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42

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9303	MRTX1133	Ras	GPCR/G Protein; MAPK
	MRTX1133 是一种 KRAS G12D 抑制剂 (KD=0.2 pM)，具有强效性、选择性和非共价性。MRTX1133 对 KRAS G12D 突变的肿瘤具有抑制活性，而对 KRAS 野生型肿瘤无抑制活性。
T0411	Gluconate Calcium Calcium D-gluconate,Gluconic acid hemicalcium salt,Calcium gluconate,葡萄糖酸钙	Others	Others
	Gluconate Calcium (Gluconic acid hemicalcium salt) 是矿物质补充剂, 由葡糖酸和石灰或碳酸钙中和制成。
T10674	Potassium Channel Activator 1 钾离子通道激活剂1,ZINC34634569	Potassium Channel	Membrane transporter/Ion channel
	Potassium Channel Activator 1 可用于治疗多巴胺能系统被破坏的疾病或病症的研究，例如情绪障碍 ADHD、精神分裂症和其他精神病状态。
T20702	Ormetoprim Ro5-9754,奥美普林,Ro 5-9754,Ro-5-9754	Antibiotic	Microbiology/Virology
	Ormetoprim (Ro 5-9754) 是一种兽用抗菌剂，通常用于水产养殖和家禽行业，可以预防疾病在淡水水产养殖中的传播，促进家畜的生长。
T0285	Isoxicam 伊索昔康,Isoxicamum,Isoxicamo,Maxicam	COX	Immunology/Inflammation; Neuroscience
	Isoxicam (Isoxicamum) 是可口服的非甾体抗炎剂，可通过抑制环氧合酶 1 和 2 来阻断前列腺素的合成，可用于关节炎的研究。
T3285	Eslicarbazepine Acetate Zebinix,Aptiom,BIA 2-093,Exalief,艾司利卡西平醋酸酯,Stedesa	Beta-Secretase; Sodium Channel	Membrane transporter/Ion channel; Neuroscience
	Eslicarbazepine Acetate (Zebinix) 是一种抗癫痫药物。Eslicarbazepine acetate 也是 β-内分泌酶(β-Secretase)和电压门控钠离子通道的双抑制剂。
T1175	Bromopride Bromoprida,溴灭吐灵,Valopride,Artomey	Dopamine Receptor	GPCR/G Protein; Neuroscience
	Bromopride (Valopride) 是一种多巴胺拮抗剂，常用作止吐药，有促动力特性。
T1442	Pizotifen Pizotyline,BC-105,苯噻啶	5-HT Receptor	GPCR/G Protein; Neuroscience
	Pizotifen (Pizotyline) 是5-HT2受体的有效拮抗剂，并对5-HT1C 有高亲和力。它是一种强血清素和色胺拮抗剂，具有较弱的抗胆碱能、抗组胺和抗激肽作用，还具有镇静和刺激食欲的特性。
T16472	Pericyazine Propericiazine,氰噻嗪,RP 8909	Dopamine Receptor	GPCR/G Protein; Neuroscience
	Pericyazine (Propericiazine) 是第一代抗精神病药物，是一种选择性的 D2 多巴胺受体 (D2-dopamine receptor) 拮抗剂，具有肾上腺溶解、抗胆碱能和锥体外系作用，被用作短期管理严重焦虑状态和精神病的辅助药物。
T2189	Sodium orthovanadate Sodium vanadate,钒酸钠,Trisodium vanadate,Sodium pervanadate	ATPase; Phosphatase	Membrane transporter/Ion channel; Metabolism
	Sodium orthovanadate 是一种蛋白酪氨酸磷酸酶，碱性磷酸酶和一些ATP 酶的抑制剂，有可能充当磷酸盐类似物。它具有胰岛素样作用、对心室肌的正性肌力作用和其他代谢作用。
T2585	Bedaquiline R207910,TMC207,贝达喹啉	Antibacterial; Antibiotic	Microbiology/Virology
	Bedaquiline (R207910) 是一种二芳基喹啉药物，能同时靶向 c-亚基和 ε-亚基，抑制结核分枝杆菌 (Mtb) F1FO-ATP 合酶。它具有解偶联活性和有用于耐多药结核病的潜力。
T0811	Amisulpride DAN 2163,氨磺必利,阿米舒必利	Dopamine Receptor; 5-HT Receptor	GPCR/G Protein; Neuroscience
	Amisulpride (DAN 2163) 是多巴胺D2/D3受体拮抗剂，对于人多巴胺D2和D3的Ki 分别为 2.8 和 3.2 nM。
T1519L	Rimonabant SR141716,利莫那班	Cannabinoid Receptor; Antibacterial; Acyltransferase	GPCR/G Protein; Metabolism; Microbiology/Virology
	Rimonabant (SR141716) 是一种选择性的、能透过血脑屏障的中心大麻素受体 1 拮抗剂， Ki 值为 1.8 nM。它也能够抑制分枝杆菌膜蛋白 3。
T0454	Florfenicol 氟苯尼考,Nuflor,Aquafen	Others	Others
	Florfenicol (Aquafen) 是甲砜霉素的氟化合成类似物。在美国，氟苯尼考目前用于治疗与溶血性曼氏杆菌(巴氏杆菌)、多杀性巴氏杆菌和嗜血嗜血杆菌相关的牛呼吸道疾病(BRD)，以治疗与坏死梭杆菌和黑色素拟杆菌相关的牛趾间痰。
T1551	Tegaserod maleate HTF-919,马来酸替加色罗,SDZ-HTF-919	5-HT Receptor	GPCR/G Protein; Neuroscience
	Tegaserod maleate (SDZ-HTF-919) 是选择性5-HT4受体的部分激动剂和5-HT2B 受体的拮抗剂，用于治疗肠易激综合征和便秘。
