69
5
5
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T27719 |
KD-026
SLx 4090,SLx4090,KD026,SLx-4090 |
CETP | Metabolism |
KD-026 (SLx 4090) 是具有口服活性的、肠细胞特异性的微粒体甘油三酯转移蛋白 (MTP)抑制剂,IC50为 8.0 nM。KD-026 (SLx 4090) 在糖尿病2型中有研究的价值。 | |||
T20625 |
Prochloraz
咪鲜胺,Sporgon,Prelude |
Estrogen Receptor/ERR; AhR; Androgen Receptor; Antifungal | Endocrinology/Hormones; Immunology/Inflammation; Metabolism; Microbiology/Virology |
Prochloraz (Prelude) 是咪唑类抗真菌剂。Prochloraz 抑制羊毛甾醇的细胞色素 P450 依赖性 14α-脱甲基作用,由此抑制麦角固醇的生物合成,从而导致真菌细胞膜破裂和细胞死亡。它也是雌激素受体和 雄激素受体的拮抗剂,IC50分别为25 μM 和4 μM, 并激活芳烃受体,EC50为1μM。 | |||
T23861 |
CAY10526
CAY-10526,BTH,CAY 10526 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
CAY10526 (BTH) 是 mPGES-1 的选择性抑制剂,可抑制 NF-κB 信号通路。 | |||
T12856 |
SC-26196
ALPHA,ALPHA-二苯基-4-[(3-吡啶亚甲基)氨基]-1-吡嗪戊腈 |
Others | Others |
SC-26196 是一种 Delta6 去饱和酶 (D6D, FADS2) 抑制剂 (在大鼠肝微粒体中,IC50=0.2 µM),具有口服活性,具有抗炎作用。 | |||
T14523 |
Beauvericin
|
Others; Acyltransferase | Metabolism; Others |
Beauvericin 是一种镰刀菌霉菌毒素。Beauvericin 在大鼠肝微粒体酶实验中对酰基-CoA:胆固醇酰基转移酶(ACAT)有抑制作用,其 IC50 值为 3 μM。 | |||
T28089 |
mPGES-1 Inhibitor-1
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
mPGES-1 Inhibitor-1 是一种新型的微粒体前列腺素 E 合酶-1(mPGES-1)选择性抑制剂,具有抗炎镇痛活性,可用于研究急性肝损伤。 | |||
T2545 |
Lomitapide Mesylate
甲磺酸洛美他派,BMS-201038 mesylate,AEGR-733 mesylate |
CETP | Metabolism |
Lomitapide Mesylate (BMS-201038 mesylate) 是一种高效MTP 蛋白抑制剂,其体外IC50值为8 nM。 | |||
T16928 |
SR144528
|
Cannabinoid Receptor | GPCR/G Protein |
SR144528 是 CB2 受体的拮抗剂 (Ki = 0.6 nM) 并抑制微粒体 ACAT 活性 (IC50 = 3.6 μM)。 | |||
T14564 |
BI-4924
|
Others | Others |
BI-4924 is an inhibitor of phosphoglycerate dehydrogenase (PHGDH) (IC50=3 nM). It has excellent Microsomal and hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis at 72 h ( IC50: 2200 nM). | |||
T16865 |
SCH28080
|
ATPase; Proton pump | Membrane transporter/Ion channel |
SCH28080 是一种可逆且具有 K+ 竞争性的胃 H+/K+-ATP 酶 (H+/K+-ATPase) 抑制剂,IC50 值为 20 nM (家兔微粒体膜)。SCH28080 在体内是有效的酸分泌抑制剂,具有抗溃疡活性、抗分泌和细胞保护活性。 | |||
T27084 |
Crisdesalazine
AAD2004,AAD 2004,AAD-2004 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Crisdesalazine (AAD 2004) 是微粒体前列腺素 E2 合酶 1 (mPGES-1) 的抑制剂。 Crisdesalazine 可减少自噬体形成、轴索病变和运动神经元变性,改善运动功能并延长寿命。 | |||
T30506 |
BMS-212122
UNII-0Z473OO6GB,BMS212122,BMS 212122 |
CETP | Metabolism |
BMS-212122 (UNII-0Z473OO6GB) 是一种有效的微粒体甘油三酯转移蛋白(MTP )抑制剂,在动物实验中显示出降血脂作用。BMS-212122 显著减少动脉粥样硬化斑块中的脂质含量和单核细胞衍生(CD68+)细胞。 | |||
T31992 |
Granotapide
|
CETP | Metabolism |
Granotapide 是一种微粒体甘油三酯转移蛋白(MTP)抑制剂,治疗和而预防动脉硬化,冠状动脉疾病,代谢综合征,肥胖,糖尿病,糖尿病前期和高血压。 | |||
T21738 |
PF-9184
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
PF-9184 是一种有效且高度选择性的人微粒体前列腺素 E 合酶 1 (mPGES-1) 的抑制剂,IC50 值为 16.5 nM。PF-9184 体外抑制 IL-1β 诱导的 PGE2 合成。 | |||
T37825 |
CAY10434
|
P450 | Metabolism |
CAY10434是一种有作用的 CYP4A 羟化酶 (CYP4A hydroxylase) 抑制剂,在人肾微粒体测试中的 IC50值为8.8 nM。CAY 10434 在改善血管紧张素 II 的收缩过程中 Emax 为 6764 mg。 | |||
T15006 |
Dirlotapide
CP742033,Slentrol |
Others; CETP | Metabolism; Others |
