74
17
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T13112 |
Tat-NR2B9c
Tat-NR2Bct,NA-1 |
NO Synthase; iGluR | Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience |
Tat-NR2B9c (NA-1) 是一种突触后密度-95(PSD-95)抑制剂,具有神经保护和抗癫痫作用。Tat-NR2B9c 可抑制PSD-95d2、 PSD-95d1 和 PSD-95,可阻止NMDA诱导的神经元NADPH氧化酶的激活,从而阻断超氧化物的产生,可减少中风后急性期的缺血性损伤。 | |||
T25245 | CHM-1-P-Na | ||
CHM-1-P-Na is used as a hydrophilic prodrug of CHM-1. | |||
T8555 |
Neuraminidase-IN-1
Novel NA Inhibitor,Compound Y-1 |
Others; Influenza Virus | Microbiology/Virology; Others |
Neuraminidase-IN-1 (Compound Y-1) 是一种神经氨酸酶抑制剂,其IC50值为 0.21 μM,具有抗H1N1流感病毒的活性。 | |||
T12181 |
NaV1.7 inhibitor-1
|
Sodium Channel | Membrane transporter/Ion channel |
NaV1.7 inhibitor-1 是有效的、选择性的电压门控钠通道 (Nav) 1.7 抑制剂,对于hNaV1.7的IC50为 0.6 nM,其选择性是 hNaV1.5 的 80 倍。 | |||
T3935 |
1-Naphthyl PP1
4 -氨基- 1 -叔丁基- 3 -(1' -萘基)吡唑并[3,4 - D]嘧啶,1-NA-PP 1 |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
1-Naphthyl PP1 (1-NA-PP 1) 是选择性的src 家族激酶抑制剂,能够抑制 v-Src (IC50:1.0 μM)、c-Fyn (IC50:0.6 μM)、c-Abl (IC50:0.6 μM)、CDK2 (IC50:18 μM) 和 CAMK II (IC50:22 μM)。 | |||
T7371 |
1-Naphthyl PP1 hydrochloride
1-叔丁基-3-(1-萘基)-1H-吡唑并[3,4-D]嘧啶-4-胺盐酸盐,1-NA-PP 1 hydrochloride |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) 是选择性的 src 家族激酶抑制剂,能够抑制 v-Src (IC50:1.0 μM)、c-Fyn (IC50:0.6 μM)、c-Abl (IC50:0.6 μM)、CDK2 (IC50:18 μM)、CAMK II (IC50:22 μM)。 | |||
T13112L1 |
Tat-NR2B9c acetate
Tat-NR2B9c acetate (500992-11-0 Free base),NA-1 acetate |
Others | Others |
Tat-NR2B9c acetate (NA-1 acetate) 是一种突触后密度 95 (PSD-95) 抑制剂,对 PSD-95d2 (PSD-95 PDZ domain 2) 和 PSD-95d1 的 EC50 值分别为 6.7 nM 和 670 nM。它破坏 PSD-95/NMDAR 相互作用,抑制 NR2A 和 NR2B 与 PSD-95 的结合,IC50 值分别为 0.5 μM 和 8 μM。它还抑制神经元一氧化氮合酶 (nNOS)/PSD-95 相互作用,并具有神经保护功效。 | |||
T12931 |
SLC13A5-IN-1
|
Stearoyl-CoA Desaturase (SCD) | Metabolism |
SLC13A5-IN-1 是柠檬酸钠协同转运蛋白 (SLC13A5)选择性抑制剂,在 HepG2 细胞中阻断 14C-柠檬酸盐摄取的 IC50 : 0.022 μM。 | |||
T3459 |
VK3-OCH3
2-[(2-Methoxy)ethylthio]-3-methyl-1,4-na |
Others | Others |
VK3-OCH3 (2-[(2-Methoxy)ethylthio]-3-methyl-1,4-na) 是一种通过血红素加氧酶(HO-1) 相关机制的选择性抗肿瘤剂;维生素 K3 类似物。 | |||
T8579 |
Nav1.8-IN-1
5-(4-Chlorophenyl)-N-[[2-(2,2,2-trifluoroethoxy)pyridin-3-yl]methyl]pyridine-3-carboxamide,CHEMBL1270208 |
Sodium Channel | Membrane transporter/Ion channel |
Nav1.8-IN-1 (CHEMBL1270208) 是一种有效的 Na(v)1.8 钠通道抑制剂,可用于研究精神性疼痛及炎症性疼痛。 | |||
T0386L |
Ropivacaine
LEA-103 HCl,罗哌卡因 |
Potassium Channel; Sodium Channel | Membrane transporter/Ion channel |
