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Cat. No. | Product Name | ||
---|---|---|---|
L9850 | 口服活性化合物库 | 2427 compounds | |
2427 种口服活性化合物独特集合,可用于高通量筛选和高内涵筛选 | |||
L2170 | 肿瘤免疫治疗小分子化合物库 | 449 compounds | |
449 种靶向肿瘤免疫治疗靶点的小分子,可用于高通量和高内涵筛选,是研究肿瘤免疫治疗的有力工具; | |||
DO1200 | 药物靶点库 | 53200 compounds | |
数量多,含53200种小分子化合物,是高通量筛选的有力工具; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2086 |
ELN-441958
ELN 441958 |
Bradykinin Receptor | GPCR/G Protein |
ELN-441958是一种B1受体拮抗剂,能够抑制B1激动剂配体[3H] DAKD 与IMR-90细胞结合(Ki:0.26 nM),相较于B2受体,它对B1受体的抑制作用具有更高的选择性,且比抑制μ阿片受体选择性高500多倍,比抑制δ阿片受体选择性高2000多倍。 | |||
T1770 |
GNE-9605
|
LRRK2 | Autophagy |
GNE-9605 是一个高效,选择性和能脑渗透的LRRK2抑制剂,IC50为19 nM。 | |||
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)。 | |||
T10606 |
BRD0705
|
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
BRD0705 是一种具有旁系选择性的、口服具有活性的GSK3α抑制剂,其 IC50=66 nM,Kd=4.8 μM。 它与 GSK3β (其 IC50=515 nM) 相比,对GSK3α的选择性更高 (8 倍)。它可用于研究急性髓细胞性白血病。 | |||
TQ0239 |
PF-06291874
Glucagon receptor antagonists-4 |
Glucagon Receptor | GPCR/G Protein |
PF-06291874 (Glucagon receptor antagonists-4) 是口服有活性的胰高血糖素受体非肽类拮抗剂。它正用于研究 2 型糖尿病。 | |||
T9173 |
HM-30181 mesylate monohydrate
|
P-gp | Membrane transporter/Ion channel; Neuroscience |
HM-30181 mesylate monohydrate 是一种口服 P-糖蛋白 (P-gp) 抑制剂,用于提高 P-gp 底物药物的口服生物利用度。 | |||
T7897 |
PK150
|
Others; Antibacterial | Microbiology/Virology; Others |
PK150 是一种 Sorafenib 类似物,具有抗菌活性。它抑制甲氧西林敏感金黄色葡萄球菌,耐甲氧西林金黄色葡萄球菌,万古霉素中介金黄色葡萄球菌的 MIC 分别为 0.3,0.3-1,0.3 µM。 | |||
T9692 |
Paltusotine
|
Somatostatin | GPCR/G Protein |
Paltusotine 是一种口服有效的,非肽选择性生长抑素 2 型受体激动剂。在长效生长抑素受体配体作用后,Paltusotine 仍可维持 GH 和 IGF-1 水平。 | |||
T7614 |
Eniluracil
GW776C85,5-Ethynyluracil |
Others | Others |
Eniluracil (GW776C85) 是不可逆的二氢嘧啶脱氢酶(DPD)抑制剂,是一种尿嘧啶类似物,能够使 5-FU 的口服生物利用度提高到 100%,促进均匀吸收和可预测的毒性。 | |||
T8850 |
sbp-7455
|
Autophagy | Autophagy |
SBP-7455 是一种高亲和力,可口服的双重ULK1/ULK2自噬抑制剂,可有效抑制ULK1/2酶活性,可研究三阴性乳腺癌,在 ADP-Glo 分析中的IC50分别为 13 nM 和 476 nM。 | |||
T15409 |
GNF179
|
Parasite | Microbiology/Virology |
GNF179 是8,8-二甲基 IP 类似物。 它表现出对多药耐药菌株 W2 的效力,具有良好的体外代谢稳定性和体内口服生物相容性。 | |||
TQ0039 |
(±)-Zanubrutinib
(±)-BGB-3111 |
BTK | Angiogenesis; Tyrosine Kinase/Adaptors |
(±)-Zanubrutinib ((±)-BGB-3111) 是一种有效的口服Bruton’s 酪氨酸激酶(Btk)抑制剂,具有优越的口服生物利用度,可实现更高的暴露量和更完整的靶点抑制。 | |||
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。 | |||
T3312 |
AM-2394
AM2394 |
Glucokinase | Metabolism |
AM-2394 是新型的 glucokinase 激活剂 (GKA)。它能够激活葡萄糖激酶 (GK),EC50=60 nM。 | |||
T60538 |
SARS-CoV-2-IN-14
3',5-Dichlorosalicylanilide |
SARS-CoV | Microbiology/Virology |
SARS-CoV-2-IN-14 是一种有效的、可口服的 SARS-CoV-2 抑制剂(IC50 :0.39 μM),是一种氯硝柳胺类似物。SARS-CoV-2-IN-14在人血浆和肝 S9 酶测定中比氯硝柳胺稳定性更强。SARS-CoV-2-IN-14以口服的方式给药可以提高其生物利用度和半衰期。 | |||
T26690 |
AVN-101
|
5-HT Receptor; Adrenergic Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
