搜索结果

Search Results for " sensitization "

TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

抑制剂 & 化合物

天然产物

如果没找到您满意的产品或者您对产品有其他要求，可以联系我们专业顾问为您提供针对性的合理建议。 QQ咨询网站留言咨询

Cat. No.	Product Name	Target	Signaling Pathways
T21955	GQ-16	PPAR	DNA Damage/DNA Repair; Metabolism
	GQ-16 是 PPARγ 的部分激动剂，Ki 为 160 nM。 GQ-16 可减少脂肪生成作用并促进胰岛素敏化而不会增加体重。
T21935L	AMN082 free base AMN082	GluR	Neuroscience
	AMN082 free base 是 mGluR7选择性激动剂，口服有活性，能够透过血脑屏障，可通过跨膜区的变构位点直接激活受体信号。在表达 mGluR7 的转染哺乳动物细胞上，它能够有效抑制 cAMP 积累并刺激 GTPγS 结合。它能够选择性针对 mGluR 的其他亚型及选择性离子型谷氨酸受体。具有抗抑郁活性。
T21935	AMN082 AMN 082 dihydrochloride	GluR	Neuroscience
	AMN082 (AMN 082 dihydrochloride) 是可口服，可透过血脑屏障的选择性mGluR7激动剂，通过跨膜区的变构位点直接激活受体信号，具有抗抑郁作用。
T14384	AZD8797 KAN-0440567,KAND567	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	AZD8797 (KAND567) 是一种可口服且具有选择性和有效性的人 CX3CR1 变构拮抗剂，对 CX3CR1 和 CXCR2 具有抑制作用，对SARS-CoV-2诱导的神经元损伤有潜在的保护作用，可防止癫痫发作后偏头痛模型大鼠痛觉过敏和小胶质细胞活化的恶化。
TP2111L	TAT-GluA2 3Y acetate(1404188-93-7 free base)	GluR	Neuroscience
	TAT-GluA2 3Y acetate 是AMPA 受体内吞作用的抑制剂。在d-安非他明诱导期全身给药Tat-GluA2(3Y)阻断大鼠行为致敏维持，减弱神经化学致敏维持。
T65086	Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride	Apoptosis; Phosphatase	Apoptosis; Metabolism
	Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride 可能会引起致敏作用。 Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride 促进 HepG2 （IC50= 62μM）和SK-Hep1（IC50= 151μM）细胞凋亡且对蛋白磷酸酶2A具有抑制作用。
T6970	RK33 RK-33,RK 33	COX	Immunology/Inflammation; Neuroscience
	RK33 (RK 33) 是 DDX3（一种 RNA 解旋酶）的一流小分子抑制剂，可导致 G1 细胞周期停滞，诱导细胞凋亡，并促进 DDX3 过表达细胞的辐射增敏。
T83212	AC-099 hydrochloride	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	AC-099 hydrochloride 是一种神经肽 FF2 受体 NPFF2R 的选择性全激动剂（EC50=1189 nM）和神经肽 FF1 受体 NPFF1R的部分激动剂功能（EC50=2370 nM），可逆转阿片类化合物诱导的痛觉过敏，可用于研究神经系统疾病。
T72947	JBSNF-000028 JBSNF-000028 free base	Others	Others
	JBSNF-000028 是一种具有口服活性和有效性的烟酰胺 N-甲基转移酶 (NNMT) 抑制剂，对人 NNMT (hNNMT)、猴 NNMT (mkNNMT) 和小鼠 NNMT (mNNMT) 具有抑制作用， IC50 分别为 0.033 μM、0.19 μM 和 0.21 μM。JBSNF-000028 可驱动胰岛素敏化、葡萄糖调节和体重减，可用于研究代谢紊乱。
T11209	EOAI3402143	DUB	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
	EOAI3402143 是一种去泛素化酶抑制剂，以剂量依赖性抑制 Usp9x/Usp24和 Usp5，增加肿瘤细胞凋亡。
T4431	Olodanrigan PD-126055,EMA401	RAAS	Endocrinology/Hormones
	Olodanrigan (EMA401) 是具有口服活性、高选择性及外周受限的血管紧张素 Ⅱ 类型 2 受体(AT2R)拮抗剂。它的缓解疼痛的机制可能是：抑制增强的 AngII/AT2R 诱导的 p38 和 p42/p44 MAPK 激活，进而阻碍 DRG 神经元的过度兴奋性及 DRG 神经元的萌发。它可用于研究神经性疼痛。
T28268	ORM-3819
	ORM-3819 is a potent and selective PDE III inhibitor. ORM-3819 promotes cardiac contractility through Ca(2+) sensitization.
T68398	MI-223
	MI-223 is an inhibitor of Mcl-1-stimulated homologous recombination (HR) DNA repair, which leads to sensitization of cancer cells to hydroxyurea- or olaparib-induced DNA replication stress.
T37963	Methylchloroisothiazolinone/Methylisothiazolinone Mixture
	Methylchloroisothiazolinone/methylisothiazolinone mixture (MCIT/MIT) is a mixture of isothiazolinone-derived biocides.1,2It is effective against Gram-positive and Gram-negative bacteria with MIC values of 0.0002, 0.0002, 0.00005, and 0.00005% (w/w) forS. aureus,P. aeruginosa,A. niger, andC. albicans, respectively.2MCIT/MIT can elicit contact sensitization.3Formulations containing MCIT/MIT have been used for controlling microbial growth in industrial and household products. 1.Frenzel, E., Schmidt...
T68870	SU-11752
	SU-11752 is a potent and selective DNA-PK inhibitor. Inhibition kinetics and a direct assay for ATP binding showed that SU11752 inhibited DNA-PK by competing with ATP. SU11752 inhibited DNA double-strand break repair in cells and gave rise to a five-fold sensitization to ionizing radiation. At concentrations of SU11752 that inhibited DNA repair, cell cycle progression was still normal and ATM kinase activity was not inhibited.
T71223	SR-33805