T0454L	Florfenicol SCH-25298,氟苯尼考,(-)-Florfenicol	Antibacterial; Antibiotic	Microbiology/Virology
	Florfenicol (SCH-25298) 是一种常见得兽用抗生素，能用于研究牛呼吸疾病，在水产养殖业中可以用来控制鲶鱼肠道败血病，也可诱导鸡蛋早期胚胎死亡，LC50 值为 1.07 μg/g。
T0910	Terpin hydrate Terpin Monohydrate,cis-Terpin hydrate,萜品(水合结晶)	Others	Others
	Terpin hydrate 是一种祛痰药，可除去急慢性支气管炎病人的黏液。
T36816	S-trityl-L-Cysteine STLC	Kinesin	Cytoskeletal Signaling
	S-Trityl-L-cysteine 是别构驱动蛋白Eg5的选择性抑制剂。rityl-L-cysteine 抑制基础 ATPase 活性的IC50为 1 μM，抑制微管激活的 ATPase 活性的IC50为 140 nM。S-Trityl-L-cysteine 显示出抗肿瘤活性。
T34903	TO-PRO3 iodide TOPRO3 iodide,TO-PRO3 iodide salt
	TO-PRO3 iodide is a nucleic acid stain that can stain the nucleus of cells in different states, including living, early apoptotic, and necrotic cells.
T11913	LY88074 Methyl ether	Others	Others
	LY88074 Methyl ether is effective in inhibiting conditions associated with estrogen deprivation syndrome, such as osteoporosis and hyperlipidemia, which occur due to various estrogen-deficient states.
T70854	Protokylol hydrochloride
	Protokylol hydrochloride is the salt form of Protokylol (free base) (Asmetil, Caytine, Palison, Ventaire), a β-adrenergic receptor agonist used as a bronchodilator in Europe and the United States. It is methylenedioxyphenyl-isoproterenol.
T31819	Fluometuron NCI C08695,Ciba 2059,C 2059,NCI-C08695,NCIC08695
	Fluometuron is an herbicide. In the United States it was approved for use on cotton and sugarcane crops in 1974, but since 1986 is only approved for use on cotton.
T13263	COX/5-LO-IN-1 Atreleuton analog	COX	Immunology/Inflammation; Neuroscience
	COX/5-LO-IN-1 is a cyclooxygenase and 5-lipoxygenase (5-LO) inhibitor, and used for inflammatory and allergic disease states.
T27521	GX-936 GX 936,PF 05196233,PF05196233,GX936,PF-05196233
	GX-936, a Nav1.7 inhibitor, inhibits Nav1.7 through a voltage-sensor trapping mechanism, likely by stabilizing inactivated states of the channel.
T37130	MRTX1133 formic
	MRTX1133 is a highly selective, first-in-class inhibitor of KRAS G12D. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells[1][2]. MRTX1133 demonstrates dose-dependent inhibition of the KRAS pathway tumor regression in G12D mutant tumor models[2]. [1]. Xiaolun Wang, et al.Kras g12d inhibitors.WO2021041671A1.[2]. KRAS G12D Inhibitor: MRTX1133. [(accessed on 22 April 2021)];2021 Available onli...
T70613	SLP120701 HCl
	SLP120701 is a potent and selective sphingosine kinase 2 inhibitor. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis, and sickle cell disease.
T0338	Minaprine Cantor,Minaprine dihydrochloride,米那卜林,米那卜林二盐酸盐,Minaprina,Minaprinum	MAO; Dopamine Receptor; 5-HT Receptor; AChR; AChE; Monoamine Oxidase	GPCR/G Protein; Metabolism; Neuroscience
	Minaprine 是一种单胺氧化酶 MAO-A 可逆性抑制剂，对乙酰胆碱酯酶有微弱抑制，是一种抗抑郁类化合物。
T4497L	Amifampridine phosphate BRN0110232,3,6-DAP,SC10,BRN 0110232,BRN-0110232,NSC 521760
