74
8
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12855 |
SB 258719
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
SB 258719 是高亲和力的、选择性的5-HT7受体拮抗剂,pKi 为7.5。SB 258719在癌症和神经系统疾病领域有研究价值。 | |||
T70038 |
MJN68390
|
Caspase | Apoptosis; Proteases/Proteasome |
MJN68390 对 CASP8 的表观 IC50值为 15 μM,对 CASP10 不显示活性。 | |||
T11303 |
Fluorobexarotene
|
Retinoid Receptor | Metabolism |
Fluorobexarotene 是一种有效的 类视黄醇 X 受体 (RXR) 激动剂。Fluorobexarotene 对 RXRα 受体的 Ki 值为 12 nM,EC50 值为 43 nM。Fluorobexarotene 具有明显的 RXR 结合亲和力,比 Bexarotene 高75%。 | |||
T7045 |
Clonidine
Nexiclon,Catapres,Kapvay,可乐定 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Clonidine (Kapvay) 是 alpha2 肾上腺素能激动剂。 | |||
T14988 |
CMPD1
|
MAPK | MAPK |
CMPD1 是非 ATP 竞争性 p38 MAPK 介导的 MK2磷酸化选择性抑制剂(Ki:330 nM)。 | |||
T6452 |
Closantel Sodium
|
Antibacterial; Parasite | Microbiology/Virology |
Closantel sodium 是抗寄生虫活性的卤化水杨酰苯胺。它是高度特异性的盘尾丝虫几丁质酶抑制剂。 | |||
T0226 |
Betaxolol hydrochloride
盐酸倍他洛尔,SL75212,SL 75212 HCl,Betaxolol HCl |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Betaxolol hydrochloride (SL 75212 HCl) 是一种 β1 肾上腺素受体阻断剂,可用于研究高血压和青光眼。 | |||
T0085L |
Entecavir
BMS200475,SQ34676,恩替卡韦 |
HBV | Microbiology/Virology |
Entecavir (SQ34676) 是一种选择性 HBV 抑制剂,在 HepG2细胞中的 EC50值为3.75 nM。 | |||
T9240 |
sulfopin
Acetamide, 2-chloro-N-(2,2-dimethylpropyl)-N-(tetrahydro-1,1-dioxido-3-thienyl)- |
Others | Others |
Sulfopin 是高选择性共价Pin1抑制剂(Ki:17 nM),在体内能够阻断 Myc 驱动的肿瘤。其中肽基脯氨酰异构酶 Pin1 在癌症中被用来激活癌基因和灭活肿瘤抑制因子。 | |||
T9263 |
cim0216
N-(5-methyl-1,2-oxazol-3-yl)-2-phenyl-2-(1,2,3,4-tetrahydroquinolin-1-yl)acetamide |
TRP/TRPV Channel | Membrane transporter/Ion channel |
CIM0216 是选择性的TRPM3激动剂,对 TRPM3 的选择性高于 TRPM1、TRPM2 和 TRPM4-8。它以TRPM3依赖性的方式引起疼痛并唤起感觉神经末梢的神经肽释放,可用于神经源性炎症的相关研究。 | |||
T1088 |
Repaglinide
AG-EE 388 ZW,AG-EE 623ZW,瑞格列奈 |
Potassium Channel; PPAR | DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism |
Repaglinide (AG-EE 623ZW) 是一种能够用于2 型糖尿病的胰岛素促分泌剂。 | |||
T2555 |
Aclidinium bromide
LAS 34273,LAS-W 330,阿地溴铵 |
AChR | Neuroscience |
Aclidinium bromide (LAS-W 330) 是长效可吸入型的毒蕈碱拮抗剂,有用于慢性阻塞性肺病 (COPD) 的研究潜力。 | |||
T0929 |
Docusate sodium
Aerosol OT,多库脂钠,Dioctyl sulfosuccinate sodium salt,Bis(2-ethylhexyl) sulfosuccinate sodium salt,Constonate |
Opioid Receptor; HSV | Endocrinology/Hormones; GPCR/G Protein; Microbiology/Virology; Neuroscience |
Docusate sodium (Aerosol OT) 是一种口服的非处方泻药和大便软化剂,可用于研究便秘。 | |||
T1472 |
Trospium chloride
Spasmex,Sanctura,曲司氯铵,曲司氯胺 |
AChR | Neuroscience |
Trospium chloride (Spasmex) 是一种可口服的特异竞争性毒蕈碱胆碱能受体拮抗剂,可与毒蕈碱受体 M1、M2 和 M3 高亲和力结合,具有抗毒蕈碱活性。 | |||
T0137 |
Mirtazapine
米氮平,6-Azamianserin,Org3770 |
