Search Result
Results for "
Tolerated
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
9
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0265
-
-
-
- HY-16700
-
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ADC Payload
Topoisomerase
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Cancer
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PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.
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- HY-B0193A
-
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Adrenergic Receptor
Autophagy
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Cardiovascular Disease
Endocrinology
Cancer
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Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively .
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- HY-112163
-
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eFT226
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Eukaryotic Initiation Factor (eIF)
SARS-CoV
Apoptosis
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Infection
Cancer
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Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex . Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM) . Zotatifin induces cell apoptosis .
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- HY-145603
-
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VX-121
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CFTR
Chloride Channel
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Neurological Disease
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Vanzacaftor (VX-121) is an orally active noval corrector of Cystic fibrosis transmembrane conductance regulator (CFTR). Vanzacaftor improves processing and trafficking of CFTR protein as well as increases chloride transport in triple combined with Tezacaftor (HY-15448) and Deutivacaftor. Vanzacaftor-Tezacaftor-Deutivacaftor is safe and well tolerated, improving lung function, respiratory symptoms, and CFTR function with cystic fibrosis, which is promising for research in the field of cystic fibrosis diseases .
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- HY-101560
-
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BMS-986205; ONO-7701
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Indoleamine 2,3-Dioxygenase (IDO)
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Cancer
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Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 value of 1.1 nM in IDO1-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers .
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- HY-109523
-
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HMG-CoA Reductase (HMGCR)
Ferroptosis
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Cardiovascular Disease
Cancer
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Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
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- HY-122611A
-
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Androgen Receptor
Apoptosis
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Cancer
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CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
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- HY-16712
-
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TGF-β Receptor
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Cancer
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LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) .
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- HY-109052
-
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JNJ-54861911
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Beta-secretase
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Neurological Disease
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Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment .
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- HY-174406
-
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Myosin
PDGFR
Reactive Oxygen Species (ROS)
Ferroptosis
Akt
mTOR
ERK
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Cancer
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MT-125 is a specific and well-tolerated inhibitor of non-muscle myosin IIA (Ki,NMIIA = 2.7 μM) and IIB (EC50 = 1.7 μM). MT-125 can pass through the blood-brain barrier. MT-125 induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 can enhance the PDGFR signaling pathway. MT-125 can be used for research on glioblastoma.
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- HY-12170
-
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AG3340; KB-R9896
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MMP
Apoptosis
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Cancer
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Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3, MMP-13 and MMP-9 with Kis of 0.05 nM, 0.3 nM, 0.03 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity .
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- HY-114237
-
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Sodium Channel
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Neurological Disease
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GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects .
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- HY-P99665
-
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LY-3209590
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Insulin Receptor
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Metabolic Disease
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Insulin efsitora alfa (LY-3209590) is a selective agonist of insulin receptor (IR). Insulin efsitora alfa is a fusion protein composed of human IR agonists fused with the crystallizable (Fc) domain of human immunoglobulin G2 (IgG2) fragment, with a molecular weight of 64.1 kDa. Insulin efsitora alfa is well tolerated and has potential applications in diabetes .
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- HY-B1895
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-
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- HY-16487
-
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TMFX; TA-167 free acid; A-62254 free acid
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Bacterial
Antibiotic
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Infection
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Temafloxacin (TMFX) is an orally active quinolone broad-spectrum antibacterial agent. Temafloxacin is well tolerated in lower respiratory and genitourinary tract infections .
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- HY-N1373
-
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Apoptosis
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Cancer
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Sophoridine is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .
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- HY-N7393
-
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Palatinitol
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Environmental Pollutants
Lactate Dehydrogenase
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Metabolic Disease
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Isomalt (Palatinitol), a well-tolerated, non-toxic polyol and a protein-stabilizing excipient, stabilizes lactate dehydrogenase (LDH) moderately during freeze-drying, and performs better during storage. Isomalt is traditionally used as a sweetening agent in the food industry and as a tabletting excipient for pharmaceutical purposes .
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- HY-16976
-
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Pim
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Cancer
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GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma .
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- HY-B1804
-
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Trioctanoin; Glyceryl trioctanoate
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Endogenous Metabolite
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Neurological Disease
Inflammation/Immunology
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Tricaprilin (Trioctanoin) is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
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- HY-100375
-
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ALKS 8700; BIIB098
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Keap1-Nrf2
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Inflammation/Immunology
|
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Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) proagent in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS). Diroximel fumarate is a Nrf2 activator that alleviate MGO-induced pain hypersensitivity .
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- HY-P1682A
-
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POL6326 TFA
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CXCR
Arrestin
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Cancer
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Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
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- HY-129650
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AV-45; Flobetapir
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Biochemical Assay Reagents
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Others
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Flobetapir (AV-45) may be a well-tolerated imaging agent. Flobetapir synthesizes Florbetapir (18F) that is a PET scanning radiopharmaceutical compound containing the radionuclide fluorine-18 .
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- HY-109148
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TD-1473; JNJ-8398
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JAK
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Inflammation/Immunology
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Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor. Izencitinib (TD-1473) can be used in the study for ulcerative colitis .
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- HY-148772
-
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DNA/RNA Synthesis
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Neurological Disease
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PTC258 is a specific and orally active splicing modulator of Elongator complex protein 1 gene (ELP1). PTC258 increases the expression of ELP1 in vitro and in vivo. PTC258 is well tolerated in mouse model .