	Amifampridine is mainly used to treat many rare muscle diseases. In the United States, aminopyridine is being studied for the treatment of Lambert-Eaton myasmus syndrome (LEMS). Amifampridine is also used to treat many congenital myasthenia syndromes, par
T70614	SLR080811 HCl
	SLR080811 is a SphK inhibitor. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis, and sickle cell disease.
T33287	Mephentermine Sulfate sulfuric acid,MLS002153976,N,2-dimethyl-1-phenylpropan-2-amine,AC1NWAW7,Mephentermine sodium
	Mephentermine sulfate is a cardiac stimulant, before as a stimulant in psychiatry, has been used as a treatment for low blood pressure. Mephentermine sulfate is a sympathomimetic agent with specificity for alpha-1 adrenergic receptors. It is used to maint
T75970	Melanin Concentrating Hormone, salmon TFA
	Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA) 是在硬骨鱼的垂体中发现的 19 个氨基酸组成的神经肽，它调节食物摄入，能量平衡，睡眠状态和心血管系统。Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA) 是 SLC-1/GPR24和 MCHR2的配体。
T70900	VT-ME6
	VT-ME6 is a potent and selective sphingosine kinase 2 inhibitor. VT-ME6, contained a quaternary ammonium group as a warhead and established that a positively charged moiety is necessary for engaging key amino acid residues in the enzyme binding pocket.13,14 This compound is moderately potent (Ki = 8 lM) and displays three-fold selectivity for SphK2 over SphK1. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK...
T69492	Ozarelix
	Ozarelix is a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells modulating expression and activity of death receptors. Mechanistically, LHRH antagonists exert rapid inhibition of luteinizing hormone and follicle stimulating hormone with an accompanying rapid decrease in sex hormones and would therefore be expected to be effective in a variety of hormonally dependent disease states including ovarian cancer, prostate cancer,...
T22572	Angiotensin 1/2 (1-7) amide	Others	Others
	Angiotensin I/II (1-7) amide is a peptide analog to angiotensin II that is used as a vasopressor in the treatment of certain types of shock and circulatory collapse. Angiotensin I/II amide is an amide derivative of angiotensin II that is a powerful vasoco
T70128	Olmutinib hydrochloride
	Olmutinib is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor, used in the treatment of T790M mutation positive non-small cell lung cancer. Olmutinib covalently binds a cysteine residue near the kinase domain of mutant EGFRs to prevent phosphorylation of the receptor. EGFRs are frequently over-expressed in lung cancer and contribute to activation of the phosphoinositide 3-kinase and mitogen-activated protein kinase pathways which both p...
T31194	Dalapon Basfapon B,Dowpon M,Dawpon-Rae
	Dalapon is a selective herbicide used to control perennial grasses. The major use of dalapon is on food crops including sugarcane and sugar beets. Its use is no longer authorized in France. The National Institute for Occupational Safety and Health in the
T82805	Butaprost free acid
