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Cat. No. Product Name Target Signaling Pathways
T9192 BIIB068

BTK Angiogenesis; Tyrosine Kinase/Adaptors
BIIB068 是可逆的、选择性的、具有口服活性的 BTK 抑制剂 (IC50:1 nM;Kd:0.3 nM)。它对 BTK 的选择性比其他激酶高 400 倍。它可用于自身免疫性疾病的研究。
T9054 RO6889678

HBV Microbiology/Virology
RO6889678 是高效的 HBV 衣壳结构抑制剂,其吸收、分布、代谢和排泄特征较为复杂。它可通过 CYP3A4 介导的氧化作用进行代谢,以及通过 UDP-葡萄糖醛酸基转移酶 UGT1A3 和 UGT1A1 介导的直接葡萄糖醛酸化作用进行代谢。它是一种诱导剂,可作用于人肝细胞中 CYP3A4 和共调节蛋白。
TQ0008 MT-DADMe-ImmA

Methylthio-DADMe-Immucillin A,MTDIA

Others Others
MT-DADMe-ImmA (MTDIA) 是一种人5'-甲硫基腺苷磷酸化酶的抑制剂 (MTAP)(Ki:90 pM)。
T2249 XEN445

XEN 445,XEN-445,2-[(3S)-3-(2-吡啶基甲氧基)-1-吡咯烷基]-5-(三氟甲基)苯甲酸

Lipase Metabolism
XEN445 是一种内皮脂肪酶抑制剂(IC50:0.237 uM),具有显著的ADME 和PK 活性,可以增强小鼠血浆中高密度脂蛋白胆固醇浓度。
T9643 ZN-c3

Wee1 Cell Cycle/Checkpoint
ZN-c3 是一种有效的选择性 Wee1 抑制剂,具有平衡的效力、ADME 和药代动力学特性。
T4347 ML355

Lipoxygenase Metabolism
ML355 是一种高选择性12-LOX 抑制剂,IC50=0.34 μM,对其他脂氧化酶和环氧化酶有很好的选择性,具有较好的药物动力学特征。
T24480 MK-8325

MK 8325,MK8325

HCV Protease Microbiology/Virology; Proteases/Proteasome
MK-8325是一种有效且可口服的HCV NS5A 抑制剂,对多种基因型具有复制活性。MK-8325在体外和体内试验显示生物利用度且具有良好的总体ADME 特征。
T31982 GNE-9822

GNE 9822

GNE-9822 is a potent selective ITK inhibitor that shows favorable ADME properties in preclinical species.
T24101 GR-125487

GR125487,GR 125487

GR-125487 is a 5-HT4R partial agonist. It also has favorable ADME properties and good in vivo efficacy.
T60761 PF-06305591 dihydrate

PF-06305591 dihydrate 是具有出色的临床前体外 ADME 和安全性的,电压门控钠通道 NaV1.8的高选择性阻断剂 (IC50 = 15 nM)。
T81881 MAGL-IN-10

MAGL Metabolism
MAGL-IN-10为一种可逆MAGL抑制剂,展现出优良的ADME特性且体内毒性低。该化合物适用于癌症、神经系统疾病和炎症病理学研究。
T63167 Antitrypanosomal agent 7

Antitrypanosomal agent 7 (compound 18c) 是一种有效的抗锥体虫剂,显示出良好的 ADME 特性。Antitrypanosomal agent 7 的抗布氏锥虫 (T. brucei) 的活性 (IC50: 0.71 μM),比 Nifurtimox 高两倍以上。Antitrypanosomal agent 7 与 DNA 有很强的相互作用,且能够选择性结合富含 AT 碱基的 DNA。
T62710 Antitrypanosomal agent 6

Antitrypanosomal agent 6 (compound 18a) 是一种有效的抗锥体虫剂,表现出良好的 ADME 特性。Antitrypanosomal agent 6 抗布氏锥虫 (T. brucei) 的活性比 Nifurtimox 高两倍以上,IC50为 0.47 μM。Antitrypanosomal agent 6 与 DNA 具有很强的相互作用,可以选择性的结合富含 AT 碱基的 DNA。
T71069 GSK1842799 HCl

