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39

抑制剂 & 化合物

12

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T36421	Immuno-Oncology Screening Library
	The Immuno-Oncology Screening Library consists of 2 plates and contains more than 90 cancer and immunology-associated compounds in a 96-well Matrix tube rack format as 10 mM stock solutions in DMSO. This library includes a variety of immuno-oncology target modulators, including but not limited to, adenosine, CCR, CXCR, and TLR agonists and antagonists, BTK, PI3K, VEGFR, and BRAF inhibitors, PD-1/PDL-1 interaction inhibitors, and HDAC inhibitors. Please review the product insert for a full list ...
T11344	G150	DNA; cGAS	DNA Damage/DNA Repair; Immunology/Inflammation
	G150 是高选择性h-cGAS 抑制剂，IC50值为 10.2 nM，用于抑制 dsDNA 引发的干扰素表达。
T21980	PD 198306	MEK	MAPK
	PD 198306 是一种具有抗痛觉过敏作用的 MAPK/ERK 激酶 (MEK) 选择性抑制剂。 PD 198306 可降低链脲佐菌素诱导的活性 ERK1 水平升高。
T13396	Zinc Protoporphyrin Zinc Protoporphyrin-9,锌原卟啉,ZnPP,Zn(II)-protoporphyrin IX	Apoptosis; Reactive Oxygen Species; Endogenous Metabolite	Apoptosis; Immunology/Inflammation; Metabolism; NF-κB
	Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) 是一种具有口服活性的，竞争性血红素加氧酶-1 抑制剂，显著减弱间苯三酚对 H2O2 的保护作用，具有抗癌活性。它用于评估人群铁状态与血红蛋白浓度的组合，也可用作个体孕妇和儿童缺铁的筛查标志物。
T67752	Compound V007-6018	Others	Others
	Compound V007-6018是一种类药化合物，用于药物筛选。
T9212	IMB-301	Others; HIV Protease	Microbiology/Virology; Others; Proteases/Proteasome
	IMB-301是根据 hA3G 模型通过虚拟筛选的一种小分子抑制剂。
T4531	GSK2200150A	Antibacterial	Microbiology/Virology
	GSK2200150A 是一种通过高通量筛选活动确定的抗结核剂，对 H37Rv 的 MIC 是 0.38 μM。
TP1204	iRGD peptide c(CRGDKGPDC)	Integrin	Cytoskeletal Signaling
	iRGD peptide (c(CRGDKGPDC)) 是由 9 个氨基酸组成的环肽，具有靶向肿瘤和肿瘤渗透的作用。
T3572	NSC 15364 1,3-Bis(4-aminophenyl)urea,NSC15364	Apoptosis; Others; VDAC	Apoptosis; Membrane transporter/Ion channel; Others
	NSC 15364 (1,3-Bis(4-aminophenyl)urea) 是一种 VDAC1寡聚化和细胞凋亡抑制剂。
T24859	TC-AQP1-1	Aquaporin	Membrane transporter/Ion channel
	TC-AQP1-1 是一种通过虚拟筛选鉴定的水通道蛋白 1 通道的阻断剂，并在低微摩尔浓度下抑制非洲爪蟾卵母细胞肿胀试验中通过 hAQP1 的水通量。
T4062	CAY10602	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	CAY10602 是一种SIRT1激活剂，可剂量依赖性地抑制 THP-1 细胞中脂多糖对 TNF-α 的 NF-κB 依赖性诱导。
T41256	SP-96	Aurora Kinase	Cell Cycle/Checkpoint; Chromatin/Epigenetic
	SP-96 是一种高效的特异性 Aurora B 抑制剂，IC50 为 0.316 nM。 SP-96 在 NCI60 筛选中显示特异性生长抑制，如 MDA-MD-468 (GI50=107 nM)。 SP-96 可用于三阴性乳腺癌研究。
T12258	NSC 601980 (analog)	Others	Others
	NSC 601980 analog is the analog of the NSC601980 which shows antitumor activity in the yeast screening experiment.
T25542	Isamfazone Isamfazona,Isamfazonum
	Isamfazone is utilized in the chemical and pharmacological studies on substituted pyridazones, the discovery of novel anti-inflammatory agents by aligning screening.