Dopamine Receptor; 5-HT Receptor; Opioid Receptor; Adrenergic Receptor; Histamine Receptor | Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Mirtazapine (6-Azamianserin) 是一种有效的具有口服活性的去甲肾上腺素能和特异性血清素能抗抑郁剂 (NaSSA)。它也是一种5-HT2、5-HT3、组胺 H1 受体和 α2-肾上腺素受体拮抗剂,pKi 值分别为 8.05、8.1、9.3 和 6.95。 | |||
T1655 |
Ambrisentan
BSF-208075,BSF 208075,安倍生坦,LU 208075 |
Endothelin Receptor | GPCR/G Protein |
Ambrisentan (BSF 208075) 是 ET A 型受体选择性拮抗剂。 | |||
T4297 |
Flibanserin
BIMT-17BS,氟立班丝氨,Girosa,BIMT-17 |
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
Flibanserin (Girosa) 一种具有口服活性的 5-HT1A 受体激动剂和 5-HT2A 受体拮抗剂,Ki 值分别为 1 和 49 nM。它与多巴胺 D4 受体结合,Ki 值在 4 到 24 nM 之间。它是一种血清素能抗抑郁药,用于治疗性欲减退症。 | |||
T0078L |
Lapatinib ditosylate monohydrate
Lapatinib ditosylate monohydrate,Lapatinib ditoluenesulfonate monohydrate,Lapatinib tosilate hydrate,Lapatinib tosilate,Tykerb,二甲苯磺酸拉帕替尼单水合物,Tyverb |
EGFR; Ferroptosis; Autophagy | Angiogenesis; Apoptosis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Lapatinib ditosylate (Lapatinib tosilate) monohydrate 是一种有效的 EGFR 和 ErbB2 抑制剂,对 EGFR 和 ErbB2的 IC50值分别为 10.8 和 9.2 nM。它用于治疗晚期乳腺癌和其他实体瘤。 | |||
T1677L |
Montelukast sodium
MK0476,孟鲁司特钠 |
Leukotriene Receptor; LTR | GPCR/G Protein; Immunology/Inflammation |
Montelukast sodium (MK0476) 是可口服的半胱氨酸白三烯受体1 选择性拮抗剂,可用于研究预防哮喘和肝损伤。它还可减少心脏损伤,在肠缺血-再灌注损伤中也具有抗氧化作用。 | |||
T0192 |
Levetiracetam
左乙拉西坦,UCB L059,SIB-S1 |
DNA Methyltransferase; Others; Calcium Channel | Chromatin/Epigenetic; Membrane transporter/Ion channel; Metabolism; Others |
Levetiracetam (SIB-S1) 是一种化学增敏剂,增强 Temozolomide 对胶质母细胞瘤干细胞增殖和凋亡的影响。它调节 HDAC 水平,最终使 MGMT 沉默从而提高 Temozolomide 的有效性。它是一种抗癫痫药,可结合突触小泡蛋白 SV2A。 | |||
T0083 |
Eplerenone
Epoxymexrenone,CGP 30083,依普利酮,SC-66110 |
Glucocorticoid Receptor | Endocrinology/Hormones |
Eplerenone (CGP 30083) 是一种竞争性的、选择性的、具有口服活性的醛固酮 (aldosterone) 拮抗剂,IC50=138 nM。它对孕酮,雄激素,雌激素和糖皮质激素受体的亲和力低,可用于研究高血压和心肌梗死后的心力衰竭。 | |||
T3142 |
Drostanolone Propionate
|
Others | Others |
Dromostanolone propionate (Drostanolone propionate) 是一种具有抗乳腺癌活性的化合物。Dromostanolone propionate 抑制肿瘤对雌二醇 -17 的摄取,但对正常乳腺组织的摄取没有明显影响。Dromostanolone propionate 植入颗粒可使动物的体重增加,并抑制雌性动物的发情。 | |||
T1951 |
Asenapine Maleate
Org 5222 maleate,Org 5222,马来酸阿塞那平,阿塞那平马来酸盐 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Asenapine Maleate (Org 5222 maleate) 是5-HT 和D2的拮抗剂,Ki 值分别为 0.03-4.0 nM, 1.3 nM。它也是抗精神病药物,用于治疗与双相 1 型障碍相关的精神分裂症和躁狂或混合发作。 | |||
T2004 |
Ciproxifan maleate
FUB 359 maleate,FUB 359 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Ciproxifan maleate (FUB 359) 是一种选择性的,可口服和竞争性的组胺H3受体拮抗剂,IC50值为 9.2 nM。它对其他受体亚型的表观亲和力低,可用于研究衰老性疾病和阿尔兹海默症。 | |||
T6875 |
Lesinurad
RDEA594,雷西那德,来司诺雷 |
OAT | Membrane transporter/Ion channel |
Lesinurad (RDEA594) 是URAT1和OAT 抑制剂。Lesinurad 用作肾转运蛋白OAT1 和OAT3 的底物,Km 分别为 0.85 和 2 μM。 | |||
T0189L |
Pemetrexed disodium
