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DiscoveryProbe™ FDA-approved Drug Library

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Referência L1021-.1-1

Tamanho : 100uL/well(10mMsolution),96WellRacksWithScrewCap

Marca : APExBIO Technology

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DiscoveryProbe™ FDA-approved Drug Library

Catalog No.
L1021
2320 approved drugs and API from pharmacopoeia

Background

The DiscoveryProbe™ FDA-approved Drug Library consists of 2,320 bioactive compounds that have been clinically approved by regulatory agencies such as FDA, EMA, HMA, CFDA, and PMDA, or listed in recognized pharmacopeias. These pharmaceutical compounds cover a broad spectrum of well-characterized mechanisms of actions, including receptor agonists and antagonists, enzyme inhibitors, ion channel modulators, and signal pathway regulators. Representative agents include well-studied clinical drugs such as doxorubicin, metformin, and atorvastatin. Due to their widely validated pharmacological activities and established safety data, these compounds serve as a valuable resource for high-throughput (HTS) and high-content screening (HCS), drug repositioning efforts, and identification of novel therapeutic targets across biomedical research fields.

Product Citation

Featured Products of the Library

Catalog No. Product Name Summary Targets CAS Number Smiles
A3298 Cetirizine Antihistamine Neuroscience|Histamine Receptor 83881-51-0 C1CN(CCN1CCOCC(=O)O)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl
A3789 Salmeterol xinafoate β2-adrenergic receptor agonist GPCR/G protein|Adrenergic Receptor 94749-08-3 C1=CC=C(C=C1)CCCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O.C1=CC=C2C(=C1)C=CC(=C2O)C(=O)O
A4363 Fluvastatin Sodium HMG-CoA reductase inhibitor Metabolism|HMG-CoA Reductase 93957-55-2 CC(C)N1C2=CC=CC=C2C(=C1C=CC(CC(CC(=O)[O-])O)O)C3=CC=C(C=C3)F.[Na+]
A4370 Moclobemide (Ro 111163) Reversible inhibitor of MAO-A Metabolism|MAO 71320-77-9 C1COCCN1CCNC(=O)C2=CC=C(C=C2)Cl
A8252 Nintedanib(BIBF 1120) VEGFR/PDGFR/FGFR inhibitor Tyrosine Kinase/Adaptors|PDGFR 928326-83-4 CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)NC(=C3C4=C(C=C(C=C4)C(=O)OC)NC3=O)C5=CC=CC=C5
B1792 Montelukast Sodium Leukotriene receptor antagonist GPCR/G protein|CysLT1 receptor 151767-02-1 CC(C)(C1=CC=CC=C1CCC(C2=CC=CC(=C2)C=CC3=NC4=C(C=CC(=C4)Cl)C=C3)SCC5(CC5)CC(=O)[O-])O.[Na+]
N1674 Piperine MAPK inhibitor Natural Products 94-62-2 C1CCN(CC1)C(=O)C=CC=CC2=CC3=C(C=C2)OCO3
N1707 Coumarin Precursor in chemical reaction Natural Products 91-64-5 C1=CC=C2C(=C1)C=CC(=O)O2

Quality Control

Related Biological Data

Related Biological Data

Related Biological Data

Related Biological Data

Related Biological Data

Related Biological Data

Related Biological Data

Related Biological Data

Related Biological Data

Related Biological Data

Related Biological Data

 

Signaling Pathway

Dopamine Receptor Compare Products
Histamine Receptor Compare Products
HMG-CoA Reductase Compare Products
 

Storage and Shipping Information

Form Pre-dissolved DMSO solutions Stability Solution: -20°C for 12 months, -80°C for 24 months
Packaging 96-well Microplate format with peelable foil seal;
96-well DeepWell format with peelable foil seal and EVA cap (100 μL/well, 10 mM DMSO);
96-well rack with Matrix 2D Barcoded ScrewTop Storage tubes (250 μL or 100 μL/well, 10 mM DMSO).
Shipping Condition Evaluation sample solution: ship with blue ice
All other available size: ship with RT, or blue ice upon request

References

1. Barrows NJ, Campos RK, Powell ST, et al. A Screen of FDA-Approved Drugs for Inhibitors of Zika Virus Infection. Cell Host Microbe. 2016 Jul 27. pii: S1931-3128(16)30303-1.
Abstract
We interrogated a FDA-approved chemicals library for their ability to block infection of human HuH-7 cells by a newly isolated ZIKV strain (ZIKV MEX_I_7). In our in vitro screening assay, more than 20 out of 774 tested compounds reduced ZIKV infection. Then these compounds were further validated for inhibition of ZIKV infection in human neural, cervical and placental stem cell lines, as well as primary human amnion cells. We found that others that had no previously known antiviral activity (e.g., daptomycin) and anti-flaviviral drugs (e.g., bortezomib and mycophenolic acid) were identified as inhibitors of ZIKV infection. There were several drugs that reduced ZIKV infection across multiple cell types, which could be tested in clinical studies of ZIKV infection and provided small molecules to study ZIKV pathogenesis.
2. Stavrovskaya IG, Narayanan MV, Zhang W, et al. Clinically approved heterocyclics act on a mitochondrial target and reduce stroke-induced pathology. J Exp Med. 2004 Jul 19;200(2):211-22.
Abstract
Mitochondria are a major checkpoint in several pathways leading to neuronal cell death and the mitochondrial permeability transition (mPT) may be critical in stroke-related injury. In order to prove this hypothesis, 1,040 FDA-approved drugs and other bioactive compounds were tested as potential mPT inhibitors. We found that 28 structurally related drugs, including tricyclic antipsychotics and antidepressants, capable of delaying the mPT. Clinically achievable doses of promethazine inhibited mPT and were protective in both in vitro and mouse models of stroke. Also, promethazine protected primary neuronal cultures subjected to oxygen-glucose deprivation and reduced neurological impairment and infarct size in mice subjected to middle cerebral artery occlusion/reperfusion. These results provided a class of safe, tolerable drugs for stroke and neurodegeneration and also provided new tools for understanding mitochondrial roles in neuronal cell death.

Compound Library Composition

Storage

  • 【APExBIO】Compound Library Usage Instructions

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