Dirlotapide (CP742033) 是一种肠道选择性微粒体甘油三酯转移蛋白(MTP)抑制剂。它可以减轻糖尿病狗的体重。Dirlotapide 以剂量依赖性方式减少食物摄入量,可能是通过增加 肽YY 释放到循环中。 | |||
T1055 |
Ifosfamide
NSC109724,Isophosphamide,异环磷酰胺 |
DNA Alkylator/Crosslinker; DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
Ifosfamide (NSC-109724) 是一种烷化剂,具有抗肿瘤活性。它烷基化并形成 DNA 交联,从而防止 DNA 链分离和 DNA 复制。它是一种前药,必须通过肝微粒体酶的羟基化来激活。 | |||
T6267 |
Lomitapide
AEGR-733,洛美他派,BMS-201038 |
CETP | Metabolism |
Lomitapide (AEGR-733) 是一种高效的微粒体甘油三酯转移蛋白(MTP)抑制剂,体内试验的IC50值为8 nM。 | |||
T9394 |
CHIKV-IN-2
|
Dehydrogenase | Metabolism |
CHIKV-IN-2 基孔肯雅病毒的选择性抑制剂,具有强大的细胞抗病毒活性 (EC90=270 nM) 以及能够改善肝微粒体稳定性。它能够抑制细胞靶二氢乳清酸脱氢酶的活性。 | |||
T72470 |
Estrone O-sulfamate
Estrone 3-O-sulfamate |
Others | Others |
Estrone O-sulfamate (Estrone 3-O-sulfamate) 是一种高效的的类固醇硫酸酯酶 (STS) 抑制剂。Estrone O-sulfamate 是一种胎盘微粒体抑制剂 (P.M.) ,IC50 值分别为 18 nM。Estrone O-sulfamate 在 MCF-7 细胞中对 STS 显示出抑制作用,IC50 值分别为 0.83 nM。Estrone O-sulfamate 可用于研究癌症。 | |||
T35610 |
2,5-dimethyl Celecoxib
|
Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor | Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells |
2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂,mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。 | |||
T6412 |
CVT-12012
|
Stearoyl-CoA Desaturase (SCD) | Metabolism |
CVT-12012 是口服具有活性的硬脂酰-CoA 去饱和酶抑制剂,能够抑制大鼠微粒体和人 HEPG2 的活性,它们的IC50值分别为 38 nM,6.1 nM。 | |||
T12765 |
RPR107393 free base
|
Others | Others |
RPR107393 free base is a selective inhibitor of squalene synthase(rat liver microsomal squalene synthase, with an IC50 of 0.8 nM). | |||
T33110 |
M 79193
M79193,M-79193 |
Others | Others |
M 79193 induces total hepatic microsomal cytochrome P-450. | |||
T25440 |
FR20
FR-20,FR 20 |
Others | Others |
FR20 is a human microsomal prostaglandin synthase 1 (mPGES 1) inhibitor. | |||
T13418 |
CP-319340(free base)
|
Others | Others |
CP-319340 free base is a inhibitor of microsomal triglyceride transfer protein (MTP) . | |||
T24223 |
JTT 130
JTT-130,JTT130 |
Others | Others |
JTT 130 is an agent of hypolipidemic. It inhibits microsomal triglyceride transfer protein. | |||
T15570 |
Implitapide
英普他派,AEGR 427 |
CETP | Metabolism |
Implitapide is an inhibitor of microsomal triglyceride transfer protein (MTP). | |||
T35005 |
Usistapide
R-256918,JNJ-16269110,JNJ16269110,R256918,JNJ 16269110,R 256918 |
Others | Others |
UsISpide(JNJ-16269110 R256918) is an inhibitor of microsomal triglyceride transfer protein (MTTP) under development for the treatment of obesity and type 2 diabetes. | |||
T23596 |
A-933548
A933548,A 933548 |
Others | Others |
A-933548 is a potent Calpain inhibitor. A-933548 features enhanced selectivity versus related cysteine protease cathepsins, favorable microsomal stability, and efficacy in cellular assays. | |||
T10504 | Implitapide Racemate | Others | Others |
Implitapide Racemate is the racemate of Implitapide. Implitapide is an inhibitor of microsomal triglyceride transfer protein (MTP). | |||
T12100 | mPGES1-IN-3 | Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