	(R)-Butaprost (free acid) 是PGE2的一个结构类似物，特异性地对EP2受体亚型有选择性。该化合物用于药理学研究，以确定不同人类及动物组织和细胞中EP受体的分布。去除甲酯基团并恢复C-1自然羧酸后，增强了(R)-butaprost与前列腺素受体的结合亲和力，通常情况下，游离酸形式的亲和力是相应酯形式的10到100倍。尽管(R)-butaprost作为C-16的较低活性差向异构体，其药理作用未经充分研究，但在1986年Gardiner的论文中提到的TR 4979即布他前列素，结构中的差向异构体错误表达为16(R)，实际为16(S)，该错误直至1990年代后期才被美国和日本的研究纠正。
T35961	Prostaglandin Bx
	PGBx is a mixture of oligomers of PGB1 with a molecular weight of 1,000-1,500. It has antioxidant and free radical trapping activity that was first studied in isolated mitochondria.1 PGBx has anti-inflammatory and cytoprotective activity which may be attributed to inhibition of the 14 kDa sPLA2.2,3 At a dose of 1 mg/kg, PGBx significantly reduces the incidence of ulcers in rats.2References1. Polis, B.D., Polis, E., and Kwong, S. Protection and reactivation of oxidative phosphorylation in mitocho...
T35538	HPI-1 (hydrate) HPI-1 hydrate
	HPI-1 (hydrate) is a Hedgehog (Hh) pathway inhibitor that suppresses signaling through Sonic Hh (IC50= 1.5 μM) without significantly affecting Wnt signaling (IC50≥ 30 μM).1HPI-1 suppresses Hh activation induced by loss of Suppressor of Fused or by Gli overexpression, suggesting action at posttranslational modification of Gli protein or at the interaction of Gli with a co-factor.1HPI-1 (hydrate) also inhibits signaling through the oncogenic Smoothened (Smo) mutant SmoM2 in neuron precursors, prev...
T38161	STING Agonist C11 STING Agonist C11
	STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.1 It induces secretion of type I IFN from THF and MM6 cells when used at a concentration of 50 μM. STING agonist C11 induces phosphorylation of IFN regulatory factor 3 (IRF3) and increases expression of IFIT1 and viperin, but not IL-1β, IL-6, or IL-8 in THF cells in a STING-dependent manner. It reduces viral titers of chikungunya, Venezuelan equine encephalitis, o'nyong-nyong, Mayaro, and Ross River viruses gro...
T35904	O-11
	O-11 is an analog of the fully saturated, 14-carbon fatty acid myristic acid, in which the methylene group at position 11 is replaced with oxygen. It is highly effective and selective at killingTrypanosoma brucei, the protozoan parasite responsible for African sleeping sickness, exhibiting an LD50of less than 1 μM in a cell culture assay.1,2The toxic effects of O-11 appear to be caused by its ability to inhibit the incorporation of a single myristate into the GPI anchor of the variant surface gl...
T35568	BODIPY-aminoacetaldehyde diethyl acetal
	BODIPY-aminoacetaldehyde diethyl acetal (BAAA-DA) is a stable precursor to BODIPY-aminoacetaldehyde, a cell-permeable fluorescent substrate for aldehyde dehydrogenase (ALDH).1,2BODIPY-aminoacetaldehyde diethyl acetal is converted under acidic conditions to BODIPY-aminoacetaldehyde (BAAA).2BAAA is cell-permeant and is converted intracellularly by ALDH to BODIPY aminoacetate (BAA), which is retained by cells and can be used to identify cells with high ALDH activity.1BAA is a substrate for the effl...