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- HY-12170A
-
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AG3340 hydrochloride; KB-R9896 hydrochloride
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MMP
Apoptosis
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Cancer
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Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3, MMP-13 and MMP-9 with Kis of 0.05 nM, 0.3 nM, 0.03 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity .
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- HY-126810A
-
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Fungal
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Infection
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NP213 TFA is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 TFA targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 TFA is effective and well-tolerated in resolving nail fungal infections .
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- HY-112163A
-
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rel-eFT226
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Eukaryotic Initiation Factor (eIF)
SARS-CoV
Apoptosis
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Infection
Cancer
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rel-Zotatifin is the racemic isomer of Zotatifin, acts as an eIF4A inhibitor with activity less than Zotatifin. Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex .
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- HY-P1682
-
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POL6326
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CXCR
Arrestin
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Cancer
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Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
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- HY-18060
-
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TC-5619
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nAChR
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Neurological Disease
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Bradanicline (TC-5619) is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
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- HY-161672
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IRE1
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Cancer
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G-5758 is a selective and orally effective IRE1α inhibitor with an IC50 of 38 nM (detected by the XBP1s luciferase reporter cell assay). G-5758 is still well tolerated in rats at oral doses up to 500 mg/kg. G-5758 can be used in the research of multiple myeloma .
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- HY-122347A
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GW823296 maleate
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Neurokinin Receptor
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Neurological Disease
Inflammation/Immunology
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Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment .
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- HY-112081
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DNA/RNA Synthesis
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Cancer
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BAY-707, a chemical probe, is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy .
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- HY-107345
-
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Ombolan
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Prostaglandin Receptor
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Inflammation/Immunology
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Droxicam (Ombolan) is a non-steroidal anti-inflammatory agent, with strong analgesic activity. Droxicam acts by inhibiting PGE2 varies, and is characterised by being a pro-drug of Piroxicam (HY-B0253). Droxicam is well tolerated with slight side effects in the said mucosa. Droxicam does not show cardiovascular or respiratory effects in cats, and inhibits peritoneal capillary permeability in mouse .
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- HY-125999
-
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Reactive Oxygen Species (ROS)
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Neurological Disease
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EPI-589, a quinone derivative, is a safe and well tolerated oxidoreductase enzyme inhibitor and a free radical scavenger, with blood-brain barrier permeable and orally available. EPI-589 is a redox-active neuroprotectant that effectively delays the symptoms of motor neuron disease in wobbler mice. EPI-589 can be used in amyotrophic lateral sclerosis (ALS) research .
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- HY-34222
-
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DYRK
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Cancer
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7-Deazaguanine (Compound 1) is a highly selective, well-tolerated, brain-penetrant DYRK1A inhibitor. 7-Deazaguanine is promising for research of cancers and Down’s syndrome .
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- HY-124674A
-
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Monoamine Oxidase
EGFR
Akt
TGF-beta/Smad
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Cancer
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CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties .
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- HY-126810
-
|
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Fungal
|
Infection
|
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NP213 is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 is effective and well-tolerated in resolving nail fungal infections .
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-
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- HY-121212
-
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LDLR
|
Metabolic Disease
Inflammation/Immunology
|
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Icosabutate, an orally active ω-3 polyunsaturated fatty acid, is an aeicosapentaenoic acid (EPA) derivative. Icosabutate overcomes the drawbacks of unmodified EPA for liver targeting and improves insulin sensitivity, hepatic inflammation and fibrosis . Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia .
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- HY-B1804S
-
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Trioctanoin-13C3; Glyceryl trioctanoate-13C3
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
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Tricaprilin- 13C3 (Trioctanoin- 13C3) is a 13C-labeled Tricaprilin (HY-B1804) . Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
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-
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- HY-103262
-
-
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- HY-B0265B
-
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(S)-BAY-e 9736
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Calcium Channel
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Cardiovascular Disease
|
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(S)-Nimodipine ((S)-BAY-e 9736) is an enantiomer of Nimodipine. Nimodipine (BAY-e 9736) is an orally active, well-tolerated and light-sensitive dihydropyridine calcium antagonist. Nimodipine can be used for the research of cerebrovascular disorders .
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-
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- HY-B1895R
-
-
-
- HY-18317
-
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VEGFR
RET
c-Kit
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Cancer
|
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JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively .
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-
-
- HY-107495
-
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NSC19005
|
MOFs
Histamine Receptor
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Inflammation/Immunology
|
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Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine . Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA) .
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-
-
- HY-129458
-
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HMG-CoA Reductase (HMGCR)
Ferroptosis
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Cardiovascular Disease
Cancer
|
|
Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
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-
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- HY-122611
-
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Androgen Receptor
Apoptosis
|
Cancer
|
|
CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
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- HY-117621
-
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CCR
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Metabolic Disease
|
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PF-0463481 is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy .
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- HY-117621A
-
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CCR
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Metabolic Disease
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PF-0463481 succinate is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 succinate is safe and well-tolerated and has the potential for the study of diabetic nephropathy .
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- HY-102036
-
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Btk
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Inflammation/Immunology
|
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G-744 is a highly potent, selective and orally active Btk inhibitor with an IC50 of 2 nM. G-744 is metabolically stable, well tolerated and efficacious to treat arthritis .
