4 NF-κB p-IKKβ/ IκBα p-IRAK4 / IRAK4 31332209
Growth inhibition assay Cell viability Cell viability 31332209

化学信息&溶解度

分子量 207.25 分子式

C10H9NO2S

CAS号 19542-67-7 SDF Download BAY 11-7082 SDF
Smiles CC1=CC=C(C=C1)S(=O)(=O)C=CC#N
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 41 mg/mL ( (197.82 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 10 mg/mL (48.25 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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