Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T0343 |
Nimodipine
尼莫地平,BAY-e 9736 |
Glucocorticoid Receptor; AhR; Calcium Channel; Autophagy | Autophagy; Endocrinology/Hormones; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism |
Nimodipine (BAY-e 9736) 是一种具有口服活性,耐受性良好的光敏二氢吡啶钙拮抗剂。它可研究脑血管疾病。 | |||
T15549 |
Icosabutate
|
Others | Others |
Icosabutate is a structurally engineered and orally active ω-3 polyunsaturated fatty acid. Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia. | |||
T67805 |
Oxepinac
|
||
oxepinac 是一种治疗疼痛性骨关节炎的有效且耐受性良好的化合物。oxepinac 在动物实验中对小鼠和家兔胎儿无致畸作用。 | |||
T0217 |
Levodropropizine
(S)-(-)-Dropropizine,左羟丙哌嗪,DF-526 |
5-HT Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Levodropropizine ((S)-(-)-Dropropizine) 是一种组胺受体抑制剂,可用作外周镇咳药。 | |||
T9186 |
Ervogastat
PF-06865571 |
Transferase | Metabolism |
Ervogastat (PF-06865571) 是一种有效且耐受性良好的二酰基甘油酰基转移酶 2 抑制剂。 Ervogastat 可降低非酒精性脂肪性肝炎 (NASH) 中的脂肪变性和肝脏甘油三酯水平。 | |||
T22349 |
JNJ-38158471
CS-2660 |
VEGFR; c-RET; c-Kit | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
JNJ-38158471 (CS-2660) 是一种耐受性好的,有口服活性的、高效的、选择性的 VEGFR-2抑制剂 (IC50:40 nM),还能抑制 Ret (IC50:180 nM) 和 Kit (IC50:500 nM)。 | |||
T1458 |
Epalrestat
ONO2235,依帕斯他,依帕司他 |
Reductase | Endocrinology/Hormones; Metabolism |
Epalrestat (ONO2235) 是醛糖还原酶抑制剂,在长期治疗中具有良好的耐受性。 它可以有效改善糖尿病神经病变的相关症状并延缓疾病的进展,特别是在微血管病变有限且血糖控制良好的患者中。 | |||
T10896L |
CSRM617 hydrochloride
CSRM617 hydrochloride(787504-88-5 Free base) |
Apoptosis; Others; Androgen Receptor | Apoptosis; Endocrinology/Hormones; Others |
CSRM617 hydrochloride 是转录因子ONECUT2(OC2,雄激素受体 AR 的主要调节剂) 的选择性小分子抑制剂,在 SPR 测定中Kd 为 7.43 uM,直接与 OC2-HOX 结构域结合。CSRM617 hydrochloride 通过裂解 Caspase-3 和 PARP 诱导细胞凋亡 (apoptosis)。CSRM617 hydrochloride 在小鼠的前列腺癌模型中具有良好的耐受性。 | |||
T14922 |
Cefodizime
|
Antibacterial; Antibiotic | Microbiology/Virology |
Cefodizime 是一种新型头孢菌素抗生素,具有广泛的生物活性。Cefodizime 对肾脏没有毒性且具有良好的耐受性和免疫调节活性,具有抗菌活性,可用于研究呼吸系统和泌尿系统的严重感染。 | |||
T37535 |
Camrelizumab
SHR-1210 |
||
Camrelizumab (SHR-1210) 是一种具有高亲和力且针对 PD-1的人源 IgG4-κ单克隆抗体。Camrelizumab 与 PD-1 的结合亲和力高达 3 nM,对 PD-1/PD-L1具有抑制作用, IC50 为 0.70 nM。Camrelizumab 具有抗肿瘤活性和耐受性,可用于研究包括 NSC-LC、ESCC、霍奇金淋巴瘤和晚期 HCC 等的癌症。 | |||
T3334 |
Velpatasvir
GS-5816,维帕他韦 |
HCV Protease; SARS-CoV | Microbiology/Virology; Proteases/Proteasome |
Velpatasvir (GS-5816) 是一种的 HCV NS5A 抑制剂。它也是 SARS-CoV 3CLpro 的抑制剂,IC50为 2.16 μM。 | |||
T4306 |
CCG-203971
CCG203971 |
Rho; Ras | Cell Cycle/Checkpoint; GPCR/G Protein; MAPK |
CCG-203971 是一种Rho/MRTF/SRF 通路抑制剂,具有潜在的抗转移作用。它有效靶向 RhoA/C 激活的 SRE 荧光素酶,IC50为 6.4 μM。它抑制 PC-3 细胞迁移,IC50为 4.2 μM。 | |||
T4615 |
Balsalazide sodium hydrate
巴柳氮钠水合物,Balsalazide disodium dihydrate,巴柳氮钠,Balsalazide disodium salt dihydrate,Balsalazide disodium |
STAT; Interleukin | Immunology/Inflammation; JAK/STAT signaling; Stem Cells |
Balsalazide sodium hydrate (Balsalazide disodium) 可通过调节IL-6/STAT3通路起抑癌作用,可用于治疗炎症性肠病。 | |||
T0866 |
Propafenone
Rythmol,普罗帕酮,Propafenonum |
Potassium Channel; MRP; Sodium Channel | Immunology/Inflammation; Membrane transporter/Ion channel |
Propafenone (Propafenonum) 是钠通道阻滞剂,它对 β 受体具有高亲和力 (IC50=32 nM)。它能够阻断瞬时外向钾电流 (Ito) (IC50: 4.9 nM) 和持续延迟整流器K+电流 (Isus) (IC50: 8.6 nM) ,具有抗心律失常的作用。它能够诱导线粒体功能障碍及诱导细胞凋亡,从而抑制食管癌增殖。 | |||
T24809 |
SMU-B
SMU B |
||
SMU-B is a well-tolerated c-Met/ALK dual inhibitor. | |||
