Cat. No. | Product Name | Target | Signaling Pathways |
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T60076 |
Oritinib
SH-1028 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Oritinib (SH-1028) 是一种 EGFR 抑制剂,对 EGFR (wt)、EGFR (L858R)、EGFR (L861Q)、EGFR (L858R/T790M)、EGFR (d746-750) 的 IC50 分别为 18、0.7、4、0.1、1.4 和 0.89 nM , EGFR (d746-750/T790M), 分别。奥瑞替尼可用于治疗非小细胞肺癌的研究。 | |||
T19450 |
N-desmethyl Enzalutamide
4-[3-[4-氰基-3-(三氟甲基)苯基]-5,5-二甲基-4-氧代-2-硫代-1-咪唑烷基]-2-氟苯甲酰胺,N-desmethyl MDV 3100 |
Androgen Receptor | Endocrinology/Hormones |
N-desmethyl Enzalutamide (N-desmethyl MDV 3100) 是一种 Enzalutamide 的主要活性代谢物,具有与 Enzalutamide 相似的一级和二级药效功效,并在与 Enzalutamide 大致相同的血浆浓度下循环。 | |||
T30514 |
BMS-344577
U259PQB19A,UNII-U259PQB19A,CHEMBL570867,BMS 344577 |
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BMS-344577, a lactam derivative based on arylguanidine, is a potent oral active FXA inhibitor with excellent susceptibility in vitro, good pharmacokinetics, and pharmacodynamics in animal models. | |||
T24924 |
Umibecestat HCl (1387560-01-1 free base)
CNP 520,Umibecestat HCl,Umibecestat hydrochloride,CNP520,CNP-520 |
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Umibecestat is a beta-secretase inhibitor. CNP520 has a selectivity, pharmacodynamics, and distribution profile suitable for AD prevention studies. | |||
T70930 |
GSK SYK inhibitor
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The immunoregulator spleen tyrosine kinase (SYK) is upregulated in cutaneous lupus erythematosus (CLE). This double-blind, multicentre, Phase Ib study evaluated the safety, tolerability, pharmacokinetics, pharmacodynamics and clinical efficacy of the selective SYK inhibitor GSK2646264 in active CLE lesions | |||
T69983 |
Ixazomib citrate EtOH
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Ixazomib citrate, also known as MLN9708, is a prodrug of Ixazomib (MMLN-2238). MLN9708 is an orally bioavailable second generation proteasome inhibitor (PI) with potential antineoplastic activity. MLN9708, after hydrolyzing to pharmacologically active MLN2238 (ixazomib), is a next-generation proteasome inhibitor with demonstrated preclinical and clinical antimyeloma activity. MLN9708, compared with bortezomib, has improved pharmacokinetics, pharmacodynamics, and antitumor activity in preclinic... | |||
T69664 | Umibecestat HCl | ||
Umibecestat, also known as CNP-520, is a beta-secretase inhibitor and is a drug candidate for prevention trials in Alzheimer's disease. CNP520 has a selectivity, pharmacodynamics, and distribution profile suitable for AD prevention studies. CNP520 reduced brain and cerebrospinal fluid (CSF) Aβ in rats and dogs, and Aβ plaque deposition in APP-transgenic mice. CNP520 reduces Aβ load and neuroinflammation in APP‐transgenic mice | |||
T72125 |
Cap-dependent endonuclease-IN-9
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Influenza Virus | Microbiology/Virology |
Cap-dependent endonuclease-IN-9 是高效的 CEN 抑制剂,其对流感病毒具明显抑制作用,同时展现低细胞毒性、良好的体内药剂动力学及药效学特性。此化合物强力抑制 A 病毒 RNA 聚合酶活性。 | |||
T81661 |
NNMT-IN-4
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NNMT-IN-4(compound 38),一种选择性、非竞争性且具有膜通透性的烟酰胺N-甲基转移酶(NNMT)抑制剂,在体外生化及细胞实验中的IC50值为42 nM和38 nM。该抑制剂展现出良好的PK/PD关系和安全性,同时具备优秀的口服生物利用度和药物制剂性质,适合作为NNMT活性研究的体内化学探针。 | |||
T38266 |
Nirogacestat dihydrobromide
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Potent γ-secretase inhibitor (IC50 values are 1.2 and 6.2 nM in whole cell and cell-free assays, respectively). Reduces Aβ in brain, CSF and plasma in mice and guinea pigs. Lanz et al (2010) Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014. J.Pharmacol.Exp.Ther. 334 269 PMID:20363853 | |||
T37176 | Edoxaban impurity 6 | ||
Edoxaban impurity 6 is an impurity of Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention[1][2]. [1]. Furugohri T, et al. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008 Sep;6(9):1542-9.[2]. Mendell J, Lee F, Chen S, The Effe... |