AVN-101 是一种非常有效的 5-HT7 受体拮抗剂 (Ki = 153 pM)。 AVN-101 还对组胺 H1 (Ki = 0.58 nM) 和肾上腺素能 α2A、α2B 和 α2C (Ki = 0.41-3.6 nM) 受体表现出相当高的亲和力。 AVN-101在中枢神经系统疾病动物模型中显示出良好的口服生物利用度和促进脑血屏障通透性、低毒性和合理的疗效。 | |||
T32005 |
GSK1842799
GSK 1842799 |
Others | Others |
GSK1842799 is a selective S1P1 receptor agonist with good oral bioavailability. | |||
T10448 |
Bacampicillin
|
Others | Others |
Bacampicillin is an improved oral bioavailability penicillin antibiotic which is a prodrug of ampicillin. | |||
T33763 |
NVP CXCR2 20
NVP-CXCR2 20,NVP CXCR2-20,NVP CXCR220 |
Others | Others |
NVP CXCR2 20 is an effective selective CXCR2 antagonist (IC50 = 40 nM) with oral bioavailability. | |||
T70166 |
Indinavir monohydrate
|
Others | Others |
Indinavir monohydrate is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability. | |||
T10448L |
Bacampicillin hydrochloride
|
Others | Others |
Bacampicillin hydrochloride is an improved oral bioavailability penicillin antibiotic which is a prodrug of ampicillin. | |||
T16755 |
RIPK-IN-4
|
TNF | Apoptosis |
RIPK-IN-4 is an effective and selective inhibitor of RIPK2. It also has excellent oral bioavailability (IC50: 3 nM). | |||
T14500 |
BAY-1316957
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
BAY-1316957 is a highly potent and selective EP4 receptor antagonist. With an IC50 of 15.3 nM. Good oral bioavailability[1]. | |||
T18652 |
RTC-30
|
Others | Others |
RTC-30 is an optimized phenothiazine compound possessing potent anti-cancer properties. It is formulated with a hydroxylated linker (N) which enhances its oral bioavailability[1]. | |||
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. | |||
T39935 |
TRPA1-IN-1
TRPA1-IN-1 |
Others | Others |
TRPA1-IN-1 is a potent, selective antagonist of the TRPA1 channel, demonstrating significant oral bioavailability as a small molecule. | |||
T70179 |
THIQ-40
|
Others | Others |
THIQ-40 is a novel potent erα antagonist and selective estrogen receptor degrader (serd), exhibiting good oral bioavailability, antitumor efficacy, and serd activity in vivo | |||
T84873 |
RS-127445 maleate
|
Others | Others |
RS-127445 maleate is a chemically selective antagonist with a high affinity for the 5-HT2B receptor, boasting an oral bioavailability and a pKi of 9.5. | |||
T38990 |
MGS0274
|
Others | Others |
MGS0274, an ester-based lipophilic prodrug of the metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, demonstrates enhanced oral bioavailability and holds promise for schizophrenia research applications. | |||
T38298 |
Tuberculosis inhibitor 3
|
Others | Others |
Tuberculosis inhibitor 3 (compound 2i) displays potent anti-TB activity (MIC < 0.016 μg/mL) against drug-sensitive/resistant MTB strains. Tuberculosis inhibitor 3 (compound 2i) shows acceptable PK profiles with oral bioavailability[1]. | |||
T29151 |
WAY267464 HCl
WAY267464,WAY-267464,WAY 267,464 dihydrochloride,WAY-267,464 dihydrochloride,WAY 267464 dihydrochloride,WAY 267464 |
