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Cat. No. | Product Name | ||
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L5100 | 含氟化合物库 | 574 compounds | |
574 个含氟化合物的独特集合,可用于高通量筛选和高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1803 |
GNF-5
GNF 5 |
SARS-CoV; Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors |
GNF-5是 Bcr-Abl 的特异性非 ATP 竞争性抑制剂,IC50为0.22uM。它是 GNF-2 的类似物,具有改进的药代动力学特性。 | |||
T13099 |
TC ASK 10
|
ASK; MAPK | Apoptosis; MAPK |
TC ASK 10 是选择性的,口服有效的细胞凋亡信号调节激酶 1 抑制剂,IC50为 14 nM。它对其他代表性激酶的抑制活性低于 50%,除 ASK2之外 (IC50为 0.51 μM)。 | |||
T4989 |
Fosfomycin Tromethamine
|
Antibacterial; Antibiotic | Microbiology/Virology |
Fosfomycin tromethamine 是一种能透过血脑屏障的广谱抗生素,不可逆地抑制细胞壁合成的早期阶段。它对多种细菌具有杀菌活性,包括耐多药、广泛耐药和耐全药细菌。 | |||
T2397 |
Topiroxostat
托匹司他,FYX-051 |
P450; ROS; Xanthine Oxidase | Immunology/Inflammation; Metabolism |
Topiroxostat (FYX-051) 是一种有效的口服黄嘌呤氧化还原酶 (XOR) 抑制剂,IC50=5.3 nM,Ki=5.7 nM。它还表现出弱的CYP3A4抑制活性 (18.6%)。它有用于高尿酸血症的研究潜力。 | |||
T3131 |
Fosfomycin calcium
Phosphomycin calcium salt,Fosmicin,磷霉素钙 |
Antibacterial; Antibiotic | Microbiology/Virology |
Fosfomycin calcium (Phosphomycin calcium salt) 是一种能透过血脑屏障的广谱抗生素,不可逆地抑制细胞壁合成的早期阶段。它对多种细菌具有杀菌活性,包括耐多药、广泛耐药和耐全药细菌。 | |||
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。 | |||
T19858 |
Brodimoprim
|
DHFR; Antibacterial | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology |
Brodimoprim 是甲氧苄啶的一种类似物,是口服有效的二氢叶酸还原酶抑制剂,对广谱革兰氏阴性和革兰氏阳性细菌具有高度的抑制作用。 | |||
T37082 |
HS271
|
IRAK | Immunology/Inflammation; NF-κB |
HS271 是一个选择性的、口服有效的 IRAK4 抑制剂 (IC50= 7.2 μM)。HS271 表现出优越的体外酶活性和细胞活性以及药代动力学特征。 | |||
T26252 |
PI3Kδ-IN-3
TC KHNS 11 |
PI3K | PI3K/Akt/mTOR signaling |
PI3Kδ-IN-3 (TC KHNS 11) 是一种 PI3Kδ 抑制剂,IC50 值为 9 nM。PI3Kδ-IN-3 具有良好的药代动力学特性且对 B 细胞功能有抑制作用。 | |||
T22338 |
2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
GDC046 |
Others; JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Others; Stem Cells |
2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide (GDC046) 是一种具有口服活性的选择性TYK2抑制剂,对 TYK2、JAK1、JAK2 和 JAK3 的Ki 分别为 4.8、0.7、0.7 和 0.4 nM。 | |||
T26969 |
CCT365623
CCT-365623,CCT 365623 |
Monoamine Oxidase | Neuroscience |
CCT365623 是一种口服生物可利用的赖氨酰氧化酶抑制剂,具有良好的抗 LOX 效力、选择性、药代动力学特性以及抗转移功效。 | |||
T26863 |
BMS-929075
BMS 929075,BMS929075 |
HCV Protease | Microbiology/Virology; Proteases/Proteasome |
BMS-929075是一种具有口服活性 HCV NS5B 复制酶 (HCV NS5B replicase) 手掌位点变构抑制剂,具有有效性、 较高的口服生物利用度和药代动力学参数 。BMS-929075 显示出细胞毒性。 | |||
T16679 |
Belzutifan
PT2977,MK-6482 |
HIF | Angiogenesis; Chromatin/Epigenetic |
Belzutifan (MK-6482) 是具有口服活性的 HIF-2α选择性抑制剂,IC50为 9 nM。Belzutifan 具有提高的效力和改善的药代动力学特征。Belzutifan (MK-6482) 可以抑制透明细胞肾细胞癌。 | |||
T6100 |
Torin 2
|
Apoptosis; ATM/ATR; DNA-PK; mTOR; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Torin 2 是一种特异性 mTOR 抑制剂,IC50值为0.25 nM,并改善了药代动力学特性。它抑制 ATM/ATR/DNA-PK 的 EC50 分别为 28 nM/35 nM/118 nM。 | |||
T9642 |
ZW4864 free base
|
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
ZW4864 free base 是口服有效的,选择性的 β catenin/ B-Cell lymphoma 9 蛋白-蛋白相互作用 (β catenin/BCL9 PPI) 抑制剂 (Ki= 0.76 μM, IC50= 0.87 μM)。 | |||
T63208 |
Aβ-IN-1
|
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Aβ-IN-1 是一种新型有效且具有口服活性的 γ 分泌酶调节剂 (GSM)。 Aβ-IN-1 在不抑制 CYP3A4 的情况下,在培养细胞中有效降低 Aβ42 水平,IC50值为 0.091 μM。Aβ-IN-1 显示出良好的药代动力学特征。 | |||
T64355 |
TDI-10229
|
cAMP | GPCR/G Protein |
