Search Result
Results for "
clinical isolates
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-10844
-
|
PA-824; (S)-PA 824
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
|
-
-
- HY-111964
-
Lenacapavir
Maximum Cited Publications
19 Publications Verification
GS-6207
|
HIV
|
Infection
|
|
Lenacapavir (GS-6207) is an HIV-1 capsid inhibitor. Lenacapavir binds to the interface between capsid hexamers and CA monomers, disrupts capsid assembly and viral maturation, inhibits nuclear translocation of HIV-1 DNA, interferes with CA-mediated protein-protein interactions, reduces the formation of 2-LTR circles and pre-integration proviruses, induces aberrant capsids, and decreases the production of mature HIV-1. Lenacapavir exhibits activity against a variety of HIV-1 subtypes and clinical isolates. Lenacapavir is applicable to research related to human immunodeficiency virus type 1 (HIV-1) infection .
|
-
-
- HY-17040
-
|
TMC114; UIC-94017
|
HIV
HIV Protease
|
Infection
Inflammation/Immunology
|
|
Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity .
|
-
-
- HY-B1005
-
|
8-Quinolinol
|
Environmental Pollutants
Antibiotic
Bacterial
|
Cancer
|
|
8-Hydroxyquinoline (8-Quinolinol) is a lipophilic metal chelator that can be used as a fungicide .8-Hydroxyquinoline shows the MIC range of 27.56-55.11 μM (4-8 μg/mL) against the clinical isolates of Neisseria gonorrhoeae. 8-Hydroxyquinoline can bind to copper form complexes and transport copper into cells. 8-Hydroxyquinoline increases in the number of micronucleated polychromatic erythrocytes and can also make hair depigmented in mice .
|
-
-
- HY-16911
-
|
API-1252; Debio 1452
|
Bacterial
Antibiotic
|
Infection
|
|
AFN-1252 is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 exhibits typical MIC90 values of ⩽0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith .
|
-
-
- HY-N2340
-
|
(+)-Melezitose; D-Melezitose
|
Bacterial
|
Infection
|
|
D-(+)-Melezitose can be used to identify clinical isolates of indole-positive and indole-negative Klebsiella spp.
|
-
-
- HY-12993
-
RSV604
2 Publications Verification
A-60444
|
RSV
|
Infection
|
|
RSV604 (A-60444) is an inhibitor of respiratory syncytial virus (RSV) replication. RSV604 targets the nucleocapsid protein, with a Kd of 1.6 μM. RSV604 displays submicromolar activity against numerous clinical isolates of both the A and B subtypes of RSV (average EC50s=0.8 μM) .
|
-
-
- HY-139602
-
|
|
Flavivirus
Dengue Virus
Virus Protease
|
Infection
|
|
(+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models .
|
-
-
- HY-122587
-
|
|
DNA/RNA Synthesis
RSV
|
Infection
|
|
AVG-233 is a potent, orally active RNA dependent RNA polymerase (RdRp) inhibitor. AVG-233 prevents initiation of the viral polymerase complex at the promoter. AVG-233 binding site is present in the L1-1749 fragment. AVG-233 has nanomolar activity against both RSV strains and clinical RSV isolates (EC50=0.14-0.31 μM). AVG-233 can be used for research of respiratory syncytial virus (RSV) .
|
-
-
- HY-N125722
-
|
Aabomycin A1
|
ATP Synthase
Antibiotic
|
Infection
|
|
Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL.
|
-
-
- HY-159828
-
|
VH-499; VH4011499
|
HIV
|
Infection
|
|
Dezecapavir (VH-499) is a HIV-1 capsid protein inhibitor. Dezecapavir exhibits picomolar-level antiviral activity against a variety of HIV-1 laboratory strains and clinical isolates in vitro. Dezecapavir inhibits the early and late stages of the HIV-1 life cycle, blocking nuclear import, reverse transcript production, virion assembly, maturation, and post-nuclear import/pre-integration replication processes. Dezecapavir can be used in studies related to HIV-1 infection .