T39185	pp60 (v-SRC) Autophosphorylation Site, Phosphorylated pp60 (v-SRC) Autophosphorylation Site, Phosphorylated
	pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is a phosphorylated peptide derived from an EGFR substrate. It serves as a valuable tool for quantifying phosphorylated substrates in screening EGFR Kinase inhibitors.
TP1476	WKYMVM TFA
	WKYMVm is a selective FPR2 agonist with high affinity, which was identified through screening of a synthetic peptide library.
T73752	Glutarylcarnitine lithium
	Glutarylcarnitine lithium 丙二酸尿症和 I 型戊二酸尿症的重要诊断代谢物。
T74626	BBR-BODIPY
	BBR-BODIPY 是一种荧光探针 (fluorescent probe)，可以筛选其与靶细胞的相互作用。BBR-BODIPY 诱导细胞凋亡改变凋亡相关蛋白的表达。储存方式：避光。
T12259	NSC 601980	Others	Others
	NSC 601980 酵母筛选实验结果中显示了抗肿瘤活性, 能够在COLO 205 and HT29细胞株里很好的抑制细胞增殖，Log GI 50分别是-6.6和 -6.9。
T69911	CU-6PMN
	CU-6PM is a new fluorescent RXR agonist. CU-6PMN was designed based on the fact that umbelliferone emits strong fluorescence in a hydrophilic environment, but the fluorescence intensity decreases in hydrophobic environments such as the interior of proteins. The developed assay CU-6PMN enabled screening of rexinoids to be performed easily within a few hours by monitoring changes of fluorescence intensity with widely available fluorescence microplate readers, without the need for processes such a...
T83800	6-Biotin-17-NAD+ sodium 6-Biotin-17-Nicotinamide adenine dinucleotide,β-Nicotinamide-N6-(2-(6-(6-[biotinyl]aminohexanoyl)aminohexanoyl)aminoethyl)adenine dinucleotide
	6-Biotin-17-NAD+ 是信号分子及酶辅因子NAD+的生物素化衍生物，已应用于高通量筛选(HTS)中，用于测定线粒体复合物I（又称NADH脱氢酶）的活性。
T14529L	Bentiromide acetate Bentiromide acetate(37106-97-1 Free base)	Others	Others
	Bentiromide acetate 是一种肽，用于外分泌胰腺功能不全的筛选试验和监测补充胰腺治疗的充分性。它被胰酶胰凝乳蛋白酶分解，生成对氨基苯甲酸(PABA)。
T80151	α-Synuclein 4554W
	α-Synuclein4554W是一种α-Synuclein(aSyn)聚集抑制剂，对应毒性相关。它含GIVNGVKA序列，该序列通过细胞内文库筛选鉴定而来。α-Synuclein4554W能够减少与帕金森病相关的aSyn突变体的原纤维形成。
T36743	CDK7/9 tide
	CDK7/9 tide is peptide substrate for CDK7 or CDK9[1]. [1]. Robert T, et, al. Development of a CDK10/CycM in vitro Kinase Screening Assay and Identification of First Small-Molecule Inhibitors. Front Chem. 2020 Feb 27; 8:147.
T35411	(+)-Biotin 4-Amidobenzoic Acid (sodium salt)
	(+)-Biotin 4-amidobenzoic acid is a substrate of biotinidase, which cleaves biotin amide to give biotin in vivo. Biotin is an essential coenzyme for certain carboxylases and is used to modify histones and regulate gene transcription. Biotinidase has key roles in intestinal absorption of biotin, the transport of biotin in plasma, and in the regulation of histone biotinylation. (+)-Biotin 4-amidobenzoic acid is hydrolyzed by biotinidase to release 4-aminobenzoic acid (PABA), which can be quantifie...