TDI-10229 是一种口服有效的可溶性腺苷酸环化酶 (sAC, ADCY10) 抑制剂 (IC50 值为 195 nM)。TDI-10229 在生化和细胞分析中都显示出对 sAC 的纳摩尔级抑制,并表现出足以保证其用作体内工具化合物的小鼠药代动力学特性。 | |||
T73593 |
PDS-0330
|
Others | Others |
PDS-0330是一种 claudin-1小分子抑制剂抑制。PDS-0330抑制 claudin-1依赖性 CRC 进展,以微摩尔亲和力直接和特异性地与claudin-1结合。PDS-0330通过抑制与转移性癌基因Src 的关联,表现出具有良好药代动力学特性的抗肿瘤和化学增敏活性。PDS-0330干扰claudin-1 / Src 关联以抑制CRC 进展和转移。 | |||
T14835 |
BTRX-335140
CYM-53093 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
BTRX-335140 (CYM-53093) 是一种有效的选择性口服活性 κ 阿片受体 (KOR) 拮抗剂,对 κOR、μOR 和 δOR 具有拮抗活性,IC50 值分别为 0.8、110 和 6500 nM。它可以很好地分布到 CNS 中,在大鼠中具有良好的体外吸收、分布、代谢、排泄和毒性以及体内药代动力学特征。 | |||
T21537L |
TMC647055 Choline Hydroxide Salt
TMC647055 Choline Hydroxide Salt (1204416-97-6 free base) |
HCV Protease | Microbiology/Virology; Proteases/Proteasome |
TMC647055 Choline Hydroxide Salt 是一种新型有效的 HCV NS5B 聚合酶非核苷抑制剂,可用于治疗 HCV 感染。它具有纳摩尔级细胞效力(EC(50) 为 82 nM),相关细胞毒性较小(CC(50)>20 μM),在大鼠和狗中具有良好的药代动力学特征。 TMC647055 显示出有体外生化、动力学和病毒学特征的前景。 | |||
T33442 |
MK-8718
MK 8718 |
Others | Others |
MK-8718 is an HIV protease inhibitor with a selective orally bioavailable inhibitor with good pharmacokinetic characteristics. | |||
T30303 |
BAY8040
BAY 8040,BAY-8040 |
Others | Others |
BAY8040 is a potent selective human neutrophilic elastase inhibitor with excellent potency and selectivity with promising pharmacokinetic characteristics. | |||
T32006 |
GSK-2262167 sodium
GSK-2262167,GSK2262167,GSK 2262167 |
Others | Others |
GSK-2262167 is a potent S1P1 agonist, as effective as fingolimod in collagen-induced arthritis models, and shows good preclinical pharmacokinetic properties. | |||
T70033 |
NCATS-SM1440
|
Others | Others |
NCATS-SM1440 is a Lactate Dehydrogenase Inhibitor with Optimized Cell Activity and Pharmacokinetic Properties. | |||
T12795 |
(S)-Ceralasertib
(S)-AZD6738 |
Others | Others |
(S)-Ceralasertib is a potent and selective inhibitor of sulfoximine morpholinopyrimidine ATR with excellent preclinical physicochemical and pharmacokinetic (PK) characteristics. . | |||
T40238 |
Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium
Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium |
Others | Others |
Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) displays a prolonged half-life (t1/2) compared to tenofovir in human liver microsomes. Moreover, it demonstrates potent in vitro anti-HIV activity and improves in vivo pharmacokinetic properties. | |||
T35852 |
FAPI-34
|
Others | Others |
FAPI-34, a fibroblast-activating protein (FAP) inhibitor, boasts advantageous pharmacokinetic and biochemical attributes. | |||
T24366 |
L 870810
L-870,810,L870810,L 870,810,L870,810,L-870810 |
Others | Others |
L 870810 is a small-molecule inhibitor of HIV-1 integrase with potent antiviral activity in cell culture and good pharmacokinetic properties. | |||
T26309 |
Umirolimus
Biolimus-A9,TRM-986,TRM 986,TRM986,Biolimus A9 |
Others | Others |
Umirolimus is a sirolimus derivative from a biodegradable polylactic acid polymer. It has enhanced anti-inflammatory and antiproliferative activity with an improved pharmacokinetic profile. | |||
T68826 |
A33903
|
Others | Others |
A33903 is a 1,4-benzodiazepine analog that is being studied as a potential inhibitor of respiratory syncytial virus. This molecule was moderately active and demonstrated good pharmacokinetic properties. | |||