Ropivacaine (LEA-103 HCl) 是有效的钠通道阻断剂,通过可逆地抑制钠离子内流从而引起神经纤维脉冲传导阻滞。Ropivacaine 也是一种 K2P(双孔钾通道)TREK-1的抑制剂,在 COS-7 细胞膜上的 IC50值为 402.7 μM。Ropivacaine 可以用于神经性疼痛的缓解的相关研究。 | |||
T0386 |
Ropivacaine hydrochloride
盐酸罗哌卡因,Ropivacaine monohydrochloride |
Potassium Channel; Sodium Channel | Membrane transporter/Ion channel |
Ropivacaine hydrochloride (Ropivacaine monohydrochloride) 是钠通道阻断剂,通过可逆地抑制钠离子内流从而引起神经纤维脉冲传导阻滞。Ropivacaine hydrochloride 也是 K2P(双孔钾通道)TREK-1的抑制剂。在动物实验模型中,Ropivacaine hydrochloride 可用于神经性疼痛的缓解。 | |||
T3470 |
Cis-ACBD
cis-1-aminocyclobutane-1,3-dicarboxylic acid,氨基二羧酸 |
Amino Acids and Derivatives | Metabolism |
Cis-ACBD (cis-1-aminocyclobutane-1,3-dicarboxylic acid) 是一种有效的选择性 N-甲基-D-天冬氨酸受体激动剂。 | |||
T13112L |
Tat-NR2B9c TFA
NA-1 (TFA) |
Others | Others |
Tat-NR2B9c TFA is a 20-aa peptide, and acts as an inhibitor of postsynaptic density-95 (PSD-95)(EC50 of 6.7 nM for PSD-95d2), and possesses neuroprotective efficacy. | |||
T25953 |
PHPS1 Sodium
PHPS1 Na,PHPS1 Sodium salt |
||
PHPS1 sodium 是 Shp2的选择性抑制剂,对 Shp2,Shp2-R362K,Shp1,PTP1B 和 PTP1B-Q 的Ki 值分别为 0.73,5.8,10.7,5.8 和 0.47 μM。 | |||
T6645 |
Ropivacaine hydrochloride monohydrate
Ropivacaine HCl,Ropivacaine HCl monohydrate,LEA 103,盐酸罗哌卡因,盐酸罗哌卡因一水合物,LEA-103 HCl |
Potassium Channel; Sodium Channel | Membrane transporter/Ion channel |
Ropivacaine hydrochloride monohydrate (LEA-103 HCl) 是钠通道阻断剂,通过可逆地抑制钠离子内流从而引起神经纤维脉冲传导阻滞。Ropivacaine HCl monohydrate 也是 K2P(双孔钾通道)TREK-1的抑制剂。在动物实验模型中,Ropivacaine HCl monohydrate 可用于神经性疼痛的缓解。 | |||
T0843 |
Triamterene
氨苯蝶啶,Ademine,SKF8542 |
Sodium Channel; GPCR19 | GPCR/G Protein; Membrane transporter/Ion channel |
Ademine 是一种压敏型上皮钠离子通道(ENaC)阻断剂,具有利尿的作用。 | |||
T67073 | 1,2-Distearoyl-sn-glycero-3-phosphatidic acid (Na+ salt) | ||
1,2-Distearoyl-sn-glycero-3-phosphatidic acid (Na+ salt) 是一种有用的有机化合物,可用于生命科学领域的相关研究,其产品编号为 T67073。 | |||
T12219 |
NHE3-IN-1
|
Sodium Channel | Membrane transporter/Ion channel |
NHE3-IN-1 是钠/质子交换剂 3 (NHE-3) 的抑制剂。 | |||
T5319 |
Rimeporide
EMD-87580 |
Sodium Channel | Membrane transporter/Ion channel |
Rimeporide (EMD-87580) 是有效的 Na+/H+交换泵 (NHE-1) 选择性抑制剂。 | |||
T5333 |
Rimeporide hydrochloride
盐酸Rimeporide,EMD-87580 hydrochloride |
Sodium Channel | Membrane transporter/Ion channel |
Rimeporide hydrochloride (EMD-87580 hydrochloride) 是一种有效的 Na+/H+交换泵(NHE-1) 选择性抑制剂。 | |||
T17243 |
VU0463271
N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide |
Potassium Channel | Membrane transporter/Ion channel |
VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) 是一种有效的、特异性的 KCC2 拮抗剂,其 IC50 为 61 nM,特异性是密切相关的 Na-K-2Cl 协同转运蛋白 1 (NKCC1) 的 100 倍以上,在更大的 GPCR、离子通道和转运蛋白面板中没有活性。 | |||