|
-
-
- HY-111964A
-
|
GS-6207 sodium
|
HIV
|
Infection
|
|
Lenacapavir (GS-6207) sodium is an HIV-1 capsid inhibitor. Lenacapavir sodium binds to the interface between capsid hexamers and CA monomers, disrupts capsid assembly and viral maturation, inhibits nuclear translocation of HIV-1 DNA, interferes with CA-mediated protein-protein interactions, reduces the formation of 2-LTR circles and pre-integration proviruses, induces aberrant capsids, and decreases the production of mature HIV-1. Lenacapavir sodium exhibits activity against a variety of HIV-1 subtypes and clinical isolates. Lenacapavir sodium is applicable to research related to human immunodeficiency virus type 1 (HIV-1) infection .
|
-
-
- HY-122470
-
|
|
Reverse Transcriptase
HIV
|
Infection
|
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively .
|
-
-
- HY-10844R
-
|
PA-824 (Standard); (S)-PA 824 (Standard)
|
Reference Standards
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Pretomanid (Standard) is the analytical standard of Pretomanid. This product is intended for research and analytical applications. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
|
-
-
- HY-162066
-
|
|
Parasite
|
Infection
|
|
DNDI-6174 is an orally active Leishmania cytochrome b (Qi site of cytochrome bc1 complex/complex III) inhibitor. DNDI-6174 binds to the Qi site of Leishmania cytochrome b, inhibits cytochrome bc1 complex activity in the parasite's electron transport chain across promastigote and axenic amastigote stages. DNDI-6174 reduces parasite burden in rodent models, inhibits growth of various Leishmania species, drug-resistant clinical isolates, and Trypanosoma cruzi, with marginal activity against Trypanosoma brucei. DNDI-6174 can be used for the research of visceral leishmaniasis, cutaneous leishmaniasis .
|
-
-
- HY-13053
-
|
Ro-0335
|
Reverse Transcriptase
|
Cancer
|
|
RO-0335 is a novel and potent diphenylether nonnucleoside reverse transcriptase inhibitor(NNRTI). RO-0335 inhibits Wt HIV-1 with an IC50 of 1.1 nM and retained activity (IC50< 100 nM) against 92% of a large number of NNRTI-resistant clinical isolates .
|
-
-
- HY-14891
-
|
GSK2248761; FDV
|
HIV
Reverse Transcriptase
|
Infection
|
|
Fosdevirine (GSK2248761) is is a potent, selective, non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1) replication with low nanomolar activity in vitro. Fosdevirine shows good activity against a broad range of HIV-1 strains, including efavirenz (HY-10572)-resistant clinical isolates .
|
-
-
- HY-10844S1
-
|
PA-824-d5; (S)-PA 824-d5
|
Antibiotic
Bacterial
Isotope-Labeled Compounds
|
Infection
Cancer
|
|
Pretomanid-d5 is deuterated labeled Pretomanid (HY-10844). Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
|
-
-
- HY-N2340A
-
|
(+)-Melezitose hydrate; D-Melezitose hydrate
|
Bacterial
|
Infection
|
|
D-(+)-Melezitose hydrate ((+)-Melezitose hydrate) can be used to identify clinical isolates of indole-positive and indole-negative Klebsiella spp .
|
-
-
- HY-135184
-
|
CBR-2092; TNP-2092
|
Antibiotic
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
Rifaquizinone (CBR-2092) is a Rifamycin-Quinolone Hybrid Antibiotic. Rifaquizinone inhibits wild-type S. aureus RNA polymerase with an IC50 of 34 nM. Rifaquizinone is effective against S. aureus infections, with MICs ranged from 0.008 to 0.5 μg/mL for 300 clinical isolates of staphylococci and streptococci .
|
-
-
- HY-P11080
-
|
|
Bacterial
|
Infection
|
|
Oncocin is an antibacterial peptide. It belongs to proline-rich antimicrobial peptides (PrAMPs). Oncocin works against Gram-negative bacteria. It has MIC values of 0.125-8 μg/mL for 34 strains and clinical isolates of Enterobacteriaceae and nonfermenters. Oncocin binds to the substrate-binding domain of the chaperone DnaK. The binding has dissociation constants in the micromolar range. This binding causes protein misfolding and aggregation and the bacteria death .