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- HY-123490
-
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INS50589
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P2Y Receptor
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Inflammation/Immunology
|
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Regrelor disodium (INS 50589) is a platelet P2Y12 receptor antagonist. Regrelor disodium is a well-tolerated, reversible ADP competitive antagonist. Regrelor disodium inhibits cell proliferation. Regrelor disodium can be used in inflammation-related research .
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- HY-151174
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
|
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PDE4-IN-12 is a potent pan-PDE4 inhibitor, with IC50s of 3.5 and 15 nM for PDE4 and PDE7, respectively (SI=2.71 and 4.27, respectively). PDE4-IN-12 shows well tolerated, can be used in study of inflammatory bowel diseases (IBDs) .
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- HY-14834
-
-
- HY-163460
-
-
- HY-113595
-
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TMFX hydrochloride; TA-167; A-62254
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Antibiotic
Bacterial
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Infection
|
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Temafloxacin (TMFX) hydrochloride is an orally active quinolone broad-spectrum antibacterial agent. Temafloxacin hydrochloride is well tolerated in lower respiratory and genitourinary tract infections .
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-
- HY-B1895S
-
-
- HY-14135
-
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BMS 043
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HIV
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Infection
Inflammation/Immunology
|
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BMS 488043 (BMS 043) is an orally active and well-tolerated inhibitor of the attachment of human immunodeficiency virus type 1 (HIV-1) to CD4+ lymphocytes .
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-
- HY-107176A
-
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HS-25
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Others
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Metabolic Disease
|
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Hyzetimibe is a cholesterol absorption inhibitor. Hyzetimibe blocks the intestinal absorption of cholesterol and phytol. Hyzetimibe is well tolerated in animal models, with an LDmax 2000 mg/kg in rats and an LDmax 500 mg/kg in rhesus monkeys .
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- HY-B0265S
-
-
- HY-N15404
-
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Parasite
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Infection
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Glaucarubin is a bitter lactone found in Simaruba glauca. Glaucarubin can be used as an amœbicide for amebiasis research. Glaucarubin is well tolerated, with LD50s of 1,600 mg/kg for mice and 6,400 mg/kg for rats .
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- HY-105040
-
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LY2140023 hydrate
|
mGluR
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Neurological Disease
|
|
Pomaglumetad methionil (LY2140023 hydrate) is an oral methionine prodrug of the potent specific mGlu2/3 receptor agonist LY404039 (HY-50906). Pomaglumetad methionil is well-tolerated and has a distinct safety profile, and can be used for schizophrenia .
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- HY-139068
-
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Drug Derivative
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Others
|
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Ibuprofen arginine is an orally active L-arginine of Ibuprofen (HY-78131). With rapid absorption and high bioavailability, Ibuprofen arginine can effectively relieve a variety of acute pain, and has little damage to gastric mucosa and is well tolerated. Ibuprofen arginine can be used in research for pain relief .
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- HY-N1373A
-
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(+)-Sophoridine
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Apoptosis
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Cancer
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d-Sophoridine ((+)-Sophoridine) is the dextro isoform of Sophoridine (HY-N1373), which is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .
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-
- HY-P990966
-
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JR-142
|
GHR
IGF-1R
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Others
|
|
Redalsomatropin alfa (JR-142) is a recombinant long-acting growth hormone. Redalsomatropin alfa extends its half-life through fusion with modified serum albumin. Redalsomatropin alfa is well-tolerated and can maintain IGF-1 levels. Redalsomatropin alfa can be used in research related to growth hormone deficiency .
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- HY-14240
-
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PG 530742; PGE 530742; PGE 7113313
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MMP
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Cardiovascular Disease
|
|
PG 116800 (PGE 530742; PGE 7113313) is an orally active, selective and high-affinity inhibitor of MMP. PG 116800 acts as an inhibitor of ventricular remodeling, reduces left ventricular volumes and infarct zone collagen content, and improves ejection fraction. PG 116800 is generally well tolerated, but is associated with higher rates of arthralgia, joint stiffness, and dyspepsia. PG 116800 can be used for the research of myocardial infarction .
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- HY-16700G
-
|
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ADC Payload
Topoisomerase
|
Cancer
|
|
PNU-159682 GMP is a GMP grade PNU-159682 (HY-16700). PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.
|
-
- HY-117287A
-
|
BMS-986165 hydrochloride
|
Interleukin Related
JAK
IFNAR
|
Inflammation/Immunology
|
|
Deucravacitinib hydrochloride (BMS-986165 hydrochloride) is a highly selective all-site inhibitor with potent inhibitory activity against TYK2. Deucravacitinib hydrochloride can effectively block IL-12, IL-23 and type I interferon signaling. Deucravacitinib hydrochloride demonstrates significant efficacy in preclinical models of inflammatory bowel disease. Deucravacitinib hydrochloride demonstrated superiority over placebo and apremilast on multiple efficacy endpoints in moderate to severe plaque psoriasis. Deucravacitinib hydrochloride was well tolerated in inhibition .
|
-
- HY-123319A
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the research of infections caused by a diverse group of bacterial species .