T17296 |
Zotatifin
eFT226 |
Others | Others |
Zotatifin is a potent and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM). Zotatifin effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein b | |||
TP2149L |
NP213
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
NP213 is a rapidly acting synthetic antimicrobial peptide (AMP). NP213 is effective and well-tolerated in resolving nail fungal infections. NP213 has anti-fungal activities. NP213 targets the fungal cytoplasmic membrane and plays its role via membrane perturbation and disruption. | |||
T11013 |
Dextrorotation nimorazole phosphate ester
|
Others | Others |
Dextrorotation nimorazole phosphate ester is an anti-anaerobic and anti-parasitic agent. D-morpholine ornidazole organic phosphate is a newly developed, highly efficient, well-tolerated fourth-generation nitroimidazole derivative. Objective: Antibacterial | |||
T24699 |
R1498
R-1498,R 1498 |
||
R1498 is an inhibitor of cyclin-dependent kinase 2. It also acts by targeting angiogenesis and mitosis pathways. It is well-tolerated and orally active for hepatocellular carcinoma and gastric cancer treatment. | |||
T11214 |
EPI-589
|
Others | Others |
EPI-589, a quinone derivative and oxidoreductase enzyme inhibitor, is considered safe and well tolerated, showing promise for the treatment of amyotrophic lateral sclerosis (ALS). | |||
T25959 |
Pipebuzone
LD-4644,LD 4644,LD4644,Pipebuzonum |
||
Pipebuzone 是一种抗炎、解热、镇痛药,用于治疗各种风湿性疾病。它在临床和病理上都具有良好的耐受性,并具有可靠的抗炎作用。 | |||
T62571 | Clomifene hydrochloride | ||
Clomifene hydrochloride 可以诱导排卵,能够用于不孕症。hydrochloride 是一种简单的、相对安全的、易于给药且耐受性良好的、口服具有活力的化合物。 | |||
T10870 |
CP-547632 hydrochloride
|
FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
CP-547632 hydrochloride is a well-tolerated and orally-bioavailable inhibitor of the VEGFR-2 and basic FGF kinases (IC50s: 11 nM and 9 nM) with antitumor efficacy. | |||
T15365 |
G-744
|
BTK | Angiogenesis; Tyrosine Kinase/Adaptors |
G-744 is a selective and orally active inhibitor of Btk (IC50: 2 nM). G-744 is well-tolerated, metabolically stable. It also has an efficacious to treat arthritis. | |||
T33815 |
ORC-13661 HCl
ORC 13661,BPN13661,ORC13661,ORC-13661,BPN 13661,BPN-13661 |
||
Orc-13661 (BNP-13661) is a potent and well-tolerated oral active protective agent for the prevention of aminogrogycoside-induced hearing loss. | |||
T41082 |
Flobetapir
AV-45,Flobetapir |
||
Flobetapir (AV-45) is a well-tolerated imaging compound used in PET scanning. It is synthesized to create Florbetapir (18F), which is a radiopharmaceutical compound containing fluorine-18 radionuclide. | |||
T14509 |
BAY-707
|
Others | Others |
BAY-707, a highly potent and selective substrate-competitive inhibitor of MTH1 (NUDT1) with an IC50 of 2.3 nM, is well-tolerated in mice and exhibits a favorable pharmacokinetic (PK) profile compared to other MTH1 compounds. However, it demonstrates a clear lack of anticancer efficacy both in vitro and in vivo[1]. | |||
T26581 |
AIC-292
|
||
AIC-292 is a potent reverse transcriptase inhibitor with well tolerated in different cell lines. In addition, activity of AIC292 could be demonstrated against a broad panel of wild-type HIV-1 group. AIC292 also retained activity against viruses harboring | |||