mPGES1-IN-3 is a potent and selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) . | |||
T16158 |
PF-02575799
|
Adenosine Receptor | GPCR/G Protein; Neuroscience |
PF-02575799 is an inhibitor of microsomal triglyceride transfer protein (MTP) (IC50: 0.77±0.29 nM). | |||
T68375 |
KD026-metabolite
|
Others | Others |
KD026-metabolite, is a metabolite of KD-026. KD026, also known as SLx-4090, is a microsomal triglyceride transfer protein (MTTP) inhibitor potentially for the treatment of type 2 diabetes. | |||
T23598 |
A-953227
A 953227,A953227 |
Others | Others |
A-953227 is a highly effective and selective inhibitor of calpain. A-953227 features enhanced selectivity versus related cysteine protease cathepsins, favorable microsomal stability, and efficacy in cellular assays. | |||
T16504 |
PF-4693627
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
PF-4693627 is an effective and selective microsomal prostaglandin E synthase-1 inhibitor (IC50=3 nM). It is used for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA). | |||
T39000 |
Zaloglanstat
GRC-27864,ISC-27864 |
Others | Others |
Zaloglanstat (ISC-27864) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1). It is utilized in the research of various conditions, including asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain, and neurodegenerative diseases. | |||
T38666 |
CP-346086 dihydrate
|
Others | Others |
CP-346086 dihydrate is a potent and orally active inhibitor of microsomal triglyceride transfer protein (MTP), exhibiting an IC50 value of 2.0 nM for both human and rodent MTP. This compound effectively lowers plasma cholesterol and triglyceride levels in vivo. | |||
T38143 |
Elaidamide
|
Others | Others |
Elaidamide is a fatty acid amide that has been found in the cerebrospinal fluid of sleep-deprived cats.1 It inhibits rat microsomal epoxide hydrolase (mEH; Ki = 70 nM).2 Elaidamide also inhibits porcine pancreatic and human synovial phospholipase A2 (PLA2).3 In vivo, elaidamide (10 mg/animal) induces physiological sleep in rats.1References1. Cravatt, B.F., Prospero-Garcia, O., Siuzdak, G., et al. Chemical characterization of a family of brain lipids that induce sleep. Science 268(5216), 1506-150... | |||
T84952 |
2-Bromoestradiol
2-bromo E2 |
Others | Others |
2-Bromoestradiol 为雌激素2-羟化酶 (estrogen 2-hydroxylase) 抑制剂,能降低放射性标记的雌二醇代谢产物与微粒体蛋白之间的不可逆结合。 | |||
T39303 |
CP-346086
|
Others | Others |
CP-346086 is a highly potent and orally bioavailable inhibitor of microsomal triglyceride transfer protein (MTP), exhibiting an IC50 value of 2.0 nM against both human and rodent MTP. This compound effectively reduces plasma levels of cholesterol and triglycerides when administered in vivo. | |||
T37840 |
20-hydroxy Prostaglandin F2α
20-hydroxy Prostaglandin F2α |
Others | Others |
20-hydroxy Prostaglandin F2α (20-hydroxy PGF2α) is the ω-oxidation product of PGF2α. Cultured type II alveolar cells from pregnant rabbits metabolize exogenous PGF2α via microsomal cytochrome P450 ω-oxidation, producing 20-hydroxy PGF2α and its 15-hydroxy PGDH metabolites. Cells from male rabbits exhibit only the 15-hydroxy PGDH pathway. | |||