|
-
- HY-112935
-
|
BAX326; Coagulation Factor IX [Recombinant]; BeneFIX
|
Ser/Thr Protease
|
Others
|
|
Nonacog alfa (BAX326) is a recombinant human factor IX that can be used for the research of haemophilia B .
|
-
- HY-121307
-
|
|
Drug Derivative
|
Metabolic Disease
|
|
Gliamilide is an active and well tolerated sulfamylurea derivative and displays a very short plasma half-life. Gliamilide is promising for research of maturity-onset diabetic deseases .
|
-
- HY-128386
-
-
- HY-118269
-
|
|
c-Met/HGFR
|
Cancer
|
|
OSI-296 is a potent, oral and selective inhibitor of cMET and RON kinases. OSI-296 shows in vivo efficacy in MKN45 tumor xenografts models and well tolerated .
|
-
- HY-136676
-
|
|
Renin
|
Cancer
|
|
Cgp 38560 methanesulfonate is a well-tolerated renin inhibitor. Cgp 38560 methanesulfonate caused a dose-dependent decrease in angiotensin II and plasma renin activity, and a dose-dependent increase in active renin.
|
-
- HY-106567
-
|
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
|
Fluocortin butyl ester is a developed corticosteroid compound with no detectable systemic corticosteroid activity when it is used topically. Fluocortin butyl ester appears to be an effective well-tolerated topical steroid useful in the research of perennial rhinitis .
|
-
- HY-148719
-
|
|
Topoisomerase
|
Cancer
|
|
ARN24139(compound 3f) is a topoisomerase II (topoII) inhibitor with the IC50 of 7.3 μM. ARN24139 can inhibit cancer cell proliferation and is well tolerated in vivo .
|
-
- HY-146615
-
|
|
TAM Receptor
|
Cancer
|
|
Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model .
|
-
- HY-16487R
-
|
TMFX (Standard); TA-167 free acid (Standard); A-62254 free acid (Standard)
|
Reference Standards
Bacterial
Antibiotic
|
Infection
|
|
Temafloxacin (Standard) is the analytical standard of Temafloxacin. This product is intended for research and analytical applications. Temafloxacin (TMFX) is an orally active quinolone broad-spectrum antibacterial agent. Temafloxacin is well tolerated in lower respiratory and genitourinary tract infections .
|
-
- HY-146692
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
IQTub4P is a potent microtubule (MT) inhibitor. IQTub4P has the cytotoxicity in in HeLa cells, with EC50 of 170 nM. IQTub4P inhibits microtubule structure and function. IQTub4P is well-tolerated in vivo .
|
-
- HY-B0265R
-
|
BAY-e 9736 (Standard)
|
Reference Standards
Autophagy
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Nimodipine (Standard) is the analytical standard of Nimodipine. This product is intended for research and analytical applications. Nimodipine (BAY-e 9736) is an orally active, well-tolerated and light-sensitive dihydropyridine calcium antagonist. Nimodipine can be used for the research of cerebrovascular disorders .
|
-
- HY-B1895S1
-
-
- HY-129650R
-
|
AV-45 (Standard); Flobetapir (Standard)
|
Biochemical Assay Reagents
Reference Standards
|
Others
|
|
Flobetapir (Standard) (AV-45 (Standard)) is the analytical standard of Flobetapir (HY-129650). This product is intended for research and analytical applications. Flobetapirmay is a well-tolerated imaging agent. Flobetapir synthesizes Florbetapir (18F) that is a PET scanning radiopharmaceutical compound.
|
-
- HY-N1373R
-
|
|
Reference Standards
Apoptosis
|
Cancer
|
|
Sophoridine (Standard) is the analytical standard of Sophoridine. This product is intended for research and analytical applications. Sophoridine is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .
|
-
- HY-15106
-
|
|
CaSR
|
Metabolic Disease
Inflammation/Immunology
|
|
SB-423557 is an orally active calcium-sensing receptor (CaR) antagonist (IC50=520 nM), precursor of SB-423562 (IC50=73 nM). SB-423557 is well tolerated in human and increases plasma concentrations of exogenous parathyroid hormone (PTH) and stimulates bone formation .
|
-
- HY-106546
-
|
KC 9147
|
Fungal
|
Infection
|
|
Tolciclate (KC 9147) is an antifungal agent with in vitro inhibitory activity against dermatophytes, effective at concentrations of 0.01-0.1 μg/mL. Tolciclate is colorless and soluble in well-tolerated excipients, and it is more lipophilic than Tolnaftate (HY-B0370). Tolciclate can be used in research related to antifungal infections .
|
-
- HY-162572
-
|
|
Parasite
|
Infection
|
|
Bitipazone, diacetylbis(piperidinethyl)thiourea cysteine ester (I), has potent anticoccidial activity. Bitipazone showed significant efficacy and good tolerability in rabbits and turkeys, and in chronic toxicity tests, bitipazone was tolerated in turkeys at concentrations below 90 ppm in feed. Pharmacokinetic studies show that bitipazone is eliminated slowly from the blood and organs of these animal species .
|
-
- HY-122347
-
|
GW823296
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
Orvepitant (GW823296) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant can across the blood-brain barrier. Orvepitant has the potential for depressive disorder and chronic refractory cough (CRC) treatment .