化合物

Cat.No: T9303

Target: Ras

Gluconate Calcium

Cat.No: T0411

Synonym: Calcium D-gluconate,Gluconic acid hemicalcium salt,Calcium gluconate,葡萄糖酸钙

Target: Others

Potassium Channel Activator 1

Cat.No: T10674

Synonym: 钾离子通道激活剂1,ZINC34634569

Target: Potassium Channel

Cat.No: T20702

Synonym: Ro5-9754,奥美普林,Ro 5-9754,Ro-5-9754

Target: Antibiotic

Cat.No: T0285

Synonym: 伊索昔康,Isoxicamum,Isoxicamo,Maxicam

Target: COX

Eslicarbazepine Acetate

Cat.No: T3285

Synonym: Zebinix,Aptiom,BIA 2-093,Exalief,艾司利卡西平醋酸酯,Stedesa

Target: Beta-Secretase, Sodium Channel

Cat.No: T1175

Synonym: Bromoprida,溴灭吐灵,Valopride,Artomey

Target: Dopamine Receptor

Cat.No: T1442

Synonym: Pizotyline,BC-105,苯噻啶

Target: 5-HT Receptor

Cat.No: T16472

Synonym: Propericiazine,氰噻嗪,RP 8909

Target: Dopamine Receptor

Sodium orthovanadate

Cat.No: T2189

Synonym: Sodium vanadate,钒酸钠,Trisodium vanadate,Sodium pervanadate

Target: ATPase, Phosphatase

Cat.No: T2585

Synonym: R207910,TMC207,贝达喹啉

Target: Antibacterial, Antibiotic

Cat.No: T0811

Synonym: DAN 2163,氨磺必利,阿米舒必利

Target: Dopamine Receptor, 5-HT Receptor

Cat.No: T1519L

Synonym: SR141716,利莫那班

Target: Cannabinoid Receptor, Antibacterial, Acyltransferase

Cat.No: T0454

Synonym: 氟苯尼考,Nuflor,Aquafen

Target: Others

Tegaserod maleate

Cat.No: T1551

Synonym: HTF-919,马来酸替加色罗,SDZ-HTF-919

Target: 5-HT Receptor

Cat.No: T0454L

Synonym: SCH-25298,氟苯尼考,(-)-Florfenicol

Target: Antibacterial, Antibiotic

Cat.No: T0910

Synonym: Terpin Monohydrate,cis-Terpin hydrate,萜品(水合结晶)

Target: Others

S-trityl-L-Cysteine

Cat.No: T36816

Synonym: STLC

Target: Kinesin

Cat.No: T34903

Synonym: TOPRO3 iodide,TO-PRO3 iodide salt

LY88074 Methyl ether

Cat.No: T11913

Target: Others

Protokylol hydrochloride

Cat.No: T70854

Cat.No: T31819

Synonym: NCI C08695,Ciba 2059,C 2059,NCI-C08695,NCIC08695

Cat.No: T13263

Synonym: Atreleuton analog

Target: COX

Cat.No: T27521

Synonym: GX 936,PF 05196233,PF05196233,GX936,PF-05196233

MRTX1133 formic

Cat.No: T37130

Cat.No: T70613

Cat.No: T0338

Synonym: Cantor,Minaprine dihydrochloride,米那卜林,米那卜林二盐酸盐,Minaprina,Minaprinum

Target: MAO, Dopamine Receptor, 5-HT Receptor, AChR, AChE, Monoamine Oxidase

Amifampridine phosphate

Cat.No: T4497L

Synonym: BRN0110232,3,6-DAP,SC10,BRN 0110232,BRN-0110232,NSC 521760

Cat.No: T70614

Mephentermine Sulfate

Cat.No: T33287

Synonym: sulfuric acid,MLS002153976,N,2-dimethyl-1-phenylpropan-2-amine,AC1NWAW7,Mephentermine sodium

Melanin Concentrating Hormone, salmon TFA

Cat.No: T75970

Cat.No: T70900

Cat.No: T69492

Angiotensin 1/2 (1-7) amide

Cat.No: T22572

Target: Others

Olmutinib hydrochloride

Cat.No: T70128

Cat.No: T31194

Synonym: Basfapon B,Dowpon M,Dawpon-Rae

Butaprost free acid

Cat.No: T82805

Prostaglandin Bx

Cat.No: T35961

HPI-1 (hydrate)

Cat.No: T35538

Synonym: HPI-1 hydrate

STING Agonist C11

Cat.No: T38161

Synonym: STING Agonist C11

Cat.No: T35904

BODIPY-aminoacetaldehyde diethyl acetal

Cat.No: T35568

Cat. No.	Product Name	Target	Signaling Pathways
T21532	Anisodamine 6-Hydroxyhyoscyamine,6-beta-Hydroxyhyoscyamine	AChR	Neuroscience
	Anisodamine (6-beta-Hydroxyhyoscyamine) 是毒蕈碱和烟碱胆碱受体的拮抗剂，对毒蕈碱受体的亲和力与东莨菪碱和阿托品相似。 Anisodamine 改善休克状态下的微循环，可用于有机磷中毒的研究。
T4S0797	Berberine 小檗碱,Berberin,Umbellatine,黄连素	Reactive Oxygen Species; Topoisomerase; Endogenous Metabolite; Antibacterial; Antibiotic; Autophagy	Autophagy; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB
	Berberine (Umbellatine) 是从中草药黄连中分离出来的一种生物碱抗生素。它诱导活性氧生成并抑制 DNA 拓扑异构酶，具有抗肿瘤特性。

天然产物

Cat.No: T21532

Synonym: 6-Hydroxyhyoscyamine,6-beta-Hydroxyhyoscyamine

Target: AChR

Cat.No: T4S0797

Synonym: 小檗碱,Berberin,Umbellatine,黄连素

Target: Reactive Oxygen Species, Topoisomerase, Endogenous Metabolite, Antibacterial, Antibiotic, Autophagy

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