|
-
-
- HY-10844S
-
|
|
Isotope-Labeled Compounds
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Pretomanid-d4 is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL .
|
-
-
- HY-139698
-
|
LCB10-0200
|
Antibiotic
Bacterial
|
Infection
|
|
GT-1 (LCB10-0200), a siderophore-linked cephalosporin, is effective against clinical isolates of P. aeruginosa, Klebsiella oxytoca, Proteus spp., Serratia marcescens, and Enterobacter aerogenes.
|
-
-
- HY-123022
-
|
CS-023; RO4908463; R-115685
|
Bacterial
|
Infection
|
|
Tomopenem (CS-023; RO4908463; R-115685) is a longer-half-life parenteral carbapenem. Tomopenem shows broad activity against 63 reference species. The activity of tomopenem against 293 clinical isolates is potent (MIC90, 0.06 to 4 μg/mL). Antianaerobic activity .
|
-
-
- HY-P11191
-
|
|
Bacterial
|
Infection
|
|
AR-23 is a melittin-related antimicrobial peptide that can be isolated from Rana tagoi. AR-23 exhibits broad-spectrum growth inhibitory activity against aerobic bacteria, the opportunistic yeast pathogen Candida albicans and clinical isolates of Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA). AR-23 can be used for antimicrobial research .
|
-
-
- HY-16745A
-
|
KRP-AM1977 hydrochloride
|
Bacterial
|
Infection
|
|
Lascufloxacin (KRP-AM1977) hydrochloride is a potent antibacterial compound candidate with broad-spectrum activity against various clinical isolates. Lascufloxacin hydrochloride shows the most potent activity against Gram-positive bacteria compared to other tested quinolones. Lascufloxacin hydrochloride demonstrates incomplete cross-resistance against existing quinolone-resistant strains. Lascufloxacin hydrochloride has potent inhibitory activity against both wild-type and mutated target enzymes.
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-
-
- HY-17040R
-
|
TMC114 (Standard); UIC-94017 (Standard)
|
HIV
HIV Protease
Reference Standards
|
Infection
Inflammation/Immunology
|
|
Darunavir (Standard) is the analytical standard of Darunavir. This product is intended for research and analytical applications. Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity .
|
-
-
- HY-B1005R
-
|
8-Quinolinol (Standard)
|
Reference Standards
Bacterial
Antibiotic
|
Cancer
|
|
8-Hydroxyquinoline (Standard) is the analytical standard of 8-Hydroxyquinoline. This product is intended for research and analytical applications. 8-Hydroxyquinoline (8-Quinolinol) is a lipophilic metal chelator that can be used as a fungicide .8-Hydroxyquinoline shows the MIC range of 27.56-55.11 μM (4-8 μg/mL) against the clinical isolates of Neisseria gonorrhoeae. 8-Hydroxyquinoline can bind to copper form complexes and transport copper into cells. 8-Hydroxyquinoline increases in the number of micronucleated polychromatic erythrocytes and can also make hair depigmented in mice .
|
-
-
- HY-117845
-
|
LL-E19085α
|
Antibiotic
Bacterial
|
Infection
|
|
Citreamicin alpha (LL-E 19085-alpha) is an antibiotic whose in vitro antimicrobial activity against 429 clinical isolates of Gram-positive cocci has been tested by the agar dilution method. These microorganisms included 313 strains of Staphylococci and 116 strains of Streptococci. The in vitro activity of Citreamicin alpha was compared with that of ampicillin, amoxicillin, ceftriaxone, erythromycin, and vancomycin. For Staphylococci, the MIC values of Citreamicin alpha ranged from 0.12-4.0 μg/ml, and for Streptococcus pyogenes of the genus Streptococcus, it was 0.03-0.12 μg/ml. However, enterococci were relatively resistant, requiring 2.0 μg/ml of the agent to inhibit 64% of the 62 tested strains. The in vitro activity of this antibiotic was much better than that of ampicillin, amoxicillin, ceftriaxone, and erythromycin, but comparable or slightly inferior to that of vancomycin.