T2238 |
Cariporide
卡立泊来德,HOE-642 |
Sodium Channel | Membrane transporter/Ion channel |
Cariporide (HOE-642) 是一种选择性的Na+/H+交换抑制剂。 | |||
T6641 |
Rilmenidine Phosphate
|
Apoptosis; Adrenergic Receptor; Autophagy; Imidazoline Receptor | Apoptosis; Autophagy; GPCR/G Protein; Neuroscience |
Rilmenidine phosphate 是一种新型的抗高血压药物和口服活性选择性 I1 咪唑啉受体激动剂。它可调节白血病细胞增殖,刺激促凋亡蛋白 Bax,从而诱导人白血病 K562 细胞线粒体通路的紊乱和凋亡。它可通过减少交感神经过度活跃而发挥中枢作用,并通过抑制 Na+/H+反向转运而在肾脏中发挥作用。 | |||
TP1033L |
Transdermal Peptide Disulfide Acetate
TD 1 (peptide) acetate,Transdermal Peptide Disulfide Acetate (888486-23-5 free base) |
ATPase | Membrane transporter/Ion channel |
Transdermal Peptide acetate(888486-23-5 free base) (TD 1 (peptide) acetate) 是一种 11 个氨基酸的肽,与 Na+/K+-ATPase β 亚基 (ATP1B1) 结合,主要与 ATP1B1 的 C 端相互作用。透皮肽可以增强许多大分子的透皮传递。透皮肽 TD 1 酰胺是一种新型肽,旨在增强透皮药物传递。 | |||
T36949 |
Niaprazine
|
5-HT Receptor; Adrenergic Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Niaprazine 是有效的组胺 H1 受体拮抗剂,具有抗组胺和抗血清素活性。Niaprazine 在睡眠障碍方面有研究的价值。 | |||
T2238L |
Cariporide Mesylate
Cariporide Mesylate salt,HOE-642,HOE 642,HOE642 |
||
Cariporide Mesylate is a selective inhibitor of the Na+/H+ exchanger isoform 1. | |||
T60652 |
NHE3-IN-2
|
||
NHE3-IN-2 是Na+/H+交换体 3(NHE3)的抑制剂 。 | |||
T37473 |
SBFI AM
Sodium-binding Benzofuran Isophthalate Acetoxymethyl ester |
||
SBFI AM is a membrane-permeant, fluorescent Na+ indicator dye. It is selective for Na+ over K+ with Kd values of 20 and 120 mM for these ions, respectively. [1]Increasing concentration of Na+ increases the ratio of excitation efficiency at 330-345 nm to that at 370-390 nm with emission collected at 450-550 nm. [1] Therefore, ratio fluorometry and imaging can be performed with the same wavelengths. SBF AM is suitable for single intracellular dye injection and is typically used for high-resolutio... | |||
T80451 |
Ceratotoxin-2
CcoTx2,β-TRTX-cm1b |
Sodium Channel | Membrane transporter/Ion channel |
Ceratotoxin-2 (CcoTx2) 为针对电压门控的钠通道阻滞剂,显示对Nav1.2/β1和Nav1.3/β1的强效选择性,其IC50值分别为8 nM及88 nM。 | |||
T80039 |
ATX-II
|
Sodium Channel | Membrane transporter/Ion channel |
ATX-II为特定Na+通道调节剂,源自海葵(Anemonia sulcata)毒液。该化合物会使细胞培养物对Na+Halothane、Caffeine及Ryanodine敏感,并可诱发肺静脉心律失常及心房颤动。 | |||
T75280 | Prilocaine acetate | ||
Prilocaine acetate 是一种氨基酰胺。Prilocaine acetate 是一种Na/K-ATPase 抑制剂。Prilocaine acetate 具有神经毒性作用。 | |||
T76374 |
SPAI-1
|
||
SPAI-1,特异性单价阳离子ATP酶抑制剂,源自猪十二指肠。能体外抑制Na+,K+-ATP酶和H+,K+-ATP酶,同时刺激Mg2+-ATP酶。 | |||