T79556	NDBM	Autophagy	Autophagy
	NDBM为一种结合Pim-1 kinase的肿瘤特异性探针，具备释放强荧光及细胞毒性，用于筛选及杀伤肿瘤细胞。该化合物特异性地靶向溶酶体并对pH值具有高度敏感性，适用于监测自噬(autophagy)过程及细胞内环境在外部刺激下的pH变化。
T69117	Pinafide
	Pinafide is a rodenticide and anti-protozoal agent. Pinafide shows strong cytostatic activity against both HeLa and KB cells and is moderately toxic to both mice and rats. It has been proved active against experimental tumors and shown to be inhibitor of two DNA viruses. Pinafide blocks cell growth by inhibiting DNA and RNA synthesis. It has been shown to bind to double-helical DNA by intercalation. Pinafide inhibited the activity of M. tuberculosis NAD⁺-dependent DNA ligase A at concentrations ...
T82789	Caloxin 1B1
	Caloxin 1B1是一种对PMCA4亲和力高的生物活性肽。该化合物是经由筛选与PMCA4胞外结构域1的结合而发现，能够特异性地在胞外环境中抑制PMCA。鉴于Caloxin 1B1被筛选用于与PMCA的细胞外结构域相结合，它可以被直接应用于细胞和组织中，用以评估其对平滑肌和内皮细胞功能的影响。
T78520	CYT296	Others	Others
	CYT296是一种靶向染色质去凝集的化合物，能增强定义因子(OSKM)介导诱导多能干细胞(iPSC)的生成，并通过诱导小鼠胚胎成纤维细胞(MEFs)染色质的开放状态来促进体细胞的重编程，适用于细胞替代治疗和药物筛选的研究领域。
T35905	Oasomycin B
	Oasomycin B is a bacterial metabolite that has been found inS. baldaciiand has antiprotozoal activity.1It is active againstT. vaginalis(MIC = 62.5 μg/ml). 1.Grabley, S., Kretzschmar, G., Mayer, M., et al.Secondary metabolites by chemical screening, 24. Oasomycins, new macrolactones of the desertomycin familyLiebigs Ann. Chem.5573-589(1993)
T35706	25-Desacetyl Rifampicin
	25-Desacetyl rifampicin is a major active metabolite of the rifamycin antibiotic rifampicin .125-Desacetyl rifampicin is active againstM. smegmatis(MIC99= 2.66 μM). 1.Kigondu, E.M., Njoroge, M., Singh, K., et al.Synthesis and synergistic antimycobacterial screening of chlorpromazine and its metabolitesMed. Chem. Commun.5502-506(2014)
T83131	AMC-GlcNAc
	AMC-GlcNAc (compound 1) 作为一款高效荧光探针，主要用于β-己糖胺酶活性的检测与表征。该探针能在连续监测中开启荧光，并且在宽广pH值范围内维持稳定的荧光信号（Ex=325 nm, Em=390 nm）。AMC-GlcNAc还支持高灵敏度与低背景信号的比率荧光检测，适用于筛选大肠杆菌细胞裂解物中重组分散素B的活性。
T38187	6-Aminophenanthridine
	6-Aminophenanthridine is an antiprion agent. It inhibits prion formation in yeast- and mammalian-based screening assays when used alone and, to a greater extent, when used in combination with the α2-adrenergic receptor agonist guanabenz . 6-Aminophenanthridine (300 μM) inhibits protein folding activity of the ribosome (PFAR) by directly competing with protein substrates for the active site and decreases the yield of refolded protein without affecting the refolding rate. It prevents progressive w...
T37062	L-Leucine-7-amido-4-methylcoumarin hydrochloride