培美曲塞二钠盐,LY-231514,LY231514 disodium,培美曲塞二钠,Pemetrexed |
Apoptosis; DHFR; DNA/RNA Synthesis; Antifolate; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism |
Pemetrexed disodium (LY-231514) 是一种叶酸拮抗剂,用于治疗非小细胞肺癌和恶性间皮瘤。它抑制胸苷酸合成酶,二氢叶酸还原酶和甘氨酰胺核苷酸甲酰转移酶的Ki 分别为 1.3 nM,7.2 nM 和 65 nM。 | |||
T1674 |
Nateglinide
那格列奈,A4166,Senaglinide |
Potassium Channel; Proteasome; PPAR | DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Proteases/Proteasome; Ubiquitination |
Nateglinide (Senaglinide) 是 D-苯丙氨酸的一种衍生物,是口服有效的、短效促胰岛素释放化合物,也是 DPP IV 抑制剂。 Nateglinide 抑制胰岛 β 细胞中 ATP 敏感的 K+通道。Nateglinide 在 2 型糖尿病中具有研究价值。 | |||
T6647 |
Rotigotine-
Neupro,N-0923,罗替戈汀,N-0437,SPM 962 |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Rotigotine (N-0923) 是多巴胺受体激动剂,是5-HT1A receptor 的部分激动剂,以及α2B-肾上腺素受体的拮抗剂,用于治疗帕金森病和不宁腿综合征。 | |||
T1189 |
Milnacipran hydrochloride
盐酸米那普仑,Milnacipran HCl,Savella,Dalcipran |
Serotonin Transporter; Norepinephrine | Neuroscience |
Milnacipran hydrochloride (Savella) 是一种5-羟色胺-去甲肾上腺素重吸收抑制剂(SNRI),可用于纤维肌痛的研究。 | |||
T1786 |
Daclatasvir dihydrochloride
BMS-790052 dihydrochloride,盐酸达拉他韦 |
HCV Protease | Microbiology/Virology; Proteases/Proteasome |
Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) 是有机阴离子转运多肽 1B(OATP1B) 和 OATP1B3抑制剂,IC50分别为 1.5 µM 和 3.27 µM。它也具有口服活性的 HCV NS5A 蛋白抑制剂,多种 HCV 复制子基因型的 EC50范围为 9-146 pM。 | |||
T1476 |
Pramipexole
SND 919,普拉克索 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
Pramipexole (SND 919) 是能够透过血脑屏障的 D2 型多巴胺受体的选择性激动剂,对 D2 型受体、D2、D3、D4亚型受体的Ki 分别为 2.2 nM、3.9 nM、0.5 nM、1.3 nM。它可用于研究帕金森综合症和腿多动综合征。 | |||
T28946 |
Tenofovir exalidex
Tenofovir,HDP-Tenofovir,CMX-157,CMX157,CMX 157 |
Antiviral | Immunology/Inflammation |
Tenofovir exalidex (CMX 157) 是一种非环核苷酸类似物 Tenofovir 的脂质结合物,对野生型和抗逆转录病毒耐药的 HIV 毒株,包括多药核苷/核苷酸类似物耐药病毒,都有活性。Tenofovir exalidex 对人外周血单个核细胞中所有主要的HIV-1和HIV-2亚型以及单核细胞来源的巨噬细胞中所有 HIV-1 菌株具有活性,EC50 范围在 0.2 和 7.2 nM 之间。Tenofovir exalidex 具有口服活性,无明显毒性。Tenofovir exalidex 对 HBV 也有活性。 | |||
T17193 |
UBP 302
|
Others | Others |
UBP 302 is an effective and selective GLUK5-subunit-containing kainate receptor antagonist (apparent Kd=402 nM) and displays very little affinity on GluK2 kainate receptors. | |||
T28563 |
Ro 18-5364
Ro-18-5364,Ro 185364 |
||
Ro 18-5364 is a potent inhibitor of the gastric (H+ + K+)-ATPase with an apparent Ki of 0.1 μM at pH 6. | |||
T41184 |
Clocinnamox mesylate
C-CAM,NIH 10443 |
||
Clocinnamox mesylate is a systemically active, irreversibleμ-opioid receptor antagonist (apparent Kivalues are 0.7, 1.9 and 5.7 nM for mouseμ,δandκreceptors respectively). | |||
T70148 |
CDK8-IN-4k
|
||
CDK8-IN-4k is a potent and highly selective CDK8 inhibitor, with no apparent potential for time-dependent CYP3A4 inhibition. | |||
T23941 |
DA 4360