GSK1842799 is a selective S1P1 receptor agonist for multiple sclerosis. Upon phosphorylation, GSK1842799 showed subnanomole S1P1 agonist activity with >1000× selectivity over S1P3. GSK1842799 demonstrated good oral bioavailability. On the basis of the favorable in vitro ADME and in vivo PK/PD properties as well as broad toxicology evaluations, GSK1842799 was selected as a candidate for further clinical.
T77254 Maltodextrin, dextrose equivalent 16.5-19.5

Maltodextrin(麦芽糊精),dextrose equivalent(葡萄糖当量)为16.5-19.5,可作为药用辅料。药用辅料,亦称药用助剂,非药物成分的化学物质,用于辅助药物制剂过程。此类辅料提升药物制剂的稳定性、溶解性及加工性,同时影响药物的吸收、分布、代谢及排泄(ADME)过程。
T70005 LY3325656

LY3325656 is a GPR142 agonist suitable for clinical testing in human. LY3325656 demonstrated anti-diabetic benefits in pre-clinical studies and ADME/PK properties suitable for human dosing. LY3325656 is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.
T16490 PF-06380101

Auristatin-0101,Aur0101

Others Others
PF-06380101 is an auristatin microtubule inhibitor and is a cytotoxic Dolastatin 10 analogue. When compared to other synthetic auristatin analogues that are used in the preparation of ADCs, PF-06380101 displays excellent potencies in tumor cell proliferat
T75329 Cellulose

Cellulose 可用作药用辅料。药用辅料或药用助剂,是指制药过程中使用的除药物成分以外的其他化学物质。药用辅料一般是指药物制剂中的非活性成分,能提高药物制剂的稳定性、溶解性和加工性。药用辅料还会影响合并用药的吸收、分布、代谢和消除 (ADME) 过程。
T79447 IRAK4-IN-25

IRAK Immunology/Inflammation; NF-κB
IRAK4-IN-25(化合物38)是口服活性IRAK4抑制剂,具有低清除率(Cl=12 mL/min/kg)和IC50值为7.3 nM。它能抑制促炎细胞因子产生,表现出良好的体外安全性和ADME特性。IRAK4-IN-25主要用于研究炎症和自身免疫性疾病。
T79316 Antitrypanosomal agent 15

Proteasome Proteases/Proteasome; Ubiquitination
Antitrypanosomal agent 15 (compound 26) 是一种具有口服活性、能穿透血脑屏障、对克氏锥虫蛋白酶体具有高选择性的抑制剂,其对克氏锥虫蛋白酶体的pIC50值为7.4,而对人蛋白酶体的pIC50值小于4。该化合物展现出良好的ADME性质,适合用于恰加斯病研究。
T70782 PF-05139962

PF-05139962 is a novel potent mTOR inhibitor with excellent mTOR biochemical inhibition, cellular potency, kinase selectivity and in vitro ADME properties. PF-05139962 has pS473 and pS6 cellular IC50 = 48 and 6 nM respectively. PF-05139962 has great selectivity against other receptors and kinases. No genotoxicity was observed on this compound and no more than 25% inhibiton was observed for major CYP enzymes (3A4, 1A2, 2C9, 2D6) at 3 uM. This compound has LE = 0.35 and LipE up to 6.8 which is in ...
T72999 PF-06455943

PF-06455943, 作为一种LRRK2 (富含亮氨酸的重复激酶 2) 抑制剂,具有3 nM的IC50值,主要用于帕金森病(PD)的研究。
T69686 BMS-986318

BMS-986318 是一种有效的非胆汁酸FXR 激动剂,在FXRGal4 和 SRC-1 募集试验中的EC50分别为 53 和 350 nM。 BMS-986318 具有合适的 ADME 特性,并在肝胆汁淤积和纤维化的小鼠胆管结扎模型中具有效果。BMS-986318 可用于非酒精性脂肪性肝炎 (NASH)的研究。
T77228 Polyoxyethylene Sorbitan Monostearate

Polyoxyethylene Sorbitan Monostearate 是一种由饱和脂肪酸硬脂酸 (C18:0) 构成的酯,广泛应用作药用辅料,包括表面活性剂、乳化剂、增溶剂和润湿剂。作为药用助剂,其主要作用是改善药物制剂的稳定性、溶解性和加工性,同时对药物的吸收、分布、代谢和消除 (ADME) 过程具有影响。
T70391 AMG151 HCl