T33583 |
Naldemedine
S-297995,S297995,Naldemedine,S 297995,S297,995,S 297,995,S297,995;Naldemedine,S-297,995 |
||
Naldemedine (S 297995) is a peripheral selective μ-opioid receptor antagonist being developed by Shionogi for the treatment of opioid-induced adverse reactions, including constipation, nausea, and vomiting. They are usually well tolerated, mainly with mil | |||
T16406 |
Orvepitant maleate
GW823296 maleate |
Neurokinin receptor | GPCR/G Protein; Neuroscience |
Orvepitant maleate is an effective, selective, and well-tolerated neurokinin-1 receptor (NK-1) antagonist (pKi: 10.2 for human neurokinin-1 receptor). Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatmen | |||
TP2141 |
Balixafortide TFA (1051366-32-5 free base)
Balixafortide TFA,POL6326 TFA |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
Balixafortide TFA (POL6326 TFA) is a selective, well-tolerated peptidic CXCR4 antagonist (IC50 < 10 nM). It shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium fl | |||
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. | |||
T62864 |
Hetrombopag
|
||
Hetrombopag 是一种 thrombopoietin receptor 的有效激动剂。Hetrombopag 具有良好的耐受性且安全性可控。Hetrombopag 具有潜力进行免疫性血小板减少症的研究。 | |||
T14682 |
BMS-962212
|
Others | Others |
BMS-962212, a direct, reversible, and selective factor XIa (FXIa) inhibitor, demonstrates fast pharmacodynamic (PD) response onset and rapid elimination with a well-tolerated profile. It dependently increases activated partial thromboplastin time and decreases FXI clotting activity exposure [1]. | |||
T12419L | PF-04634817 | CCR | Immunology/Inflammation; Microbiology/Virology |
PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy. PF-0463481 is an effective and orally active dual CCR2/CCR5 antagonist. It also has comparable human and rodent CCR2 potency (rat IC50=20.8 nM). PF-0463481 | |||
T29979L |
Amidantel free base
BAYd 8815,BAY d8815,BAYd-8815,Amidantel,BAY d-8815,BAY d 8815 |
||
Amidantel free base is a new aminophenylamidine with an interesting anthelminthic spectrum. In rodents the compound is active against nematodes, filariae and cestodes. Of special interest is the high efficacy in dogs against hookworms and large roundworms | |||
T14931 | Cerivastatin | Others | Others |
Cerivastatin is a highly potent, well-tolerated, and orally active HMG-CoA reductase inhibitor (Ki: 1.3 nM/L). Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition with anti-cancer effect. Cerivastatin r | |||
T69724 | Cilofexor tromethamine | ||
Cilofexor, also known as GS-9674, is a farnesoid X receptor (FXR) agonist. The nonsteroidal FXR agonist cilofexor (GS-9674) improves markers of cholestasis and liver injury in patients with PSC. In clinical study, cilofexor was well tolerated and led to significant improvements in liver biochemistries and markers of cholestasis in patients with PSC. | |||
TP2141L |
Balixafortide
POL6326 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM and it is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2]. Balixafortide blocks β-arresti | |||
T15376 |
GDC-0339
|
Pim | Chromatin/Epigenetic; JAK/STAT signaling |
GDC-0339 是可口服的、耐受性良好的泛 Pim 激酶高效抑制剂,具有研究多发性骨髓瘤的潜力,对 Pim1、Pim2 和 Pim3 作用的 Ki 值分别为 0.03、0.1 和 0.02 nM。 | |||
T28271 |
OSI-296
|