T74520 |
TD-802
|
Others | Others |
TD-802 (Compound 33c) 是一种雄激素受体 (androgen receptor)PROTAC 降解剂。TD-802 具有良好的体内抗肿瘤效果,能被用于转移性去势抵抗性前列腺癌的研究。 | |||
T62850 |
IRAK4-IN-13
|
Others | Others |
IRAK4-IN-13 (compound 21) 是一种选择性的、有效的 IRAK4 抑制剂 (IC50: 0.6 nM)。IRAK4-IN-13 具有高代谢清除率,人肝微粒体 (HLM) 固有清除率为 96 μL/min/mg。 | |||
T60346 |
PDE4-IN-10
|
Others | Others |
PDE4-IN-10 (compound 7a) 是一种有效的PDE4抑制剂,其对PDE4B 的IC50值为 7.01 μM。PDE4-IN-10 表现出选择性,微粒体稳定性,对TNF-α有抑制作用,并且在体外无明显毒性。 | |||
T61504 |
PKM2 activator 3
|
Others | Others |
PKM2 activator 3 is a highly potent compound that activates PKM2, with an AC 50 value of 90 nM. It exhibits excellent Caco-2 permeability, a low efflux ratio, and remarkable microsomal stability. PKM2 activator 3 is particularly valuable for anticancer research purposes [1]. (AC 50: the concentration at which 50% enzyme activation occurs.) | |||
T61690 |
mEH-IN-1
|
Others | Others |
mEH-IN-1 (Compound 62) is a potent inhibitor of microsomal epoxide hydrolase (mEH), with an IC50 value of 2.2 nM. mEH is an α/β-fold hydrolase enzyme that is widely expressed in various mammalian tissues, responsible for the hydrolysis of a diverse range of epoxide-containing molecules. This enzyme is primarily localized in the endoplasmic reticulum (ER) of eukaryotic cells. Research involving mEH-IN-1 can contribute to the understanding of preeclampsia, hypercholanemia, and cancer [1]. | |||
T79533 |
PDE5-IN-10
|
Others | Others |
PDE5-IN-10 (compound 4b),一有效PDE5抑制剂,IC50值为20 nM。该化合物体外微粒体稳定性增强(t1/2= 44.6 分钟),在长期增强恢复方面效果显著,适用于阿尔茨海默病(AD)研究。 | |||
T79440 |
DprE1-IN-5
|
Others | Others |
DprE1-IN-5(Compound 10)为一种DprE1抑制剂,对Mtb H37Rv菌株表现出抗结核活性(MIC: 4 μM),并对耐药菌株具有抗分枝杆菌效果,同时展现出较高的微粒体稳定性。 | |||
T75067 | Antimalarial agent 19 | Parasite | Microbiology/Virology |
Antimalarial agent 19(compound 6e)是一种活性抗疟疾化合物,对K1型恶性疟原虫和伯氏疟原虫展现出较强的抑制效果,其EC50值分别为0.3 µM和15.3 µM。相较于γ-肝硫平,该化合物具有更好的水溶性、肠道渗透性以及微粒体稳定性。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5261 |
(E)-Oct-2-enoic acid
trans-2-Octenoic acid,2-Octenoate,2-辛烯酸,2-Octenoic acid |
Others; Endogenous Metabolite | Metabolism; Others |
(E)-Oct-2-enoic acid (2-Octenoate) 是内源性代谢产物的一种。 | |||
TN1818 |
Kaempferol 3-O-β-D-glucuronide
Kaempferol-3-O-glucuronide,Kaempferol-3-beta-O-glucuronide,山奈酚葡萄糖醛酸苷,Kaempferol-3-glucuronide |
IL Receptor | Immunology/Inflammation |
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-beta-O-glucuronide) 具有抗氧化活性。 类黄酮葡糖苷酸可以被来自各种人体细胞的微粒体 α2-葡糖苷酸酶解偶联。 | |||
TN1674 |
Garcinone D
伽升沃 D |
Reactive Oxygen Species; Nrf2; STAT | Immunology/Inflammation; JAK/STAT signaling; Metabolism; NF-κB; Stem Cells |
Garcinone D 是来自山竹的一种呫吨酮,可促进 C17.2 神经干细胞的增殖。它以浓度和时间依赖的方式增加磷酸化信号转导和转录激活因子 3 (p-STAT3)、Cyclin D1 和核因子红细胞 2 相关因子 (Nrf2)、以及血红素加氧酶-1 (HO-1) 的蛋白质水平。 | |||
TN3069 |
4beta-Carboxy-19-nortotarol
|
NADPH-oxidase | Immunology/Inflammation |