DA4360,DA-4360 |
||
DA 4360 is an H2-receptor antagonist. The compounds which were investigated in a wider concentration range, behaved as simple competitive antagonists, yielding apparent KB values comparable with those estimated in conventional H2-receptor assays. | |||
T23942 |
DA 4626
DA4626,DA-4626 |
||
DA 4626 is H2-receptor antagonism. The compound which was investigated in a wider concentration range, behaved as simple competitive antagonists, yielding apparent KB values comparable with those estimated in conventional H2-receptor assays. | |||
T24407 |
LG190119
LG-190119,LG 190119 |
||
LG190119 is a nonsecosteroidal vitamin D receptor modulator. It effectively inhibited LNCaP xenograft tumor growth without increased serum calcium levels or any other apparent side effects. It also inhibits the growth of LNCaP xenograft tumors in athymic | |||
T61140 |
IDO1/TDO-IN-3
|
||
IDO1/TDO-IN-3 is a powerful inhibitor targeting IDO1 and TDO enzymes. It displays noteworthy effectiveness against IDO1 (IC50: 0.005 μM) and TDO (IC50: 0.004 μM). Additionally, IDO1/TDO-IN-3 demonstrates considerable in vivo anti-tumor properties while exhibiting no apparent toxicity [1]. | |||
T38996 |
4α-Methylcholesterol
|
||
4α-Methylcholesterol, a derivative of Cholesterol, possesses the ability to oxidize 3-hydroxy steroid at an apparent K m of 12.6 μM. | |||
T27687 |
JNJ525
JNJ 525,JNJ-525 |
||
JNJ525 is an inhibitor of TNFα. JNJ525 inhibits protein function via an aggregation-based mechanism. JNJ525 prevents the formation of TNFα complexes with TNFR1 and TNFR2, the apparent IC50 values for the inhibition of complex formation are 1.2 ± 0.2 μM an | |||
T40359 |
Thio-ITP
6-Thio-ITP,Thio-ITP,6-Mercaptopurine-riboside-5'-triphosphate,6-Thioinosine 5′-triphosphate |
||
Thio-ITP, also known as 6-Thioinosine 5'-triphosphate, is a competitive inhibitor of RNA polymerase activity. It exhibits a strong apparent affinity towards the polymerases, with Ki values of 40.9 μM for RNA polymerase I and 38.0 μM for RNA polymerase II. | |||
T37897 |
AM-6538
|
||
AM6538 is a long-acting, high affinity, and pseudo-irreversible cannabinoid antagonist, structurally analogous to rimonabant. It serves as a valuable tool for assessing the apparent efficacy of cannabinoid partial and full agonists. Additionally, AM6538 holds potential for future investigations that necessitate temporary reductions in cannabinoid receptor availability[1]. | |||
T1503 |
Esmolol hydrochloride
ASL8052,Esmolol HCl,盐酸艾司洛尔 |
Mitophagy; Adrenergic Receptor; Autophagy | Autophagy; GPCR/G Protein; Neuroscience |
Esmolol hydrochloride 是一种心脏选择性β受体阻滞剂,用于治疗心律失常和严重高血压。 | |||
T82360 |
FXIIa-IN-2
|
||