T37707 |
14-Anhydrodigitoxigenin
|
||
14-Anhydrodigitoxigenin is a cardenolide and a derivative of digitoxin.1 It reduces the activity of guinea pig heart Na+/K+-ATPase by 15% when used at a concentration of 10 μM.2 | |||
T78564 |
Depramine
GP 31406 |
||
Depramine (GP 31406) 是三环抗抑郁剂,具药理活性。该化合物可抑制乙酰胆碱酯酶、Mg2+-ATPase 与 Na+/K+ ATPase 活性。 | |||
T60469 |
Chloroprocaine
|
||
Chloroprocaine (2-Chloroprocaine) 是一种有效的Na,K-ATPase 酶活性抑制剂(IC50 = 13 mM)。Chloroprocaine 是一种阻滞外周神经的局部麻醉剂。 | |||
T35923 |
Caloxin 2A1 TFA
|
||
Caloxin 2A1 TFA is a peptide inhibitor specifically targeting the extracellular plasma membrane Ca2+-ATPase (PMCA), without influencing the basal activities of Mg2+-ATPase or Na+-K+-ATPase[1]. | |||
T37767 |
Transdermal Peptide Disulfide TFA
|
||
Transdermal Peptide Disulfide TFA (TD 1 Disulfide(peptide) TFA), an 11-amino acid peptide, specifically binds to the Na+/K+-ATPase beta-subunit (ATP1B1), predominantly interacting with its C-terminus. This compound is capable of enhancing the transdermal delivery of various macromolecules[1]. | |||
T80494 |
Tap1a
TRTX-Tap1a,Theraphotoxin-Tap1a,µ/ω-TRTX-Tap1a |
Sodium Channel | Membrane transporter/Ion channel |
Tap1a (Theraphotoxin-Tap1a) 是抑制sodium channels的一种蜘蛛毒液肽,其对Nav1.7的IC50为80 nM,对Nav1.1为301 nM,显示出缓解疼痛的潜能。 | |||
T82936 |
ATX-II TFA
|
Sodium Channel | Membrane transporter/Ion channel |
ATX-II TFA为源自海葵(Anemonia sulcata)毒素的特定Na+通道调节剂,能使细胞培养物对Na+、Halothane、Caffeine和Ryanodine敏感,并可诱发肺静脉心律失常和心房颤动。 | |||
T61480 |
NHE3-IN-3
|
||
NHE3-IN-3 (Compound 1) is a potent inhibitor of the isoform 3 of the Na+/H+ exchanger (NHE3). It exhibits pIC50 values of 6.2 and 6.6 against human and rat NHE3, respectively. Furthermore, NHE3-IN-3 showcases exceptional oral bioavailability of 98% in Sprague–Dawley rats [1]. | |||
T75971 |
γ-1-Melanocyte Stimulating Hormone (MSH), amide
|
||
γ-1-Melanocyte Stimulating Hormone (MSH), amide为含11个氨基酸的多肽,主要通过激活黑皮质素受体3 (MC3-R) 调节钠 (Na+) 平衡及血压。 | |||
T80178 |
Dc1a
|
Sodium Channel | Membrane transporter/Ion channel |
Dc1a是一种从沙漠灌木蜘蛛Diguetia canities分离的毒素,有效促进德国小蠊Nav通道(BgNav1)的开放。 | |||
TP1268 |
CEF19, Epstein-Barr Virus latent NA-3A (458-466)
CEF19,Epstein-Barr Virus latent NA-3A 458-466 |
||
CEF19, Epstein-Barr Virus latent NA-3A (458-466) is a single peptide epitope, YPLHEQHGM, representing residues 458-466 of the type 1 Epstein-Barr Virus (EBV) nuclear antigen 3A protein (B95.8 strain). | |||
T73083 |
Nipradolol
KT 210 ; K 351 ; Hypadil,Hypadil,KT 210,K 351 |
||