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-
-
- HY-178949
-
|
|
Antibiotic
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
MRSA antibiotic 3 (Compound C8) is a small-molecule antibiotic active against Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA), showing a MIC of 0.5 μg/mL against the standard S. aureus strain (ATCC 29213). MRSA antibiotic 3 potently inhibits the ATPase activity of S. aureus DNA gyrase with an IC50 of 0.32 μM. MRSA antibiotic 3 exhibits strong inhibitory activity against five clinical MRSA isolates, with MIC values ranging from 0.5 to 1 μg/mL. MRSA antibiotic 3 demonstrates negligible cytotoxicity at effective antibacterial concentrations and causes no hemolysis in erythrocytes even at extremely high concentrations. MRSA antibiotic 3 shows significant protective effects in both Galleria mellonella infection and murine sepsis models .
|
-
-
- HY-N2340R
-
|
(+)-Melezitose (Standard); D-Melezitose (Standard)
|
Reference Standards
Bacterial
|
Infection
|
|
D-(+)-Melezitose can be used to identify clinical isolates of indole-positive and indole-negative Klebsiella spp.
|
-
-
- HY-168123
-
|
|
Bacterial
|
Cancer
|
|
Antitubercular agent-47 (compund 5C) shows potent activity against tuberculosis and was effective against DS/MDR/XDR clinical isolates .
|
-
-
- HY-129166
-
|
|
Bacterial
|
Infection
|
|
UCM53, a FtsZ inhibitor, is an antibacterial agent. UCM53 can inhibit the growth of clinical isolates of antibiotic-resistant Staphylococcus aureus and Enterococcus faecalis
|
-
-
- HY-123175
-
|
|
Bacterial
|
Others
|
|
Chinfloxacin is a compound with antibacterial activity. It is active against a variety of clinical isolates in vitro. Its antibacterial activity is similar to that of moxifloxacin, and it has a bactericidal effect in a concentration-dependent manner.
|
-
-
- HY-147871
-
|
|
Bacterial
|
Infection
|
|
Antimycobacterial agent-3 (Compound 1h) is an antimycobacterial agent against both agent-sensitive MTB strain H37Rv and drug-resistant clinical isolates (MIC: < 0.029–0.110 μM). Antimycobacterial agent-3 shows low cell cytotoxicity .
|
-
-
- HY-162527
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 216 (Compound 2a) is an antibacterial agent that exhibits significant bactericidal effects when combined with INH and RIF. Antibacterial agent 216 has demonstrated remarkable in vitro anti-tuberculosis activity against Mtb H37Rv and MDR clinical isolates and can be used for tuberculosis research .
|
-
-
- HY-155190
-
|
|
Bacterial
|
Infection
|
|
Antitubercular agent-39 (Compound P1) is a potent antitubercular agent. Antitubercular agent-39 is active against drug-resistant strains and drug-susceptible clinical isolates. Antitubercular agent-39 inhibits Mtb strain H37Rv with a MIC less than 1 μM .
|
-
-
- HY-173355
-
|
|
Bacterial
|
Infection
|
|
RCB18350 is an antituberculosis agent that belongs to the class of isoxazole derivatives. RCB18350 has bacteriostatic activity and inhibits the growth of Mycobacterium tuberculosis with an MIC of 1.25 μg/mL. RCB18350 is effective against multidrug-resistant Mycobacterium tuberculosis (MDR-TB) clinical isolates, slow-growing mycobacteria such as Mycobacterium bovis BCG and Mycobacterium avium .
|
-
-
- HY-138074
-
|
5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
|
Parasite
|
Infection
|
|
Milbemycin A4 oxime (5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime) is a derivative of Milbemycin A4 (HY-126906) and a component of Milbemycin oxime (HY-B0778), both of which have insecticidal and nematicidal activities. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae in naturally infected dogs with D. immitis and inhibits the growth of clinical isolates of Candida glabrata (MIC80=16-32 μg/mL). Milbemycin A4 oxime (2.5 μg/mL) blocks the efflux of Fluconazole (HY-B0101) from clinical isolates of Candida glabrata. Milbemycin A4 oxime enhances doxorubicin-induced cell growth inhibition and increases the intracellular accumulation of doxorubicin and P-glycoprotein substrate Rhodamine 123 (HY-D0816) in doxorubicin-resistant but not sensitive MCF-7 breast cancer cells in a concentration-dependent manner.