	L-Leu-AMC is a fluorogenic substrate for leucine aminopeptidase.1Upon enzymatic cleavage by leucine aminopeptidase, AMC is released and its fluorescence can be used to quantify leucine aminopeptidase activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively. 1.Izquierdo, M., Lin, D., O’Neill, S., et al.Development of a high-throughput screening assay to identify inhibitors of the major M17-leucyl aminopeptidase from Trypanosoma cruzi using rapidfire mass spectrometryS...
T83952	CoraFluor 1, amine reactive
	CoraFluor 1 (胺活性) 是一种基于铽的时间分辨福斯特共振能量转移(TR-FRET)供体，专为TR-FRET检测开发而设计，适用于目标结合和三元复合物检测等应用。该产品采用PFP酯，能与初级胺反应，适合标记生物分子如抗体、纳米体、蛋白质和肽段。CoraFluor 1 (胺活性) 具有极高的亮度，提供了在生物介质中的无与伦比的检测灵敏度和稳定性，超过其他市面上可获得的TR-FRET供体。它与常见的受体染料如FAM、TMR和Cyanine 5, SE兼容，能够无缝集成于高通量筛选应用中。
T37721	Dihydronovobiocin
	Dihydronovobiocin is a coumarin antibiotic and derivative of novobiocin .1It is active against the bacteriaS. aureus,S. haemolyticus,D. pneumoniae,S. typhosa,K. pneumoniae, andP. multocida(MICs = 0.6, 2, 0.6, 10, 10, and 3 μg/ml, respectively).2Dihydronovobiocin inhibits DNA gyrase subunit B with an IC50value of 64.5 nM.3 1.Berger, J., and Batcho, A.D.Coumarin - glycoside antibioticsJ. Chromatogr. Lib.15101-158(1978) 2.Hoeksema, H.Dihydronovobiocin and derivatives thereof3,175,9441-9(1965) 3.Gev...
T37614	LDN-0088050
	LDN 0088050 is selectivity adipocyte fatty acid binding protein (AFABP, FABP4) inhibitor with Ki values of 0.29 and 1.3 μM for FABP4 and FABP3, respectively. LDN 0088050 binds to FABP4 with a Kd of 2.05 μM[1]. Ki: 0.29 μM (FABP4), 1.3 μM (FABP3)[1]Kd: 2.05 μM (FABP4)[1] LDN 0088050 significantly inhibits LPS-induced expression of both TNFα and IL-6 in RAW264.7 cells[1]. [1]. Zhou Y, et al. The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biolo...
T37431	ENPP1 Inhibitor C ENPP1 Inhibitor C
	ENPP1 inhibitor C is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; IC50 = 0.26 μM in a cell-free assay).1 It is selective for ENPP1 over ENPP2-7 at 10 μM. ENPP1 inhibitor C decreases ENPP1 activity in MDA-MB-231 human breast and C6 rat glioma cancer cells when used at a concentration of 10 μM. \|1. Kawaguchi, M., Han, X., Hisada, T., et al. Development of an ENPP1 fluorescence probe for inhibitor screening, cellular imaging, and prognostic assessment of malignant brea...
T36695	TAS-103
	TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research. TAS-103 is a dual inhibitor of DNA topoisomerase I/II. TAS-103 (0.1-10 μM) is active on CCRF-CEM cells, with an IC50 value of 5 nM. TAS-103 (0.1 μM) significantly increases levels of topo IIα FITC immunofluorescence in individual CCRF-CEM cells[1]. TAS-103 (0.01-1 μM) is highly cytotoxic to Lewis lung carcinoma (LLC) cells, and Liposomal TAS-103 is almost as active as free TAS-103[2]. TAS-103 inhibits the viability ...