Nipradolol (KT-210; K-351) 是一种有效的 α-1-肾上腺素能受体的阻滞剂。Nipradolol 还抑制白化兔模型中 Phenylephrine 诱导的眼压升高 (IOP)。Nipradolol 抑制去甲肾上腺素 (NA) 引起的肌肉收缩,对犬冠状动脉也有血管扩张剂活性。 | |||
T75593 | Parabuthus Granulatus Venom | ||
Parabuthus Granulatus Venom (Granulated Thick-tailed Venom) 是蝎子 Parabuthus granulatus 分泌的一种毒液,其中包含两种主要毒素,能够抑制电压门控Ca2+和Na+ channels。 | |||
T75360 |
Oxonol VI
|
||
Oxonol VI 是一种膜电位的光学指示剂,在脂质囊泡中发挥作用。它能用于监测重组囊泡中与 (Na++K+)-ATPase 活性相关的膜电位变化。 | |||
T37766 |
Transdermal Peptide (TD 1 (peptide))
|
||
Transdermal Peptide is a 11-amino acid peptide, binds to Na+/K+-ATPase beta-subunit (ATP1B1), and enhances the transdermal delivery of many macromolecules. Transdermal Peptide (TD1) binds to ATP1B1, and mainly interacts with the C-terminus of ATP1B1 in yeast and mammalian cells. The interaction affects the expression and localization of ATP1B1 and epidermal structure, but can be antagonized by the exogenous competitor ATP1B1 or be inhibited by ouabain. Inhibition of Transdermal Peptide binding t... | |||
T80454 |
BmK-M1
|
Sodium Channel | Membrane transporter/Ion channel |
BmK-M1,一种含64个氨基酸通过四个二硫桥交联形成的蝎子毒素,作用于抑制Na+通道,属于心脏毒素和神经毒素类。 | |||
T60526 | N-Salicyloyltryptamine | ||
N-Salicyloyltryptamine(STP) 是一种色胺类似物,具有抗惊厥、抗炎、镇痛和血管舒张的作用。N-Salicyloyltryptamine 作为电压依赖性离子通道(包括Na+、Ca2+、K+离子通道)抑制剂,可抑制 K+电流,IC50值为 34.6 μM ( /to)。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6856 |
Halofuginone
卤夫酮,常山酮,Tempostatin,empostatin,RU-19110 |
Calcium Channel; DNA/RNA Synthesis; Sodium Channel; Parasite; TGF-beta/Smad | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Stem Cells |
Halofuginone (RU-19110) 是Febrifugine 的衍生物,是一种竞争性脯氨酰-tRNA 合成酶抑制剂。它也是肺血管扩张剂,可激活Kv 通道并阻断电压门控、受体操作和存储操作的钙离子通道。它具有抗炎、抗癌、抗疟疾和抗纤维化作用。 | |||
T3524 |
Halofuginone hydrobromide
卤夫酮溴氢酸盐,Tempostatin,RU-19110 (hydrobromide),Stenorol,常山酮溴酸盐 |
Others; Calcium Channel; DNA/RNA Synthesis; Sodium Channel; Parasite; TGF-beta/Smad | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Others; Stem Cells |
Halofuginone hydrobromid 是Febrifugine 的衍生物,是竞争性脯氨酰-tRNA 合成酶抑制剂。它是 I 型胶原合成的特异性抑制剂,并通过抑制TGF-β活性可减轻骨关节炎。它具有抗疟疾、抗炎、抗癌、抗纤维化作用。 | |||
T2822 |
Ginsenoside Rb1
Gypenoside Ⅲ,人参皂苷Rb1,人参皂苷 Rb1,Gypenoside III |
ATPase; Mitophagy; IRAK; NF-κB; Autophagy; HSV | Autophagy; Immunology/Inflammation; Membrane transporter/Ion channel; Microbiology/Virology; NF-κB |
Ginsenoside Rb1 (Gypenoside Ⅲ) 是中药人参的成分,可能具有抑制或阻止肿瘤生长的特性。 | |||
TN6713 |
6-Benzoylheteratisine
Heteratisan-14-one, 6-(benzoyloxy)-20-ethyl-8-hydroxy-1-methoxy-4-meth,苯甲酰新异乌头碱 |
