Search Result
Results for "
well tolerated
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-109148
-
|
TD-1473; JNJ-8398
|
JAK
|
Inflammation/Immunology
|
|
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 .
|
-
-
- HY-B1895
-
-
-
- HY-16487
-
|
TMFX; TA-167 free acid; A-62254 free acid
|
Bacterial
Antibiotic
|
Infection
|
|
Temafloxacin (TMFX) is an orally active quinolone broad-spectrum antibacterial agent. Temafloxacin is well tolerated in lower respiratory and genitourinary tract infections .
|
-
-
- HY-B0265
-
-
-
- HY-14834
-
-
-
- HY-163460
-
-
-
- HY-128386
-
-
-
- HY-A0287
-
|
Clomiphene
|
Others
|
Endocrinology
|
|
Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation .
|
-
-
- HY-A0287A
-
|
Clomiphene hydrochloride
|
Others
|
Endocrinology
|
|
Clomifene hydrochloride is an orally active compound used for infertility. Clomifene hydrochloride is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation .
|
-
-
- HY-113595
-
|
TMFX hydrochloride; TA-167; A-62254
|
Antibiotic
Bacterial
|
Infection
|
|
Temafloxacin (TMFX) hydrochloride is an orally active quinolone broad-spectrum antibacterial agent. Temafloxacin hydrochloride is well tolerated in lower respiratory and genitourinary tract infections .
|
-
-
- HY-103262
-
-
-
- HY-121307
-
|
|
Others
|
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-125999
-
|
|
Others
|
Neurological Disease
|
|
EPI-589, a quinone derivative, is a safe and well tolerated oxidoreductase enzyme inhibitor. EPI-589 has the potential for the treatment of amyotrophic lateral sclerosis (ALS) .
|
-
-
- HY-B1895S
-
-
-
- HY-122620
-
|
Hetrombopag (tautomerism); SHR-8735 (tautomerism)
|
Thrombopoietin Receptor
|
Inflammation/Immunology
Cancer
|
|
Rafutrombopag (tautomerism) is a potent thrombopoietin receptor agonist. Rafutrombopag (tautomerism) is efficacious and well tolerated with a manageable safety profile. Rafutrombopag (tautomerism) has the potential for the research of immune thrombocytopenia .
|
-
-
- HY-14135
-
|
BMS 043
|
HIV
|
Infection
Inflammation/Immunology
|
|
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 .
|
-
-
- HY-102036
-
|
|
Btk
|
Inflammation/Immunology
|
|
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 .
|
-
-
- HY-129650
-
|
AV-45
|
Others
|
Others
|
|
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 .
|
-
-
- 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
-
|
|
Others
|
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-107176A
-
|
HS-25
|
Others
|
Metabolic Disease
|
|
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 .
|
-
-
- 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-A0287S
-
|
Clomiphene-d5 (hydrochloride)
|
Isotope-Labeled Compounds
|
Others
|
|
Clomifene-d5 (hydrochloride) is a deuterium labeled Clomifene. Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation[1].
|
-
-
- HY-N1373
-
|
|
Apoptosis
|
Cancer
|
|
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-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-B0265S
-
|
|
Autophagy
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
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[1].
|
-
-
- HY-B1895R
-
|
|
Histamine Receptor
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Levodropropizine (Standard) is the analytical standard of Levodropropizine. This product is intended for research and analytical applications. Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent .
|
-
-
- HY-18317
-
|
|
VEGFR
RET
c-Kit
|
Cancer
|
|
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 .
|
-
-
- HY-148772
-
|
|
Others
|
Neurological Disease
|
|
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 .
|
-
-
- HY-16487R
-
|
|
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
-
|
|
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-107495
-
|
NSC19005
|
Histamine Receptor
|
Inflammation/Immunology
|
|
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-124674A
-
|
|
Monoamine Oxidase
EGFR
Akt
TGF-beta/Smad
|
Cancer
|
|
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 .
|
-
-
- HY-123490
-
|
INS50589
|
P2Y Receptor
|
Inflammation/Immunology
|
|
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 .
|
-
-
- HY-105040
-
|
LY2140023 hydrate
|
mGluR
|
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 .
|
-
-
- HY-N7393
-
|
Palatinitol
|
Lactate Dehydrogenase
|
Metabolic Disease
|
|
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-16976
-
|
|
Pim
|
Cancer
|
|
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 .
|
-
-
- HY-101560
-
|
BMS-986205; ONO-7701
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
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-N1373A
-
|
(+)-Sophoridine
|
Apoptosis
|
Cancer
|
|
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 .
|
-
-
- HY-N1373R
-
|
|
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-126810
-
|
|
Fungal
|
Infection
|
|
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 .
|
-
-
- 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-117290
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity .