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-
-
- HY-149581
-
|
|
Bacterial
|
Infection
|
|
DprE1-IN-9 (compound B18) is an effective reversible DprE1 inhibitor and can bind to the receptor cavity of DprE1. DprE1-IN-9 shows strong antimycobacterial activity not only against non-pathogenic strain H37Ra (MIC=0.18 µg/mL) but also against pathogenic H37Rv and the clinical MDR and XDR isolates .
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-
-
- HY-162493
-
|
|
Bacterial
|
Infection
|
|
MBL-IN-3 (compound 72922413) is a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor(IC50=54±4 μM). MBL-IN-3 is identified and shown to lower minimum inhibitory concentrations (MICs) of Meropenem (HY-13678) for a panel of E. coli and K. pneumoniae clinical isolates expressing NDM-1. MBL-IN-3 can be used for antibiotic sensitizer research .
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-
-
- HY-105097
-
|
U 87201E mesylate
|
HIV
Reverse Transcriptase
|
Inflammation/Immunology
|
|
Atevirdine (U 87201E) mesylate is a nonnucleoside reverse transcriptase (NNRT) inhibitor. Atevirdine mesylate can inhibit human immunodeficiency virus type 1 (HIV-1) with an IC50 of 0.06-1.6 μM. Atevirdine mesylate shows highly synergistic effects against Zidovudine/Didanosine-resistant clinical isolates of HIV-1 companied with Zidovudine (HY-17413)/Didanosine (Hy-B0249). Atevirdine mesylate can be used for the research of AIDS .
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-
-
- HY-112585
-
|
TMC114-d9; UIC-94017-d9
|
HIV
HIV Protease
|
Infection
Inflammation/Immunology
|
|
Darunavir-d9 (TMC114-d9) is the deuterium labeled Darunavir. Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity .
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-
-
- HY-173277
-
|
|
Bacterial
|
Infection
|
|
FtsZ-IN-13 (Compound C11) is an inhibitor of temperature-sensitive mutant Z (FtsZ), with IC50 values of 47.97, 34 μM against FtsZSa and FtsZPa, respectively. FtsZ-IN-13 has a notable antimicrobial activity against S. aureus (minimum inhibitory concentration value of 2 μg/mL), cystic fibrosis S. aureus clinical isolates, and methicillin-resistant S. aureus (MRSA) strains. FtsZ-IN-13 can be used for antimicrobial resistance study .
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-
-
- HY-114622
-
|
API-1252 tosylate; Debio 1452 tosylate
|
Bacterial
Antibiotic
|
Infection
|
|
AFN-1252 (API-1252) tosylate is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 tosylate exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 tosylate exhibits typical MIC90 values of 0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 tosylate is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith .
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-
-
- HY-W773487
-
|
|
Bacterial
|
Infection
|
|
FtsZ-IN-10 is a bacterial division inhibitor that interferes with the normal assembly of FtsZ. FtsZ-IN-10 specifically binds to Bacillus subtilis FtsZ monomers, thereby affecting their polymerization behavior. FtsZ-IN-10 may also activate nucleotide-free archaeal FtsZ to form ordered polymers. FtsZ-IN-10 can hinder the localization of FtsZ in the Z ring and inhibit bacterial cell division. Chlorinated analogs of FtsZ-IN-10 show the ability to inhibit the growth of antibiotic-resistant clinical isolates such as Staphylococcus aureus and Enterococci .
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-
-
- HY-175724
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
MBL-IN-6 (Compound 6d) is a Metallo-β-lactamase (MBL) inhibitor with Kis of 2.6 and 0.08 μM for NDM-1 and VIM-2, respectively. MBL-IN-6 has a synergistic activities with Imipenem (HY-B1369A) on MBL-producing clinical isolates (such as E. coli SI-M001, K. pneumonia T2301 and S. marcescens SI-1591) with MICs of 2-64 μg/mL. MBL-IN-6 does not have off-target effects without ACE-1 inhibition activity. MBL-IN-6 can be used for antimicrobial resistance research .