|
-
- HY-109083A
-
|
GS-9674 tromethamine
|
Autophagy
FXR
|
Metabolic Disease
|
|
Cilofexor tromethamine (GS-9674 tromethamine) is a nonsteroidal farnesene oxide receptor agonist with activity in improving markers of cholestasis and liver injury. Cilofexor tromethamine was shown to be well tolerated in patients without cirrhosis and resulted in significant improvements in liver biochemical parameters and cholestatic markers. Cilofexor tromethamine offers a potential inhibitory option for the management of primary sclerosing cholangitis .
|
-
- HY-N7393R
-
|
Palatinitol (Standard)
|
Reference Standards
Lactate Dehydrogenase
|
Metabolic Disease
|
|
Isomalt (Standard) is the analytical standard of Isomalt. This product is intended for research and analytical applications. Isomalt (Palatinitol), a well-tolerated, non-toxic polyol and a protein-stabilizing excipient, stabilizes lactate dehydrogenase (LDH) moderately during freeze-drying, and performs better during storage. Isomalt is traditionally used as a sweetening agent in the food industry and as a tabletting excipient for pharmaceutical purposes .
|
-
- HY-107495R
-
|
NSC19005 (Standard)
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
|
|
Betahistine EP Impurity C (Standard) is the analytical standard of Betahistine EP Impurity C. This product is intended for research and analytical applications. Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine . Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA) .
|
-
- HY-123319
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Antofloxacin hydrochloride is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin hydrochloride shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin hydrochloride is a weak, reversible inhibitor of CYP1A2 for the research of infections caused by a diverse group of bacterial species .
|
-
- HY-109523S
-
|
|
Ferroptosis
HMG-CoA Reductase (HMGCR)
Isotope-Labeled Compounds
|
Cardiovascular Disease
Cancer
|
|
Cerivastatin-d3 sodium is deuterated labeled Cerivastatin sodium (HY-109523). Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
|
-
- HY-B1804S1
-
|
Trioctanoin-d50; Glyceryl trioctanoate-d50
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
|
Tricaprilin-d50 (Trioctanoin-d50) is the deuterium labeled Tricaprilin (HY-B1804). Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
|
-
- HY-B1804S2
-
|
Trioctanoin-d15; Glyceryl trioctanoate-d15
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
|
Tricaprilin-d15 (Trioctanoin-d15) is the deuterium labeled Tricaprilin (HY-B1804). Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
|
-
- HY-150766
-
|
|
Bacterial
|
Infection
|
|
KPC-2-IN-1, boronic acid derivative, is a potent KPC-2 inhibitor with Ki of 0.032 μM. KPC-2-IN-1 enhances the activity of cefotaxime in KPC-2 expressing E. coli. KPC-2-IN-1 exhibits well tolerated in human HEK-293 cells, which can be used for the study of E. coli resistance to β-lactam antibiotics .
|
-
- HY-116149
-
|
|
nAChR
|
Others
|
|
A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.
|
-
- HY-18060A
-
|
TC-5619 hydrochloride
|
nAChR
|
Neurological Disease
|
|
Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline hydrochloride exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline hydrochloride possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline hydrochloride requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline hydrochloride is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
|
-
- HY-122611R
-
|
|
Reference Standards
Androgen Receptor
Apoptosis
|
Cancer
|
|
CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
|
-
- HY-N1486R
-
|
3-Ketoursolic acid (Standard)
|
Reference Standards
Apoptosis
Endogenous Metabolite
NF-κB
|
Inflammation/Immunology
Cancer
|
|
CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
|
-
- HY-101560R
-
|
BMS-986205 (Standard); ONO-7701 (Standard)
|
Indoleamine 2,3-Dioxygenase (IDO)
Reference Standards
|
Cancer
|
|
Linrodostat (Standard) is the analytical standard of Linrodostat (HY-101560). This product is intended for research and analytical applications. Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 value of 1.1 nM in IDO1-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers .
|
-
- HY-100375R
-
|
ALKS 8700 (Standard); BIIB098 (Standard)
|
Reference Standards
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Diroximel fumarate (Standard) is the analytical standard of Diroximel fumarate (HY-100375). This product is intended for research and analytical applications. Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) proagent in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS). Diroximel fumarate is a Nrf2 activator that alleviate MGO-induced pain hypersensitivity .
|
-
- HY-182059
-
|
|
Glutathione S-transferase
Reactive Oxygen Species (ROS)
|
Cancer
|
|
GSTP1-IN-1 is a selective GSTP1 inhibitor with an IC50 of 0.79 μM and a Kd of 0.63 μM. GSTP1-IN-1 inhibits the proliferation of gastric cancer cells, induces ROS production and depletes glutathione. GSTP1-IN-1 achieves systemic exposure and is well tolerated in xenograft mouse models, while inhibiting tumor growth. GSTP1-IN-1 can be used in gastric cancer-related research .
|
-
- HY-156654
-
|
PF-07817883
|
SARS-CoV
Virus Protease
|
Infection
|
|
Ibuzatrelvir (PF-07817883), a second-generation, orally bioavailable, is SARS-CoV-2 main protease (M pro and 3CL pro) inhibitor with improved metabolic stability. Ibuzatrelvir has demonstrated pan-human coronavirus antiviral activity and off-target selectivity profile in vitro and in preclinical animal studies. Ibuzatrelvir is well tolerated with a safety profile similar to placebo and prevents viral infection and transmission. Ibuzatrelvir can be used to inhibit COVID-19 .