ARRY-403, also known as AMG-151, is an orally available allosteric glucokinase (GK) activator developed for the treatment of type 2 diabetes mellitus (T2DM). ARRY-403 has many favorable physicochemical characteristics and ADME properties (low potential to cause drug–drug interactions (DDIs). ARRY-403 potently activates human glucokinase (GK) in vitro (EC50 = 79 nM at 5 mM glucose), with an S0.5 = 0.93 mM glucose (ARRY-403 at 5 mM) and Vmax = 134% compared to the no activator control. It possesse...
T73620 Poly(acrylic acid)

Poly(acrylic acid) 通过吸附作用在金属表面形成保护层,有效抑制纯铸铝在酸性介质中的腐蚀现象。此外,Poly(acrylic acid) 还可作为药物制剂中的包衣材料、释放阻断剂等药用辅料使用。药用辅料,亦称药用助剂,是指在制药过程中,除药物活性成分外使用的其他化学物质。这些辅料通常作为非活性成分加入药物制剂中,旨在提升制剂的稳定性、溶解性及加工性。同时,药用辅料对药物的吸收、分布、代谢与排泄(ADME)过程也具有一定影响。
T71933 GNE-3500

GNE-3500 is a Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C (RORc or RORγ) Inverse Agonist. Retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) is a nuclear receptor that plays a major role in the production of interleukin (IL)-17. Considerable efforts have been directed toward the discovery of selective RORc inverse agonists as potential treatments of inflammatory diseases such as psoriasis and rheumatoid arthritis. GNE-3500 poss...

化合物

BIIB068
Cat.No: T9192
Synonym:
Target: BTK
RO6889678
Cat.No: T9054
Synonym:
Target: HBV
MT-DADMe-ImmA
Cat.No: TQ0008
Synonym: Methylthio-DADMe-Immucillin A,MTDIA
Target: Others
XEN445
Cat.No: T2249
Synonym: XEN 445,XEN-445,2-[(3S)-3-(2-吡啶基甲氧基)-1-吡咯烷基]-5-(三氟甲基)苯甲酸
Target: Lipase
ZN-c3
Cat.No: T9643
Synonym:
Target: Wee1
ML355
Cat.No: T4347
Synonym:
Target: Lipoxygenase
MK-8325
Cat.No: T24480
Synonym: MK 8325,MK8325
Target: HCV Protease
GNE-9822
Cat.No: T31982
Synonym: GNE 9822
Target:
GR-125487
Cat.No: T24101
Synonym: GR125487,GR 125487
Target:
PF-06305591 dihydrate
Cat.No: T60761
Synonym:
Target:
MAGL-IN-10
Cat.No: T81881
Synonym:
Target: MAGL
Antitrypanosomal agent 7
Cat.No: T63167
Synonym:
Target:
Antitrypanosomal agent 6
Cat.No: T62710
Synonym:
Target:
GSK1842799 HCl
Cat.No: T71069
Synonym:
Target:
Maltodextrin, dextrose equivalent 16.5-19.5
Cat.No: T77254
Synonym:
Target:
LY3325656
Cat.No: T70005
Synonym:
Target:
PF-06380101
Cat.No: T16490
Synonym: Auristatin-0101,Aur0101
Target: Others
Cellulose
Cat.No: T75329
Synonym:
Target:
IRAK4-IN-25
Cat.No: T79447
Synonym:
Target: IRAK
Antitrypanosomal agent 15
Cat.No: T79316
Synonym:
Target: Proteasome
PF-05139962
Cat.No: T70782
Synonym:
Target:
PF-06455943
Cat.No: T72999
Synonym:
Target:
BMS-986318
Cat.No: T69686
Synonym:
Target:
Polyoxyethylene Sorbitan Monostearate
Cat.No: T77228
Synonym:
Target:
AMG151 HCl
Cat.No: T70391
Synonym:
Target:
Poly(acrylic acid)
Cat.No: T73620
Synonym:
Target:
GNE-3500
Cat.No: T71933
Synonym:
Target:
TargetMol Loading
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