Sodium Channel | Membrane transporter/Ion channel |
6-Benzoylheteratisine (Heteratisan-14-one, 6-(benzoyloxy)-20-ethyl-8-hydroxy-1-methoxy-4-meth) 是乌头碱的拮抗剂,乌头碱是天然 Na+通道激活剂。 | |||
T29078 |
Ursodeoxycholic acid sodium
UDCA Na,UDCA sodium,Sodium Ursodeoxycholate,熊去氧胆酸钠盐,Ursodiol sodium,Ursodeoxycholic Acid (sodium salt),Ursodeoxycholate sodium |
FXR; Endogenous Metabolite; GPCR19 | GPCR/G Protein; Metabolism |
Ursodeoxycholic acid sodium (Sodium Ursodeoxycholate) 是一种天然存在的次级胆汁酸,具有抗炎和细胞保护活性。Ursodeoxycholic acid sodium 作为信号分子,通过与胆汁酸激活受体相互作用发挥其作用,包括 G 蛋白偶联胆汁酸受体 5 (TGR5) 和法尼醇 X 受体 (FXR)。 | |||
TN5073 |
Strophanthidin
毒毛旋花子甙元,Strophanthidine,葡萄球菌素 |
ATPase; Calcium Channel | Membrane transporter/Ion channel; Metabolism |
Strophanthidin (Strophanthidine) 是黄花夹竹桃中的一种类固醇,可增加舒张期和收缩期胞内 Ca2+浓度。它在 0.1 和 1 nmol/L 增加Na+/K+-ATPase 活性,1到100 μ mol/L 抑制Na+/K+-ATPase 活性,10 和 100 nmol/L 对Na+/K+-ATPase 活性无影响。 | |||
T5S0890 |
Oleandrin
Neriostene,Folinerin,Foliandrin,欧夹竹桃苷 |
Apoptosis; ATPase; Potassium Channel; Sodium Channel | Apoptosis; Membrane transporter/Ion channel |
Oleandrin (Folinerin) 是夹竹桃属中的一种类固醇,可抑制Na+/K+-ATPase 活性,IC50为 620 nM。 | |||
T1719 |
Bufalin
|
ATPase | Membrane transporter/Ion channel |
Bufalin 是蟾酥中的一种成分,是Na+/K+-ATPase 抑制剂,具有抗肿瘤活性,可与其基 α1、α2 和 α3 结合,Kd 值分别为 42.5、45 和 40 nM。 | |||
T4973 |
Paraxanthine
1,7-二甲基黄嘌呤,1,7-DIMETHYLXANTHINE |
Endogenous Metabolite | Metabolism |
Paraxanthine (1,7-dimethylxanthine) 是一种 caffeine 的代谢物,能够刺激Ryanodine 受体通道来抑制多巴胺能细胞的死亡。 | |||
TJP2872 |
Acevaltrate
Acevaltratum,乙酰缬草三酯,Acetoxyvaltrate |
ATPase; Others | Membrane transporter/Ion channel; Others |
Acevaltrate (Acevaltratum) 对人小细胞肺癌细胞系 GLC(4) 和人结肠直肠癌细胞系 COLO 320 具有高细胞毒性,IC50 值为 1-6 uM。它抑制大鼠肾和脑半球中 Na+/K+-ATP 酶活性,IC50分别为 22.8 和 42.3 μM。 | |||
T5S1982 |
Periplocin
Periplocoside,杠柳毒苷 |
Apoptosis; Others | Apoptosis; Others |
Periplocin (Periplocoside) 是从黑龙骨中分离出的一种强心类固醇。它可促进肿瘤细胞凋亡并抑制肿瘤生长。它通过激活 Na/K-ATPase 介导的 Src/ERK 和 PI3K/Akt 途径,具有促进伤口愈合的潜力。 | |||
TCA2511 |
11Beta-hydroxyprogesterone
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Sodium Channel | Membrane transporter/Ion channel |
The progesterone derivatives 11 alpha- and 11 beta-hydroxyprogesterone are potent inhibitors of 11 beta-hydroxysteroid dehydrogenase (isoforms 1 and 2) in vitro and can confer mineralocorticoid activity on corticosterone in the rat in vivo. 11beta-Hydroxyprogesterone acts as a mineralocorticoid agonist in stimulating Na+ absorption in mammalian principal cortical collecting duct cells. | |||