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-
-
- HY-122058
-
|
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HIV
|
Infection
|
|
KRH-3955 is a CXCR4 antagonist with good bioavailability and potent anti-HIV-1 activity. KRH-3955 can effectively inhibit the replication of X4 HIV-1, including clinical isolates from different donors. KRH-3955 also shows activity against recombinant X4 HIV-1 containing reverse transcriptase, protease and tyrosinase resistance mutations. KRH-3955 can inhibit the binding of SDF-1alpha to CXCR4 and calcium ion signaling through this receptor. KRH-3955 inhibits the binding of an antibody against CXCR4 to CXCR4, showing a potent antagonistic effect on CXCR4. KRH-3955 shows an oral bioavailability of 25.6% in rats and can inhibit the replication of X4 HIV-1 in vivo .
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-
-
- HY-167690
-
|
|
Endogenous Metabolite
|
Infection
|
|
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
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-
-
- HY-182444
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Cefaloram is a cephalosporin antibiotic, but it is inactive against clinical cystic fibrosis isolates of Pseudomonas aeruginosa (MIC50 > 128 μg/mL) .
|
-
- HY-182684
-
|
|
Bacterial
Dihydrofolate reductase (DHFR)
|
Infection
|
|
MMV675968 is an inhibitor of Acinetobacter baumannii dihydrofolate reductase (AbDHFR) with an IC50 of 8.5 nM, and it exhibits selectivity against human DHFR. MMV675968 inhibits dihydrofolate reductase in Cryptosporidium, Plasmodium, and Escherichia coli, disrupting the thymidylate cycle and folate biosynthesis pathway. MMV675968 inhibits the growth of multiple A. baumannii strains, including clinical isolates and environmental isolates. MMV675968 is applicable to research related to A. baumannii infections .
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-
- HY-19281
-
|
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HIV Protease
HIV
|
Infection
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DMP-851 is a cyclic urea HIV protease inhibitor, with a Ki of 0.021 nM. DMP-851 shows antiviral activity against laboratory strains of HIV-l and HIV-2 as well as against primary clinical isolates derived from Zidovudine (HY-17413)-resistant samples (A018C, E, WR 10983) .
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- HY-183053
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Bacterial
Dihydrofolate reductase (DHFR)
Antifolate
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Infection
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UCP1173, propargyl-linked antifolate, is an antibacterial agent. UCP1173 inhibits DHFR enzymes, with IC50 values of 0.014 μM for DfrB, 0.19 μM for DfrG, 0.27 μM for DfrA, and 0.091 μM for DfrK. UCP1173 inhibits growth of Staphylococcus aureus clinical isolates carrying dfrA, dfrG, or dfrK resistance genes. UCP1173 can be used for the research of bacterial infections .
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- HY-182683
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Parasite
TrxR
Reactive Oxygen Species (ROS)
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Infection
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MMV085203 is a potent Plasmodium falciparum inhibitor, with a PfTrxR EC50 of 900 nM. MMV085203 exerts potent antimalarial activity against both blood‑stage and sexual‑stage Plasmodium falciparum parasites, with superior efficacy toward clinical isolates of high clonal diversity. MMV085203 modulates parasite redox homeostasis, induces ROS production, and elevates mitochondrial TCA cycle intermediates. MMV085203 can be used for the research of malaria .
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- HY-180191
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Bacterial
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
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Infection
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Anti-MRSA agent 42 (Compound 6d) is an anti-methicillin-resistant Staphylococcus aureus (MRSA) agent. Anti-MRSA agent 42 shows strong inhibitory effects on MRSA standard strains and 11 clinical isolates with MIC values of 0.25-0.5 μg/mL. Anti-MRSA agent 42 has low hemolytic activity and minimal cytotoxicity toward mammalian cells. Anti-MRSA agent 42 can suppress biofilm formation, compromise the cell wall, and disrupt the cytoplasmic membrane, which are accompanied by membrane depolarization, enhanced permeability, and loss of membrane integrity. Anti-MRSA agent 42 can induce ROS production and bind to DNA grooves, interfering with nucleic acid function. Anti-MRSA agent 42 can be used for the research of MRSA infection .