T40092 |
MNK/PIM-IN-1
|
Others | Others |
MNK/PIM-IN-1 is a novel dual inhibitor targeting both MNK and PIM pathways, characterized by its favorable pharmacokinetic profile. | |||
T40280 |
JH-XVI-178
|
Others | Others |
JH-XVI-178 is a highly potent and selective CDK8/19 inhibitor with favorable pharmacokinetic attributes, including low clearance and moderate oral bioavailability. | |||
T11377 |
GDC-0276
|
Others | Others |
GDC-0276, a potent, selective, reversible, and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM, offers potential for pain treatment while overcoming limitations associated with current pain medications, including addiction and off-target side effects. It is well tolerated and demonstrates a favorable pharmacokinetic profile. | |||
T38135 |
3,4-Dehydro Cilostazol
|
Others | Others |
3,4-Dehydro Cilostazol (OPC-13015) is an active metabolite of Cilostazol. 3,4-Dehydro Cilostazol is used for pharmacokinetic study[1]. [1]. T R S Satheeshmanikandan, et al. Liquid Chromatography - Tandem Mass Spectrometry for the Simultaneous Quantitation of Glipizide, Cilostazol and Its Active Metabolite 3, 4-dehydro-cilostazol in Rat Plasma: Application for a Pharmacokinetic Study. Arzneimittelforschung. 2012 Sep;62(9):425-32. | |||
T23807 |
BMS-955176 TFA
BMS 955176,GSK-3532795,BMS955176,BMS-955176,GSK3532795 |
Others | Others |
GSK3532795 is an orally active inhibitor of HIV-1 maturation. GSK3532795 combines broad coverage of polymorphic viruses (EC50: 15 nM toward a panel of common polymorphisms representative of 96.5% HIV-1 subtype B virus) with a favorable pharmacokinetic pro | |||
T40239 |
Tenofovir-C3-O-C15-CF3 ammonium
Tenofovir-C3-O-C15-CF3 ammonium |
Others | Others |
Tenofovir-C3-O-C15-CF3 (ammonium) demonstrates prolonged half-life values compared to tenofovir in human liver microsomes. It exhibits potent anti-HIV activity in vitro and enhances pharmacokinetic properties in vivo. | |||
T11548L |
HCV-IN-7 hydrochloride
|
Others | Others |
HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor (IC50s: 3-47 pM). It shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. | |||
T11548 |
HCV-IN-7
|
Others | Others |
HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor (IC50s: 3-47 pM). It shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. | |||
T25558 |
JNJ-55511118
JNJ 55511118 |
Others | Others |
JNJ-55511118 is a selective negative modulator of AMPA receptors containing TARP-γ8 (Ki: 26 nM). It had excellent pharmacokinetic properties. JNJ-55511118 exhibited a dose-dependent inhibition of neurotransmission within the hippocampus and a strong antic | |||
T68356 |
AM-3189
|
Others | Others |
AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. Similar to AMG 837, while highly potent on GPR40, AM-3189 was highly selective over the closely related GPCRs, GPR41 and GPR43. 13kdemonstrated low clearance, moderate volume of distribution, and good oral bioavai... | |||
T11972 |
Mcl-1 inhibitor 3
|
BCL | Apoptosis |
Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.Mcl-1 inhibitor 3 is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay). | |||
T69762 |
ZL0513
|
Others | Others |