4 beta-Carboxy-19-nortotarol can inhibit microsomal lipid peroxidation induced by Fe(III)-ADP/NADPH and mitochondrial lipid peroxidation induced by Fe(III)-ADP/ NADH, it inhibits linoleic acid autoxidation but not generation of superoxide anion. | |||
T37972 |
12-OxoETE
|
Others | Others |
12-OxoETE is synthesized by human platelets and Aplysia nervous tissue after incubation with arachidonic acid. Microsomal fractions of various tissues will reduce 12-oxoETE to 12(S)-HETE or a mixture of 12(S)- and 12(R)-HETE. 12-OxoETE induces a rapid, dose dependent increase of cytoplasmic free calcium via a leukotriene B4 receptor or a common activation sequence. |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-01298 |
EPHX1 Protein, Human, Recombinant (His)
EPHX1,Microsomal epoxide hydrolase,Epoxide hydratas... |
Human | E. coli |
Biotransformation enzyme that catalyzes the hydrolysis of arene and aliphatic epoxides to less reactive and more water soluble dihydrodiols by the trans addition of water. Plays a role in the metabolism of endogenous lipids such as epoxide-containing fatty acids. Metabolizes the abundant endocannabinoid 2-arachidonoylglycerol (2-AG) to free arachidonic acid (AA) and glycerol. | |||
TMPJ-00723 |
CYB5A Protein, Human, Recombinant (His)
CYB5,Cytochrome b5,Microsomal Cytochrome b5 Type A,... |
Human | E. coli |
Cytochrome b5 (CYB5A) is a membrane bound hemoprotein which function as an electron carrier for several membrane bound oxygenases. CYB5A contains one cytochrome b5 heme-binding domain and has two isoforms produced by alternative splicing. Isoform 1 is a sngle-pass membrane protein. Isoform 2 is located in cytoplasm. The defects in CYB5A can result in type IV hereditary methemoglobinemia. | |||
TMPH-03099 |
Aminopeptidase N/CD13 Protein, Pig, Recombinant (His & Myc)
gp130,pAPN,AP-M,Aminopeptidase M,CD13,AP-N,Alanyl aminopepti... |
Sus scrofa (Pig) | E. coli |
Aminopeptidase N/CD13 Protein, Pig, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 47.1 kDa and the accession number is P15145. | |||
TMPH-02110 |
SEC11C Protein, Human, Recombinant (His & SUMO)
Microsomal signal peptidase 21 kDa subunit,SEC11-li... |
Human | E. coli |
Component of the microsomal signal peptidase complex which removes signal peptides from nascent proteins as they are translocated into the lumen of the endoplasmic reticulum. | |||
TMPY-02779 |
Thyroid peroxidase Protein, Human, Recombinant (S257A & P725T, His)
thyroid peroxidase,MSA,TPX,TDH2A |
Human | Baculovirus Insect Cells |
Thyroid peroxidase is a membrane-bound glycoprotein which belongs to the peroxidase family, XPO subfamily. It contains 1 EGF-like domain and 1 Sushi (CCP/SCR) domain. Thyroid Peroxidase represents one of the main autoantigenic targets in autoimmune thyroid disease of humans. It used to be taken as the formerly so-called `microsomal antigen` several years ago. As an integral membrane glycoprotein it is restricted to the apical plasma membrane of the follicular epithelial cells and comprises two i... |