	SR-33805 is a calcium channel antagonist potentially for the treatment of atherosclerosis and heart failure. SR-33805 restored the MI-altered cell shortening without affecting the Ca(2+) transient amplitude, suggesting an increase of myofilament Ca(2+) sensitivity in MI myocytes. A SR33805-induced sensitization of myofilament activation was found to be associated with a slight increase in myosin light chain-2 phosphorylation and a more significant decrease on troponin I (TnI) phosphorylation. D...
T68663	GPI-15427
	GPI-15427 is a potent PARP-1 inhibitor capable of crossing the blood-brain barrier, which can significantly increased the antitumor activity of the methylating agent TMZ against malignant melanoma, glioblastoma multiforme, or lymphoma growing at the CNS site. GPI-15427 acts as a potent inhibitor of the enzyme, being capable of inhibiting the activity of purified PARP-1 at nanomolar concentrations. GPI-15427 induced significant sensitization to radiotherapy, representing a promising new treatment...
T35675	SW203668 (trifluoroacetate salt)
	SW203668 is an irreversible inhibitor of stearoyl-CoA desaturase (IC50 = 54 nM). It is selectively cytotoxic to H2122, H460, HCC44, and HCC95 cell lines that express cytochrome P450 (CYP) isoform CYP4F11 over eight other cancer cell lines that lack CYP4F11 in vitro (IC50s = 22-116 and >10,000 nM, respectively) and ectopic expression of CYP4F11 in SW203668-insensitive H1155 cells results in sensitization to SW203668. In vivo, SW203668 reduces tumor growth rate without reducing sebocyte production...
T69976	WS-691
	WS-691 is a highly Potent and Orally Active ABCB1 Modulator. WS-691 significantly increased sensitization of ABCB1-overexpressed SW620/Ad300 cells to paclitaxel (PTX) (IC50 = 22.02 nM). WS-691 significantly increased the intracellular concentration of PTX and [3H]-PTX while decreasing the efflux of [3H]- PTX in SW620/Ad300 cells by inhibiting the efflux function of ABCB1. WS-691 could stabilize ABCB1 by directly binding to ABCB1 WS-691 increased the sensitivity of SW620/Ad300 cells to PTX in vi...
T11682	Isofistularin-3	Others	Others
	Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM.
T83728	Tat-AKAP79 (326-336) TFA Tat-A-kinase Anchor Protein 79 (326-336)
	Tat-AKAP79 (326-336) 是一种肽，由HIV-1 Tat蛋白质转导域与对应于A-kinase anchor protein 79 (AKAP79) 326至336残基的11个氨基酸肽链相连组成。在200 µM浓度下，能抑制蛋白激酶A (PKA) 或PKC激活诱导的瞬时受体电位钒通道1 (TRPV1) 在分离的大鼠背根神经节 (DRG) 神经元中的敏感化。在体内，Tat-AKAP79 (326-336) 抑制小鼠由甲醛或phorbol 12-myristate 13-acetate (PMA014) 引发的伤害性行为。它还延长了小鼠对辐射热刺激爪子撤回的潜伏期，并在卡拉胶诱导的炎症性疼痛小鼠模型中增加了爪子撤回的机械阈力。
T36199	AZD 1152 (hydrochloride)
	AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of p...

* 搜索：		* 机关/企业：
* 邮箱：		* 电话：
备注：
验证码：

Cat. No.	Product Name	Target	Signaling Pathways
TN4585	Moronic acid	HIV Protease; Antifection; HSV	Microbiology/Virology; Proteases/Proteasome
	Moronic acid shows oral therapeutic efficacy in HSV-infected mice and possessed novel anti-HSV activity. It also shows significant anti-HIV activity (EC(50) 186) and was modified to develop more potent anti-AIDS agents. Moronic acid is a new structural lead for anti-EBV drug development, can substantially reduce the numbers of EBV particles produced by the cells after lytic induction. Morolic and moronic acids have shown sustained antidiabetic and antihyperglycemic action possibly mediated by an...
TN4584	Morolic acid	IL Receptor; COX; HIV Protease	Immunology/Inflammation; Microbiology/Virology; Neuroscience; Proteases/Proteasome
	Morolic acid and moronic acid have shown sustained antidiabetic and antihyperglycemic action possibly mediated by an insulin sensitization with consequent changes of glucose, cholesterol and triglycerides, in part mediated by inhibition of 11β-HSD 1. Moro

搜索结果

抑制剂 & 化合物

天然产物

提交您的定制咨询

化合物

天然产物