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- HY-181286
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Cytochrome P450
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Infection
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ETX1975-3 is an orally active inhibitor and bactericide targeting the bd cytochrome oxidase of Mycobacterium tuberculosis. ETX1975-3 disrupts electron transfer between the b-heme centers of the target enzyme, and in combination with Q203 (HY-101040), exerts bactericidal activity against both replicating and non-replicating Mycobacterium tuberculosis, and reduces bacterial loads in acute mouse models. ETX1975-3 retains activity against clinical isolates of multidrug-resistant/extensively drug-resistant Mycobacterium tuberculosis and non-tuberculous mycobacteria, while possessing favorable preclinical ADMET properties. ETX1975-3 can be used in studies related to tuberculosis and non-tuberculous mycobacterial infections .
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- HY-182685
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Acetyl-CoA synthetase
Parasite
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Infection
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MMV693183 is an orally active inhibitor of Plasmodium falciparum acetyl-CoA synthetase (AcAS), with an IC50 of 300 nM against Plasmodium falciparum. MMV693183 exhibits potent inhibitory activity against clinical isolates of malaria parasites, including Artemisinin (HY-B0094)-resistant strains. MMV693183 is metabolized in vivo into the active antimetabolite CoA-MMV693183, which exerts effects of killing asexual blood-stage parasites and blocking transmission to Anopheles mosquitoes by binding to and inhibiting the function of acetyl-CoA synthetase, thereby reducing the levels of acetyl-CoA and 4'-phosphopantetheine. In humanized mouse models, MMV693183 shows favorable in vivo efficacy, drug-like properties, and no significant cytotoxicity or off-target activity against human cells. MMV693183 is widely used in malaria-related research as a parasiticide and metabolic disruptor .
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- HY-181647
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Bacterial
Elastase
|
Infection
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LasB-IN-3 is a protease elastase (LasB) inhibitor of Pseudomonas aeruginosa with an IC50 value of 8.5 nM. LasB-IN-3 shows an IC50 of 58.9 nM for the Met128Val mutant. LasB-IN-3 binds to active sites of wild-type and Met128Val mutant LasB, coordinates zinc ions, forms hydrogen bonds and CH-π interactions, and inhibits LasB proteolytic activity. LasB-IN-3 increases survival rate in LasB-induced acute lung injury mice models. LasB-IN-3 can be used for the research of Pseudomonas aeruginosa infection .
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- HY-181782
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GaHP
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Bacterial
Reactive Oxygen Species (ROS)
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Infection
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Gallium hematoporphyrin is a heme analogue and a selective targeting agent against Mycobacteroides abscessus. Gallium hematoporphyrin induces ROS production and inhibits biofilm formation as well as disrupts preformed biofilms in both smooth and rough colony morphotypes of Mycobacteroides abscessus. Gallium hematoporphyrin interferes with heme-dependent metabolic pathways and suppresses the growth of clinical Mycobacteroides abscessus isolatess, with MICs ranging from 0.5 to 1 μg/ml. Gallium hematoporphyrin exhibits synergistic antibacterial activity with Clarithromycin (HY-17508) against Mycobacteroides abscessus. Gallium hematoporphyrin can be used for the research of Mycobacteroides abscessus infection .
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- HY-181282
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Bacterial
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Infection
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MSU-44147 is an inhibitor and antimicrobial agent targeting MmpL3 in Mycobacterium abscessus, with low eukaryotic cytotoxicity, a narrow antimicrobial spectrum that is specific only to mycobacteria, and low drug resistance frequency. MSU-44147 reduces trehalose dimycolate levels by inhibiting MmpL3 function, disrupts biofilm formation and reduces the viability of related bacteria, while exerting bactericidal effects on intracellular Mycobacterium abscessus. MSU-44147 exhibits additive or synergistic effects with antibiotics and can be used in research on multidrug-resistant isolates and infections of Mycobacterium abscessus .