|
-
- HY-130418
-
|
|
Adrenergic Receptor
|
Cancer
|
|
(-)-Domesticine is an anti-α-1D-adrenoceptor compound with cytotoxic activity. (-)-Domesticine showed activity in MTS cytotoxicity assays against human colon cancer cell lines HCT-116 and Caco-2. (-)-Domesticine tolerates alkoxy substituents and benzoate functional groups at the C1 position in modifications of its chemical structure. The most potent compounds of (-)-Domesticine have IC50 values in the range of 23-38 μM, similar to the known cytotoxic compound etoposide .
|
-
- HY-18060B
-
|
TC-5619 tosylate
|
nAChR
|
Inflammation/Immunology
|
|
Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline tosylate exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline tosylate possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline tosylate requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline tosylate is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
|
-
- HY-131879
-
|
|
Sodium Channel
|
Neurological Disease
|
|
NS383 is a potent and uniquely selective inhibitor of rat ASICs containing 1a and/or 3 subunits. NS383 inhibits H(+)-activated currents recorded from rat homomeric ASIC1a, ASIC3, and heteromeric ASIC1a+3 with IC50 values ranging from 0.61 to 2.2 μM. NS383 is well tolerated and capable of reversing pathological painlike behaviors, presumably via peripheral actions, but possibly also via actions within central pain circuits .
|
-
- HY-19904A
-
|
(+/-)-LY2409021
|
Endogenous Metabolite
|
Metabolic Disease
|
|
(+/-)-Adomeglivant ((+/-)-LY2409021) is a potent and selective glucagon receptor antagonist with hypoglycemic activity. (+/-)-Adomeglivant is effective in lowering blood sugar levels in both healthy people and people with type 2 diabetes. (+/-)-Adomeglivant is well tolerated by glucagon signaling blockade in patients with type 2 diabetes and significantly reduces fasting and postprandial blood glucose with a concomitant reversible elevation of aminotransferases. Glucagon signaling inhibition by (+/-)-Adomeglivant is a promising potential inhibitory approach for patients with type 2 diabetes and warrants further evaluation of its benefits and risks in longer clinical trials .
|
-
- HY-B0193AR
-
|
|
Reference Standards
Adrenergic Receptor
Autophagy
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Prazosin (hydrochloride) (Standard) is the analytical standard of Prazosin (hydrochloride). This product is intended for research and analytical applications. Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively .
|
-
- HY-153268
-
|
BDTX-1535; EGFR-IN-76
|
EGFR
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Silevertinib (BDTX-1535) is an irreversible, brain-penetrant, selective and orally active EGFR inhibitor with wild-type EGFR-sparing. Silevertinib targets key EGFR resistance mutations, including the kinase domain (C797S, L718Q, G724S, S768I), extracellular domain (EGFRvIII, A289X), and EGFR amplification. Silevertinib exerts anti-tumor activity with well tolerated in vivo. Silevertinib can be used for non-small cell lung cancer (NSCLC) and glioblastoma (GBM) research .
|
-
- HY-145603S
-
|
VX-121-d4
|
Isotope-Labeled Compounds
CFTR
Chloride Channel
|
Neurological Disease
|
|
Vanzacaftor-d4 (VX-121-d4) is the deuterium labeled Vanzacaftor (HY-145603). Vanzacaftor is an orally active noval corrector of Cystic fibrosis transmembrane conductance regulator (CFTR). Vanzacaftor improves processing and trafficking of CFTR protein as well as increases chloride transport in triple combined with Tezacaftor (HY-15448) and Deutivacaftor. Vanzacaftor-Tezacaftor-Deutivacaftor is safe and well tolerated, improving lung function, respiratory symptoms, and CFTR function with cystic fibrosis, which is promising for research in the field of cystic fibrosis diseases .
|
-
- HY-146019
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-24 (compound S-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 9.5 nM. HIV-1 inhibitor-24 has high antiretroviral activity against WT HIV-1 with an EC50 of 1.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 9.07 μM in MT-4 cells. HIV-1 inhibitor-24 is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety .
|
-
- HY-121621
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
RO5101576 is a potent LTB4 receptor antagonist with activity to inhibit LTB4-induced calcium mobilization and chemotaxis of human neutrophils. RO5101576 significantly attenuated LTB4-induced pulmonary eosinophilia in guinea pigs. RO5101576 inhibited allergen- and ozone-induced pulmonary neutrophilia in nonhuman primates with efficacy comparable to that of budesonide. RO5101576 had no effect on LPS-induced neutrophilia in guinea pigs and cigarette smoke-induced neutrophilia in mice and rats. RO5101576 performed well in toxicology studies and was well tolerated .
|
-
- HY-174406A
-
|
|
Myosin
PDGFR
Reactive Oxygen Species (ROS)
Ferroptosis
Akt
mTOR
ERK
|
Inflammation/Immunology
Cancer
|
|
MT-125 free base is a specific and well-tolerated inhibitor of non-muscle myosin IIA (Ki,NMIIA = 2.7 μM) and IIB (EC50 = 1.7 μM). MT-125 free base can pass through the blood-brain barrier. MT-125 free base induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 free base can enhance the PDGFR signaling pathway. MT-125 free base can be used for research on glioblastoma.