XIIa-IN-1-IN-2(Compound 21)为一种高效的Factor XIIa抑制剂,具有Kiapp为62.2 nM。该化合物适用于血栓形成的研究领域。 | |||
TP2027 |
GaTx2
|
||
Very high affinity ClC-2 blocker (apparent KD ~ 50 pM). Slows ClC-2 activation and inhibits slow-gating but does not inhibit open ClC-2 channels. Selective for ClC-2 over other ClC family members (ClC-0, ClC-1, ClC-3 and ClC-4), CFTR, GABAC, CaCC and KV1. | |||
T72474 |
Anticancer agent 53
|
||
Anticancer agent 53 是一种强效抗癌剂。 Anticancer agent 53 显示出体外细胞毒性。Anticancer agent 53 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 S/G2/M 期。Anticancer agent 53 具有抗肿瘤活性且无明显毒性。 | |||
T62086 | Tuberculosis inhibitor 5 | ||
Tuberculosis inhibitor 5 (Compound 11i) 是一种有效的抗结核剂,无明显细胞毒性。Tuberculosis inhibitor 5 是一种抗分枝杆菌 (antimycobacterial) 联苯类似物。 | |||
T81348 |
PTZ-LD
|
||
PTZ-LD是一种phenothiazine衍生的荧光探针,专门用于检测脂滴(LDs)。在LDs中,PTZ-LD展示出显著的高特异性发射(Ex/Em=488/570-620 nm)。此探针还可以应用于糖尿病性白内障(DC)的研究工作。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN6764 |
Simmondsin
|
Others | Others |
Simmondsin 是一种来自Simmondsia chinensis——荷荷巴的天然产物。它减少了大鼠的食物摄入量和体重,而没有明显的负面影响。 | |||
T4832 |
Cytosine
6-Aminopyrimidin-2(1H)-one,4-Amino-2-hydroxypyrimidine,Cytosinimine,胞嘧啶 |
Endogenous Metabolite | Metabolism |
Cytosine (6-Aminopyrimidin-2(1H)-one) 是 DNA 和 RNA 中发现的四个主要碱基之一。它修饰表现出与表观遗传多样性和衰老有关的昼夜节律振荡。 | |||
T6194 |
Fidaxomicin
非达米星,Tiacumicin B,OPT-80,Clostomicin B1,PAR-101 |
Apoptosis; DNA/RNA Synthesis; Antibacterial; Antibiotic | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology |
Fidaxomicin (Tiacumicin B) 是一种大环RNA 聚合酶抑制剂,具有窄谱活性。它选择性地根除致病性艰难梭菌,对构成正常健康肠道菌群的多种细菌影响很小。 | |||
T0224 |
Meropenem
美罗培南,SM 7338 |
Others; Antibacterial; Antibiotic | Microbiology/Virology; Others |
Meropenem (SM 7338) 是一种具有广谱抗菌活性的碳青霉烯抗生素,对敏感和耐药的淋病奈瑟氏球菌,流感嗜血杆菌和杜克氏杆菌的 MIC 值分别为 0.02-0.06 mg/mL,0.03-0.12 mg/mL 和 0.015-0.12 mg/mL。 | |||
T2175 |
Apigenin
C.I. Natural Yellow 1,4',5,7-Trihydroxyflavone,NSC 83244,金银花,Apigenol,芹菜素,LY 080400 |
P450; Autophagy | Autophagy; Metabolism |
Apigenin (NSC 83244) 是从韩信草中提取的一种天然产物,是一种竞争性CYP2C9抑制剂,Ki 为 2 μM。它被用作镇静剂、温和的镇痛剂和安眠药。 | |||
TN5079 |
Sulochrin
|
HCV Protease; Antifection | Microbiology/Virology; Proteases/Proteasome |
Sulochrin shows antifungal and antibacterial activities, it can inhibit hepatitis C virus (HCV) infection in a dose-dependent manner without any apparent cytotoxicity up to 50 uM. Sulochrin has an inhibitory activity to eosinophil degranulation. | |||
T73673 |
Thiomarinol A
|
||
Thiomarinol A (4-Hydroxythiomarinol C) 是一种有效的抗生素。Thiomarinol A 是二硫代吡咯酮和海藻酸的混合物。Thiomarinol A 显示出抗菌活性。Thiomarinol A 以剂量依赖性方式抑制 MRSA IleRS,Kiapp 值为 19 nM。 | |||
T10185 |
6-Phosphogluconic acid
|
Others; Endogenous Metabolite | Metabolism; Others |
6-Phosphogluconic acid 是竞争性的磷酸葡萄糖异构酶抑制剂,对6-磷酸果糖和6-磷酸葡萄糖和的 Ki 分别为 42 μM 和 48 μM。它属于人内源性代谢物。 |