化合物

Immuno-Oncology Screening Library

Cat.No: T36421

Cat.No: T11344

Target: DNA, cGAS

Cat.No: T21980

Target: MEK

Zinc Protoporphyrin

Cat.No: T13396

Synonym: Zinc Protoporphyrin-9,锌原卟啉,ZnPP,Zn(II)-protoporphyrin IX

Target: Apoptosis, Reactive Oxygen Species, Endogenous Metabolite

Compound V007-6018

Cat.No: T67752

Target: Others

Cat.No: T9212

Target: Others, HIV Protease

Cat.No: T4531

Target: Antibacterial

Cat.No: TP1204

Synonym: c(CRGDKGPDC)

Target: Integrin

Cat.No: T3572

Synonym: 1,3-Bis(4-aminophenyl)urea,NSC15364

Target: Apoptosis, Others, VDAC

Cat.No: T24859

Target: Aquaporin

Cat.No: T4062

Target: Sirtuin

Cat.No: T41256

Target: Aurora Kinase

NSC 601980 (analog)

Cat.No: T12258

Target: Others

Cat.No: T25542

Synonym: Isamfazona,Isamfazonum

pp60 (v-SRC) Autophosphorylation Site, Phosphorylated

Cat.No: T39185

Synonym: pp60 (v-SRC) Autophosphorylation Site, Phosphorylated

Cat.No: TP1476

Glutarylcarnitine lithium

Cat.No: T73752

Cat.No: T74626

Cat.No: T12259

Target: Others

Cat.No: T69911

6-Biotin-17-NAD+ sodium

Cat.No: T83800

Synonym: 6-Biotin-17-Nicotinamide adenine dinucleotide,β-Nicotinamide-N6-(2-(6-(6-[biotinyl]aminohexanoyl)aminohexanoyl)aminoethyl)adenine dinucleotide

Bentiromide acetate

Cat.No: T14529L

Synonym: Bentiromide acetate(37106-97-1 Free base)

Target: Others

α-Synuclein 4554W

Cat.No: T80151

Cat.No: T36743

(+)-Biotin 4-Amidobenzoic Acid (sodium salt)