|
-
- HY-164388
-
Z-VAD
Maximum Cited Publications
19 Publications Verification
|
Caspase
Apoptosis
Autophagy
Necroptosis
|
Cardiovascular Disease
Cancer
|
|
Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation .
|
-
- HY-183708
-
|
|
Arenavirus
|
Infection
|
|
Antiviral agent 85 is a broad-spectrum arenavirus entry inhibitor with an EC90 of 0.13 µM against Junín virus (JUNV). Antiviral agent 85 blocks the entry of various arenaviruses through both hTfR1-dependent and hTfR1-independent pathways, acting on the early and early post-entry stages of infection. Antiviral agent 85 exhibits antiviral activity against a variety of arenaviruses, is well tolerated in hTfR1-expressing JUNV-infected mouse models, but fails to provide protective effects. Antiviral agent 85 can be used in studies related to arenavirus hemorrhagic fevers .
|
-
- HY-10122
-
|
KAD 3213; KMD 3213
|
Adrenergic Receptor
Bacterial
|
Endocrinology
Cancer
|
|
Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH .
|
-
- HY-10122S
-
|
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Endocrinology
Cancer
|
|
Silodosin-d4 is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH .
|
-
- HY-116880
-
|
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
DS-2969b is an orally active GyrB inhibitor with antibacterial activity. DS-2969b is is active against Clostridium difficile infection (MIC90: 0.06 μg/mL), which is 2-, 16-, and 32-fold lower than those of Fidaxomicin (HY-17580), Metronidazole (HY-B0318), and Vancomycin (HY-B0671), respectively. DS-2969b inhibits the supercoiling activity of C. difficile DNA gyrase. DS-2969b also exhibits activity against other Gram-positive anaerobes, including strict and facultative anaerobes. DS-2969b is safe and well tolerated in preclinical toxicology studies .
|
-
- HY-182774
-
|
|
CXCR
|
Cancer
|
|
YU241279 is an orally active CXCR5 inhibitor. YU241279 inhibits CXCL13-mediated Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells. YU241279 inhibits the proliferation of CXCR5-expressing lymphoma cells. YU241279 reduces tumor burden in the peripheral blood and bone marrow of mice implanted with lymphoma tissues. YU241279 is well tolerated during oral administration in mice, maintains stable plasma drug concentrations, and shows no metabolic changes. YU241279 can be used in the research of angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma .
|
-
- HY-10122R
-
|
KAD 3213 (Standard); KMD 3213 (Standard)
|
Reference Standards
Adrenergic Receptor
Bacterial
|
Endocrinology
Cancer
|
|
Silodosin (Standard) is the analytical standard of Silodosin. This product is intended for research and analytical applications. Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH .
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- HY-182241
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c-Myc
Early 2 Factor (E2F)
TNF Receptor
MDM-2/p53
Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
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JR4-187 is an orally active, copper-dependent anticancer agent. JR4-187 downregulates genes involved in oxidative phosphorylation, MYC targets and E2F targets in cancer cells, while upregulates genes involved in the TNF-α signaling pathway, p53 pathway and KRAS signaling pathway, and downregulates CTR1 protein . JR4-187 induces ROS production, apoptosis, copper-dependent cytotoxicity, and exhibits selective cytotoxicity against KRAS-mutant cancer cells. JR4-187 is well tolerated in mouse models of pancreatic cancer. JR4-187 can be used in research related to cancers such as pancreatic ductal adenocarcinoma, colon cancer and rectal cancer .
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- HY-174374
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Topoisomerase
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Cardiovascular Disease
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Topobexin is a TOP2B-selective inhibitor with IC50 values of 0.19 μM and 4.8 μM for TOP2B and TOP2A (DNA decatenation assay). Topobexin binds to non-homologous residues in the obex pocket and targets the ATPase domain of TOP2B. Topobexin prevents anthracycline-induced DNA double-strand break formation, apoptotic signaling mediated by caspase 3/7, 8 and 9, cardiomyocyte morphological changes, mitochondrial depolarization/loss, left ventricular systolic dysfunction, extracellular matrix remodeling, fibrotic alterations, and increases in plasma cardiac troponin T and BNP. Topobexin does not impair the antiproliferative effects of anthracyclines in cancer cells, exhibits no intrinsic cytotoxicity in cardiomyocytes, and is well tolerated in rabbits. Topobexin can be used in studies related to anthracycline-induced cardiotoxicity .
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- HY-179585
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Apoptosis
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Cancer
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DD-CIP2 is a DNA damage and apoptosis inducer. DD-CIP2 demonstrates effective anti-proliferative activity against multiple cancer cell. DD-CIP2 modulates the DNA damage response pathway, triggering robust DNA damage, cell cycle arrest, and apoptosis in vitro. DD-CIP2 demonstrates significant anti-tumor efficacy in vivo at well-tolerated doses, without substantial toxicity. DD-CIP2 exhibits superior cytotoxic potency against a broad panel of blood-and solid-tumor-derived cancer cell lines independent of their BRCA1/2 status. DD-CIP2 can be used for small-cell lung cancer (SCLC) and non small-cell lung cancer (NSCLC) research .