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- HY-P11720
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Beta-lactamase
Bacterial
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Infection
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M104 peptide is an OXA-48 carbapenemase inhibitor and antibiotic potentiator. M104 peptide effectively blocks the binding and active site cavity of OXA-48 . M104 peptide restores Meropenem (HY-13678)’s antibacterial activity against OXA-48-producing Klebsiella pneumoniae. M104 peptide can be used for the research of Carbapenem-resistant Klebsiella pneumoniae infection .
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- HY-182816
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Topoisomerase
DNA/RNA Synthesis
Bacterial
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Infection
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Topoisomerase I-IN-22 is an inhibitor of MRSA DNA Topoisomerase I with an IC50 of 0.85 μg/mL. Topoisomerase I-IN-22 can specifically disrupt the cell membrane structure of MRSA, enter the interior of bacteria and inhibit the activity of DNA Topoisomerase I, thereby interfering with the processes of DNA replication and transcription. Topoisomerase I-IN-22 can be used for the research of MRSA infection .
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- HY-N17297
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Fungal
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Infection
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Leotiomycene C is an isoprenylated bisresorcinol natural product present in the freshwater fungus Helotiales sp. Leotiomycene C inhibits the quorum sensing system of methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA), with an IC₅₀ of 6.3-12.5 μM. Leotiomycene C is applicable to research related to MRSA infections .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P11080
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Bacterial
|
Infection
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Oncocin is an antibacterial peptide. It belongs to proline-rich antimicrobial peptides (PrAMPs). Oncocin works against Gram-negative bacteria. It has MIC values of 0.125-8 μg/mL for 34 strains and clinical isolates of Enterobacteriaceae and nonfermenters. Oncocin binds to the substrate-binding domain of the chaperone DnaK. The binding has dissociation constants in the micromolar range. This binding causes protein misfolding and aggregation and the bacteria death .
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- HY-P11191
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Bacterial
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Infection
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AR-23 is a melittin-related antimicrobial peptide that can be isolated from Rana tagoi. AR-23 exhibits broad-spectrum growth inhibitory activity against aerobic bacteria, the opportunistic yeast pathogen Candida albicans and clinical isolates of Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA). AR-23 can be used for antimicrobial research .
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- HY-P11720
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Beta-lactamase
Bacterial
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Infection
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M104 peptide is an OXA-48 carbapenemase inhibitor and antibiotic potentiator. M104 peptide effectively blocks the binding and active site cavity of OXA-48 . M104 peptide restores Meropenem (HY-13678)’s antibacterial activity against OXA-48-producing Klebsiella pneumoniae. M104 peptide can be used for the research of Carbapenem-resistant Klebsiella pneumoniae infection .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N2340
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- HY-N125722
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- HY-N2340A
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- HY-117845
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LL-E19085α
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Structural Classification
Microorganisms
Antibiotics
Source Classification
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Antibiotic
Bacterial
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Citreamicin alpha (LL-E 19085-alpha) is an antibiotic whose in vitro antimicrobial activity against 429 clinical isolates of Gram-positive cocci has been tested by the agar dilution method. These microorganisms included 313 strains of Staphylococci and 116 strains of Streptococci. The in vitro activity of Citreamicin alpha was compared with that of ampicillin, amoxicillin, ceftriaxone, erythromycin, and vancomycin. For Staphylococci, the MIC values of Citreamicin alpha ranged from 0.12-4.0 μg/ml, and for Streptococcus pyogenes of the genus Streptococcus, it was 0.03-0.12 μg/ml. However, enterococci were relatively resistant, requiring 2.0 μg/ml of the agent to inhibit 64% of the 62 tested strains. The in vitro activity of this antibiotic was much better than that of ampicillin, amoxicillin, ceftriaxone, and erythromycin, but comparable or slightly inferior to that of vancomycin.
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- HY-N2340R
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- HY-N17297
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-
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-10844S1
-
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Pretomanid-d5 is deuterated labeled Pretomanid (HY-10844). Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
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- HY-10844S
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Pretomanid-d4 is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL .
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| Cat. No. |
Product Name |
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Classification |
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- HY-167690
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Alkynes
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MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
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