ZL0513 is a chromone derivatives used as orally bioavailable BRD4-selective inhibitor. This BRD4 BD1 inhibitor has demonstrated impressive in vivo efficacy and overall promising pharmacokinetic properties, indicating its therapeutic potential for the treatment of inflammatory diseases. | |||
T14555 |
BI-1230
|
HCV Protease | Microbiology/Virology; Proteases/Proteasome |
BI-1230 is a potent inhibitor of HCV NS3 protease, exhibiting efficacy in the low nanomolar range, and notably suppresses viral replication. This compound demonstrates high selectivity, distinguishing effectively between other serine/cysteine proteases. Additionally, BI-1230 exhibits favorable pharmacokinetic (PK) properties[1]. | |||
T34767 |
TA-1887
TA 1887,TA1887 |
Others | Others |
TA-1887 is a new type of selective inhibitor of sglt2 for the treatment of type 2 diabetes. It has a significant hypoglycemic effect in KK (HF-KK) mice fed a high-fat diet. TA-1887 has good pharmacokinetic characteristics and significantly increases UGE | |||
T69761 |
ZL0516
|
Others | Others |
ZL0516 is a is a chromone derivatives used as orally bioavailable BRD4-selective inhibitor. This BRD4 BD1 inhibitor has demonstrated impressive in vivo efficacy and overall promising pharmacokinetic properties, indicating its therapeutic potential for the treatment of inflammatory diseases. | |||
T70754 |
NMS-P953
|
Others | Others |
NMS-P953 is a JAK2 inhibitor, displaying significant tumor growth inhibition in SET-2 xenograft tumor model. NMS-P953 has a mechanism of action confirmed in vivo by typical modulation of known biomarkers, and with a favorable pharmacokinetic and safety profile. | |||
T71653 |
GS-9256
|
HCV Protease | Microbiology/Virology; Proteases/Proteasome |
GS-9256为选择性HCV NS3蛋白酶抑制剂,展现出优良的药代动力学特性及抗病毒活性。 | |||
T68345 |
GTS511
|
Others | Others |
GTS511 is a EAAT2 Activator. Pharmacokinetic profiles (PK) of GTS511 show a >6 h half-life and higher bioavailability in plasma and the brain under all three routes of administration in rats. GTS511 can be further developed to treat neurological disorders caused by excitotoxicity | |||
T69776 |
BAY-707 acetate
|
Others | Others |
BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1. Despite superior cellular target engagement and pharmacokinetic properties, inhibition of MTH1 with BAY-707 resulted in a clear lack of in vitro or in vivo anticancer efficacy either in mono- or in combination therapies. | |||
T78189 |
JAK-IN-26
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK-IN-26(化合物2)为口服活性JAK抑制剂,展现优良药代动力学特性。该化合物有效抑制Jurkat细胞中IFN-α2B诱导的STAT3磷酸化(IC50=17.2 nM)。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8262 |
Fosfomycin sodium
Fosfomycin Disodium,磷霉素钠 |
Antibacterial; Antibiotic | Microbiology/Virology |
Fosfomycin sodium 是一种能透过血脑屏障的广谱抗生素,不可逆地抑制细胞壁合成的早期阶段。它对多种细菌具有杀菌活性,包括耐多药、广泛耐药和耐全药的细菌。 | |||
TN1048 |
Cnidilin
Knidilin |
||
Cnidilin (Knidilin) 存在与Angelica dahurica 根中,具有高BBB 通透性,在治疗中枢神经系统疾病方面具有药代动力学潜力。 | |||
TN4992 |
Senkyunolide G
|
Others | Others |
Senkyunolide G and senkyunolide I could serve as pharmacokinetic markers for sepsis care. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T27982 |
MBRI-001
MBRI 001,MBRI001. BPI-2358-d,plinabulin-d,NPI-2358-d |
||
MBRI-001 is a deuterium-substituted plinabulin derivative and a potent anti-cancer agent with better pharmacokinetic characteristics tand lower toxicity. |