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- HY-174870
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PROTACs
Estrogen Receptor/ERR
Apoptosis
Fluorescent Dye
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Cancer
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PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)) .
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- HY-128866
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Bacterial
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Infection
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TBAJ-876 is an orally active diarylquinoline anti-Mycobacterium agent. TBAJ-876 regulates energy metabolism by targeting the c and ε subunits of Mycobacterium tuberculosis F-ATP synthase, exerts bactericidal activity against replicating Mycobacterium tuberculosis, and retains activity against strains carrying the Rv0678 mutation. TBAJ-876 undergoes N-demethylation in vivo to form its major active metabolite TBAJ-876-M3, which has lower lipophilicity and hERG potassium channel binding affinity. TBAJ-876 is well tolerated in BALB/c mice and significantly reduces the colony-forming units of Mycobacterium tuberculosis in the lungs. In addition, TBAJ-876 exhibits inhibitory activity against Mycobacterium abscessus, reduces bacterial loads in the lungs and spleens of infected mice, and shows no antagonistic effect when used in combination with common antibiotics. TBAJ-876 can be used in studies related to tuberculosis and Mycobacterium abscessus pulmonary diseases .
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| Cat. No. |
Product Name |
Type |
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- HY-16700G
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Fluorescent Dye
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PNU-159682 GMP is a GMP grade PNU-159682 (HY-16700). PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.
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| Cat. No. |
Product Name |
Type |
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- HY-16700G
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Biochemical Assay Reagents
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PNU-159682 GMP is a GMP grade PNU-159682 (HY-16700). PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-164388
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Z-VAD
Maximum Cited Publications
19 Publications Verification
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Caspase
Apoptosis
Autophagy
Necroptosis
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Cardiovascular Disease
Cancer
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Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation .
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- HY-P1682A
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POL6326 TFA
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CXCR
Arrestin
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Cancer
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Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
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- HY-126810A
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Fungal
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Infection
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NP213 TFA is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 TFA targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 TFA is effective and well-tolerated in resolving nail fungal infections .
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- HY-P1682
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POL6326
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CXCR
Arrestin
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Cancer
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Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
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- HY-126810
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Fungal
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Infection
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NP213 is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 is effective and well-tolerated in resolving nail fungal infections .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P99665
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LY-3209590
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Insulin Receptor
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Metabolic Disease
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Insulin efsitora alfa (LY-3209590) is a selective agonist of insulin receptor (IR). Insulin efsitora alfa is a fusion protein composed of human IR agonists fused with the crystallizable (Fc) domain of human immunoglobulin G2 (IgG2) fragment, with a molecular weight of 64.1 kDa. Insulin efsitora alfa is well tolerated and has potential applications in diabetes .
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(5)
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- HY-P990966
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JR-142
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GHR
IGF-1R
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Others
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Redalsomatropin alfa (JR-142) is a recombinant long-acting growth hormone. Redalsomatropin alfa extends its half-life through fusion with modified serum albumin. Redalsomatropin alfa is well-tolerated and can maintain IGF-1 levels. Redalsomatropin alfa can be used in research related to growth hormone deficiency .
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(5)
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- HY-112935
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BAX326; Coagulation Factor IX [Recombinant]; BeneFIX
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Ser/Thr Protease
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Others
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Nonacog alfa (BAX326) is a recombinant human factor IX that can be used for the research of haemophilia B .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-B1804S
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Tricaprilin- 13C3 (Trioctanoin- 13C3) is a 13C-labeled Tricaprilin (HY-B1804) . Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
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- HY-145603S
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Vanzacaftor-d4 (VX-121-d4) is the deuterium labeled Vanzacaftor (HY-145603). Vanzacaftor is an orally active noval corrector of Cystic fibrosis transmembrane conductance regulator (CFTR). Vanzacaftor improves processing and trafficking of CFTR protein as well as increases chloride transport in triple combined with Tezacaftor (HY-15448) and Deutivacaftor. Vanzacaftor-Tezacaftor-Deutivacaftor is safe and well tolerated, improving lung function, respiratory symptoms, and CFTR function with cystic fibrosis, which is promising for research in the field of cystic fibrosis diseases .
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- HY-B1895S
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Levodropropizine-d8 is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is a histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.
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- HY-B0265S
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Nimodipine-d7 is the deuterium labeled Nimodipine. Nimodipine (BAY-e 9736) is an orally active, well-tolerated and light-sensitive dihydropyridine calcium antagonist. Nimodipine can be used for the research of cerebrovascular disorders .
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- HY-B1895S1
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Levodropropizine-d5 ((S)-(-)-Dropropizine-d5) is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent .
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- HY-109523S
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Cerivastatin-d3 sodium is deuterated labeled Cerivastatin sodium (HY-109523). Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
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- HY-B1804S1
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Tricaprilin-d50 (Trioctanoin-d50) is the deuterium labeled Tricaprilin (HY-B1804). Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
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- HY-B1804S2
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Tricaprilin-d15 (Trioctanoin-d15) is the deuterium labeled Tricaprilin (HY-B1804). Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
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- HY-10122S
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Silodosin-d4 is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH .
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| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-16700G
-
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ADC Payload
Topoisomerase
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Cancer
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PNU-159682 GMP is a GMP grade PNU-159682 (HY-16700). PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.
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-
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