Cat.No: T35411

Cat.No: T79556

Target: Autophagy

Cat.No: T69117

Cat.No: T82789

Cat.No: T78520

Target: Others

Cat.No: T35905

25-Desacetyl Rifampicin

Cat.No: T35706

Cat.No: T83131

6-Aminophenanthridine

Cat.No: T38187

L-Leucine-7-amido-4-methylcoumarin hydrochloride

Cat.No: T37062

CoraFluor 1, amine reactive

Cat.No: T83952

Dihydronovobiocin

Cat.No: T37721

Cat.No: T37614

ENPP1 Inhibitor C

Cat.No: T37431

Synonym: ENPP1 Inhibitor C

Cat.No: T36695

Cat. No.	Product Name	Target	Signaling Pathways
T17143	Toyocamycin 丰加霉素,Vengicide	Apoptosis; Others; IRE1; Antibiotic; Antifungal	Apoptosis; Cell Cycle/Checkpoint; Microbiology/Virology; Others
	Toyocamycin (Vengicide) 是放线菌类产生的腺苷类似物，为 X 盒结合蛋白 1 (XBP1) 抑制剂，抑制 IRE1α 诱导的 ATP 依赖性 XBP1 mRNA 的断裂，IC50值为 80 nM。它还诱导凋亡。
T4925	Thiamine monophosphate chloride (dihydrate) Thiamine monophosphate chloride dihydrat,胺氯化亚磷酸酯,Aneurine monophosphate chloride	Others; Endogenous Metabolite	Metabolism; Others
	Thiamine monophosphate chloride dihydrate (Aneurine monophosphate chloride) 是内源性代谢产物的一种。
T4S0051	Coptisine sulfate	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	Coptisine Sulfate 是一种从黄连中分离到的生物碱，是非竞争性的IDO 抑制剂，Ki=为 5.8 μM，IC50=6.3 μM。
T19340	Glutarylcarnitine O-glutaroyl-L-carnitine	Endogenous Metabolite	Metabolism
	Glutarylcarnitine (O-glutaroyl-L-carnitine) 是大多数串联质谱新生儿筛查计划中监测的丙二酸尿症和谷草酸尿症 I 型的诊断代谢物。
T3313	D-Luciferin Firefly luciferin,D-萤光素,D-荧光素,D-(-)-Luciferin	Others	Others
	D-Luciferin (D-(-)-Luciferin) 是一种萤光素酶的底物，能够催化生物发光昆虫产生典型的黄绿光。
T3888	Scopolin Murrayin,东莨菪甙,Scopoloside,东莨菪苷	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Scopolin (Scopoloside) 是从拟南芥根中分离出来的香豆素，可通过激活SIRT1介导的信号级联反应减轻了肝脂肪变性。
TN1583	Dihydromorin	TRP/TRPV Channel	Membrane transporter/Ion channel
	trans-Dihydromorin is an effective hypopigmenting agent in normal skin cells, hypopigmenting agents effective in melanoma system may not be effective on normal melanocytes, indicating that a non-tumor melanocyte system is more suitable for the screening o
TN5243	Vitexilactone	NADPH-oxidase; HIV Protease; Antifection	Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Vitexilactone is a HIV-1 reverse transcriptase inhibitor in virtual screening against Indonesian Herbal Database using AutoDock4 performed on HIV-1 reverse transcriptase. It has trypanocidal activity, the minimum lethal concentration against epimastigotes
TN5578	Abieta-8,11,13-triene-7,15,18-triol
	Abieta-8,11,13-triene-7alpha,15,18-triol,7alpha,8alpha,13beta,14beta-diepoxyabietan-18-oic acid, and 18-nor-abieta-8,11,13-triene-4alpha,7alpha,15-triol may have inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by the tum
T38038	(-)-Rasfonin
	(-)-Rasfonin is a fungal metabolite that has been found in T. terrophilus.1 It inhibits proliferation of mouse splenocytes induced by concanavalin A and LPS (IC50s = 0.7 and 0.5 μg/ml, respectively). References1. Fujimoto, H., Okamoto, Y., Sone, E., et al. Eleven new 2-pyrones from a fungi imperfecti, Trichurus terrophilus, found in a screening study guided by immunomodulatory activity. Chem. Pharm. Bull. (Tokyo) 53(8), 923-929 (2005).
T35761	Carviolin
	Carviolin is an anthraquinone fungal metabolite that has been found inZ. longicaudatawith immunosuppressive and antitrypanosomal activities.1,2It inhibits LPS- or concanavalin A-induced proliferation of mouse splenocytes (IC50s = 4 and 4.5 μg/ml, respectively).1Carviolin is active againstT. b. brucei(MIC = 41.66 μM).2 1.Fujimoto, H., Nakamura, E., Okuyama, E., et al.Six immunosuppressive features from an ascomycete, Zopfiella longicaudata, found in a screening study monitored by immunomodulatory...
T37690	Phenylpyropene A
	Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).1 Phenylpyropene A inhibits diacylglycerol acyltransferase (DGAT) in rat liver microsomes (IC50 = 78.7 μM). It induces mortality in 100% of M. persicae when used at a concentration of 5 ppm.3 \|1. Kwon, O.E., Rho, M.C., Song, H.Y., et al. Phenylpyropene A and B, new inhibitors of ...

天然产物

Cat.No: T17143

Synonym: 丰加霉素,Vengicide

Target: Apoptosis, Others, IRE1, Antibiotic, Antifungal

Thiamine monophosphate chloride (dihydrate)

Cat.No: T4925

Synonym: Thiamine monophosphate chloride dihydrat,胺氯化亚磷酸酯,Aneurine monophosphate chloride

Target: Others, Endogenous Metabolite

Coptisine sulfate

Cat.No: T4S0051

Target: Indoleamine 2,3-Dioxygenase (IDO)

Glutarylcarnitine

Cat.No: T19340

Synonym: O-glutaroyl-L-carnitine

Target: Endogenous Metabolite

Cat.No: T3313

Synonym: Firefly luciferin,D-萤光素,D-荧光素,D-(-)-Luciferin

Target: Others

Cat.No: T3888

Synonym: Murrayin,东莨菪甙,Scopoloside,东莨菪苷

Target: Sirtuin

Cat.No: TN1583

Target: TRP/TRPV Channel

Cat.No: TN5243

Target: NADPH-oxidase, HIV Protease, Antifection

Abieta-8,11,13-triene-7,15,18-triol

Cat.No: TN5578

Cat.No: T38038

Cat.No: T35761

Phenylpyropene A

Cat.No: T37690

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