|
-
-
- 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-B1804
-
|
Trioctanoin; Glyceryl trioctanoate
|
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
|
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) .
|
-
-
- HY-126810A
-
|
|
Fungal
|
Infection
|
|
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 .
|
-
-
- HY-122347A
-
|
GW823296 maleate
|
Neurokinin Receptor
|
Neurological Disease
|
|
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 .
|
-
-
- HY-109523
-
|
|
HMG-CoA Reductase (HMGCR)
Ferroptosis
|
Cardiovascular Disease
Cancer
|
|
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-112081
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
BAY-707 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 .
|
-
- HY-161672
-
|
|
Liposome
IRE1
|
Cancer
|
|
G-5758 is an orally available IRE1α inhibitor with an IC50 of 38 nM for XBP1s. G-5758 is well tolerated in multiple myeloma models (KMS-11) at oral doses up to 500 mg/kg in rats. G-5758 exhibits pharmacodynamics comparable to that of induced IRE1 knockdown .
|
-
- HY-100375
-
|
ALKS 8700; BIIB098
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
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-129458
-
|
|
HMG-CoA Reductase (HMGCR)
Ferroptosis
|
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 .
|
-
- HY-114237
-
|
|
Sodium Channel
|
Neurological Disease
|
|
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 .
|
-
- HY-121212
-
|
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
|
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 .
|
-
- HY-151174
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
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) .
|
-
- HY-N7393R
-
|
|
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-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-145603
-
|
VX-121
|
CFTR
Chloride Channel
|
Neurological Disease
|
|
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 .
|
-
- HY-114331
-
|
|
MAP3K
|
Neurological Disease
|
|
DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease.
|
-
- HY-P99665
-
|
LY-3209590
|
Insulin Receptor
|
Metabolic Disease
|
|
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 .
|
-
- HY-107345
-
|
Ombolan
|
Others
|
Inflammation/Immunology
|
|
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-122611
-
|
|
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
|
-
- HY-122611A
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
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
|
-
- HY-112163A
-
|
rel-eFT226
|
Eukaryotic Initiation Factor (eIF)
SARS-CoV
Apoptosis
|
Infection
Cancer
|
|
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-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-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-117621
-
|
|
CCR
|
Metabolic Disease
|
|
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 .
|
-
- 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-P1682
-
|
POL6326
|
CXCR
Arrestin
|
Cancer
|
|
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-117621A
-
|
|
CCR
|
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-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 .
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- HY-B0193A
-
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|
Adrenergic Receptor
Autophagy
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
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-103019E
-
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BAY-1251152; VIP152
|
Others
|
Others
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|
Enitociclib (VIP152; BAY-1251152) is a selective CDK9 inhibitor. Known for its unique benzyl sulfoxide moiety, VIP152 has demonstrated promising efficacy and tolerability both in vitro and in vivo, including in mouse and rat xenograft models via weekly intravenous infusions Highly effective and well tolerated. VIP152 shows promising long-term single-agent inhibitory activity against double-click refractory diffuse large B-cell lymphoma .
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- HY-116149
-
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Others
|
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.
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- HY-117287A
-
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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 .
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- HY-121621
-
|
|
Others
|
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 .
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- HY-16712
-
|
|
TGF-β Receptor
|
Cancer
|
|
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) [2]
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- HY-P1682A
-
|
POL6326 TFA
|
CXCR
Arrestin
|
Cancer
|
|
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 .
|
-
- HY-112163
-
|
eFT226
|
Eukaryotic Initiation Factor (eIF)
SARS-CoV
Apoptosis
|
Infection
Cancer
|
|
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 .
|
-
- 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-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 .
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-
- HY-B0193AR
-
|
|
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-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-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[1][3].
|
-
- HY-10122R
-
|
|
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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-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-126810A
-
|
|
Fungal
|
Infection
|
|
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 .
|
-
- HY-P1682A
-
|
POL6326 TFA
|
CXCR
Arrestin
|
Cancer
|
|
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 .
|
-
- HY-P1682
-
|
POL6326
|
CXCR
Arrestin
|
Cancer
|
|
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 .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99665
-
|
LY-3209590
|
Insulin Receptor
|
Metabolic Disease
|
|
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 .
|
-
- HY-112935
-
|
BAX326; Coagulation Factor IX [Recombinant]
|
Inhibitory Antibodies
|
Others
|
|
Nonacog alfa (BAX326) is a recombinant human factor IX that can be used for the research of haemophilia B .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0265S
-
|
|
|
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[1].
|
-
-
- HY-B1895S
-
|
|
|
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.
|
-
-
- HY-A0287S
-
|
|
|
Clomifene-d5 (hydrochloride) is a deuterium labeled Clomifene. Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation[1].
|
-
-
- HY-109523S
-
|
|
|
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-10122S
-
|
|
|
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[1][3].
|
-
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