T72429 |
α-Lipoic Acid sodium
Thioctic acid sodium,DL-α-Lipoic acid sodium,Thioctic acid sodium ; (±)-α-Lipoic acid sodium ; DL-α-Lipoic acid sodium,(±)-α-Lipoic acid sodium |
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α-Lipoic Acid (Thioctic acid) sodium 是一种抗氧化剂,是线粒体酶复合物的重要辅助因子。α-Lipoic Acid sodium 可抑制NF-κB 依赖性的HIV-1LTR 活化。α-Lipoic Acid sodium 诱导内质网应激 (ERS) 介导的肝癌细胞凋亡 (apoptosis)。α-Lipoic Acid sodium 可与CPUL1 合成自组装的纳米聚合体 CPUL1-LA NA,其抗肿瘤效果优于 CPUL1。 | |||
TN4108 |
Ganoderic acid Z
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Antifection | Microbiology/Virology |
The binding affinities of ganoderic acid DM and ganoderic acid Z (ÎGbind, -16.83 and-10.99 kcal mol-1) are comparable to that of current commercial drug oseltamivir (-23.62 kcal mol-1);Ganoderic acid DM is a potential source of anti-influenza ingredient, with novel binding pattern and advantage over oseltamivir, it has steric hindrance on the 150 cavity of N1 protein, and exerts activities across the H274Y and N294S mutations, is the attractive candidates of novel neuraminidase (NA) inhibitors.... | |||
T82764 |
Cd1a
β-TRTX-cd1a,β-Theraphotoxin-cd1a |
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Cd1a是从非洲蜘蛛Ceratogyrus darlingi中提取的β-毒素,具有调节钙离子通道的功能。它能够抑制人类的钙离子通道(Cav2.2)(IC50 2.6 μM)以及小鼠的钠离子通道(Nav1.7),有望用于开发治疗外周疼痛的药物。 | |||
T38069 |
Aquastatin A
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Aquastatin A is a fungal metabolite originally isolated fromF. aquaeductuumthat has diverse biological activities.1It is active againstS. aureus(MIC = 32 μg/ml) and inhibits enoyl-acyl carrier protein reductase (Fabl; IC50= 3.2 μM) andS. aureusfatty acid synthesis (IC50= 3.5 μM).2Aquastatin A also inhibits the Na+/K+-ATPase and H+/K+-ATPase (IC50s = 7.1 and 6.2 μM, respectively), as well as protein tyrosine phosphatase 1B (PTP1B; IC50= 0.19 μM).1,3 1.Hamano, K., Kinoshita-Okami, M., Minagawa, K.... | |||
T35779 |
Oosporein
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Oosporein is a mycotoxin that has been found inBeauveriaand has diverse biological activities.1,2It is cytotoxic to Sf9 and Sf21 insect cells with 50% cytotoxic concentration (CC50) values of 4.23 and 10.43 μM, respectively.3Oosporin induces lethality in day-old cockerels (LD50= 6.12 mg/kg).4It inhibits Na+/K+-, Ca2+-, and Mg2+-ATPase activities by 27, 52, and 100%, respectively, in equine erythrocyte ghosts when used at a concentration of 200 μg/ml.2Oosporein inhibits herpes simplex 1 (HSV-1), ... |