||
OSI-296 is a potent and dual inhibitor of cMET and RON kinases (IC50 value are 42 nM and 200 nM for cMet and sfRon respectively) . OSI-206 shows in vivo efficacy and is well tolerated in tumor xenografts models upon oral dosing. OSI-296 also reduces tumou | |||
T70104 |
Verubecestat tosylate
|
||
Verubecestat tosylate, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat tosylate is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat tosylate reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients. | |||
T73916 |
NP213 TFA
|
||
NP213 TFA是一种具有抗真菌(anti-fungal)活性的快速、新颖的合成抗菌肽(AMP)。该化合物通过瞄准真菌胞质膜并扰乱及破坏其结构来发挥作用,对甲真菌感染显示出高效与良好耐受性。 | |||
T38581 |
Antofloxacin
|
||
Antofloxacin is a well-tolerated, orally active, and broad-spectrum 8-amino-fluoroquinolone compound that exhibits potent antibacterial properties. It demonstrates superior activity against gyrA mutation-positive Helicobacter pylori strains, particularly in strains with mutations in the Asn87 position, when compared to levofloxacin. Additionally, Antofloxacin acts as a weak but reversible inhibitor of CYP1A2 and is clinically used to treat infections caused by various bacterial species. | |||
T70735 | Verosudil hydrochloride | ||
Verosudil, also known as AR-12286, is a potent and selective Rho kinase inhibitor. AR-12286 was well tolerated and provided statistically significant reduction in IOP (intraocular pressure) in patients with XFS (exfoliation syndrome) and OHT (ocular hypertension) or XFG (exfoliative glaucoma). This drug may represent an additional therapeutic paradigm for the treatment of XFG. | |||
T10896 | CSRM617 | Others | Others |
CSRM617 is a selective small molecule inhibitor of the transcription factor ONECUT2 (OC2, the main regulator of androgen receptor). The Kd in SPR analysis is 7.43 uM, which can directly bind to the OC2-HOX domain. CSRM617 induces apoptosis by cleaving the | |||
T68471 |
(+/-)- Adomeglivant
|
||
(+/-)- Adomeglivant, also known as LY2409021, is a potent and selective glucagon receptor antagonist. LY2409021 lowers blood glucose in healthy people and in those with type 2 diabetes. Blockade of glucagon signalling in patients with type 2 diabetes is well tolerated and results in substantial reduction of fasting and postprandial glucose with minimal hypoglycaemia, but with reversible increases in aminotransferases. Inhibition of glucagon signalling by LY2409021 is a promising potential treatm... | |||
T71899 |
Verubecestat TFA
|
||
Verubecestat TFA, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat TFA is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat TFA reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients. | |||
T70943 |
AM-9635
|
||
AM-9635 is a potent and selective PI3Kδ inhibitor. AM-9635 showes good cellular potency (in vitro pAKT IC50 = 4.2 nM ). AM-96352 inhibits KLH-specific IgG and IgM in a dosedependent manner AM-9635 is well tolerated at all doses and exhibits significantly reduced IgG and IgM specific antibodies . PI3Kα and PI3Kβ are ubiquitously expressed and play a role in cell growth, division, and survival. | |||
T62654 |
Fluocortin butyl ester
|
||
Fluocortin butyl ester 是一种发达的皮质类固醇化合物,局部使用时无法检测到全身性的皮质类固醇活性。Fluocortin butyl ester 似乎是一种有效的、耐受性良好的局部类固醇,能够用于常年性鼻炎的研究。 |