Others | Others |
WAY267464 is a nonpeptide small-molecule OT agonists with anxiolytic activity. WAY267464 may be used for modulation of potency, selectivity over the structurally similar vasopressin receptors, CNS penetration, and oral bioavailability. | |||
T27374 |
FR-181877
FR181877,FR 181877 |
Others | Others |
FR-181877, a nonprostanoid PGI2 agonist, inhibits ADP-induced aggregation of human platelets with an IC50 value of 0.081 microM and has high oral bioavailability (56%) with a long half-life (4.3 h) in rats. | |||
T11445 |
GNF179 (Metabolite)
GNF179 Metabolite |
Others | Others |
GNF179 Metabolite, the derivative of GNF179—an optimized 8,8-dimethyl IP analog—demonstrates significant potency (4.8 nM against the multidrug-resistant W2 strain) alongside in vitro metabolic stability and in vivo oral bioavailability. | |||
T25234 |
CH5447240
CH 5447240,CH-5447240 |
Others | Others |
CH5447240 is an effective Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist for the treatment of Hypoparathyroidism. CH5447240 showed a potent in vitro hPTHR1 agonist effect (EC20: 3.0 nM; EC50: 12 nM). It showed 55% oral bioavailability and a signifi | |||
T61076 |
Vildagliptin dihydrate
|
Others | Others |
Vildagliptin dihydrate (LAF237 dihydrate) is a powerful and stable dipeptidyl peptidase IV (DPP-IV) inhibitor, demonstrating selectivity with an IC50 of 3.5 nM in human Caco-2 cells. This compound exhibits exceptional oral bioavailability and significant antihyperglycemic activity [1]. | |||
T61637 |
Anti-inflammatory agent 8
|
Others | Others |
Anti-inflammatory agent 8 (compound 13) designated as an anti-inflammatory agent 8, displays enhanced activity on the COX-2 enzyme compared to COX-1, with an IC50 value of 0.09 nM. Furthermore, anti-inflammatory agent 8 exhibits oral bioavailability [1]. | |||
T74167 |
PCSK9-IN-3
|
Others | Others |
PCSK9-IN-3为新一代口服高效三环肽类PCSK9抑制剂,特征为新型化合物。 | |||
T70420 |
PHA 543613 hydrochloride
|
Others | Others |
PHA-543613 hydrochloride acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia. | |||
T68568 |
Encequidar, HCl
|
Others | Others |
Encequidar, also known as HM-30181, is an oral P-glycoprotein (P-gp) inhibitor developed to enhance the oral bioavailability of P-gp substrate drugs. Encequidar showed the highest potency (IC(50)=0.63nM) among several MDR1 inhibitors, including cycloporin A, XR9576, and GF120918, and effectively blocked transepithelial transport of paclitaxel in MDCK monolayers (IC(50)=35.4nM). Encequidar is currently under clinical trials. | |||
T30491 |
BMS 183920
BMS-183920,BMS183920 |
Others | Others |
BMS-183920 is a diacid, potent angiotensin II receptor antagonist that improves Caco-2 cell permeability and in vivo oral absorption. The relative degree of hydrolysis (biological activation) and prodrug metabolism determines whether substantial improveme | |||
T27786 |
L-796568 dihydrochloride
L 796568,L-796568,L796568 |
Others | Others |
L-796568, is a β3 adrenergic receptor agonist. L-796568 is a potent full beta(3) agonist (EC(50) = 3.6 nM, 94% activation) with >600-fold selectivity over the human beta(1) and beta(2) receptors, which also displays good oral bioavailability in several | |||
T61357 |
EP3 antagonist 3
|
Others | Others |
EP3 antagonist 3 (compound 2) is a highly effective and specific antagonist of the EP3 receptor. It displays significant oral bioavailability and exhibits a strong pKi value of 8.3. Furthermore, EP3 antagonist 3 possesses excellent pharmacokinetic characteristics, making it a suitable candidate for experimental investigations involving overactive bladder (OAB) research [1]. | |||
T61400 |
Anti-inflammatory agent 9
|
Others | Others |
Anti-inflammatory agent 9 (compound 28)Anti-inflammatory agent 9 (compound 28) is a benzimidazothiazole derivative derived from tilomisole. It exhibits a higher affinity for the COX-2 enzyme compared to COX-1, thereby demonstrating promising anti-inflammatory properties. Furthermore, it demonstrates oral bioavailability [1]. | |||
T40248 |
JNK3 inhibitor-1
JNK3 inhibitor-1 |
Others | Others |
JNK3 inhibitor-1 is a highly potent and selective compound that specifically inhibits JNK3 with an impressive IC50 value of 0.005 μM. In addition to its remarkable inhibitory effects, JNK3 inhibitor-1 possesses excellent oral bioavailability and the ability to efficiently penetrate the brain. | |||
T61480 |
NHE3-IN-3
|
Others | Others |
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]. | |||
T8795 |
met-kinase-in-2
1,6-Naphthyridin-4(1H)-one, 5-[[3-fluoro-4-[[7-(2-hydroxy-2-methylpropoxy)-4-quinolinyl]oxy]phenyl]amino]-3-phenyl- |
Others | Others |
MET kinase-IN-2 是一种有效的选择性的,具有口服活性的 MET 激酶抑制剂,IC50 值为 7.4 nM。MET kinase-IN-2 具有抗肿瘤活性。 | |||
T3430L |
(Rac)-PF-4136309(1341224-83-6 Free base)
PF-04136309,INCB8761 |
Others | Others |
PF-4136309(INCB8761, PF-04136309)是一种高效、选择性的口服 CCR2 拮抗剂,具有良好的生物可利用性,其对人CCR2的IC50值为5.2 nM。 | |||
T70951 |
ELND006
|
Others | Others |
ELND006 is a novel gamma secretase inhibitor previously under investigation for the oral treatment of Alzheimer's disease. ELND006 shows poor solubility and has moderate to high permeability. The in vivo performance of the ELND006 nanosuspension was tested in fed and fasted beagle dogs and compared with a gelatin capsule containing reference API. The results show that nanosizing ELND006 profoundly improved the oral bioavailability and virtually eliminated variation resulting from food intake. | |||
T82193 |
HJM-561
|
PROTACs | PROTAC |
HJM-561为一种有效的选择性口服生物可利用EGFRPROTAC,能够克服osimertinib耐药的EGFR三重突变,并表现出抗肿瘤活性。 | |||
T78744 |
IRAK4-IN-24
|
IRAK | Immunology/Inflammation; NF-κB |
IRAK4-IN-24(compound 16)是IRAK4高效抑制剂,显示高Cl及较低口服生物可用性,适用于炎症与自身免疫性疾病研究。 |