Search Result
Results for "
orally efficacious
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-15253
-
Tiplaxtinin
Maximum Cited Publications
15 Publications Verification
PAI-039; Tiplasinin
|
PAI-1
Apoptosis
|
Metabolic Disease
Cancer
|
|
Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM .
|
-
-
- HY-N1428C
-
|
Iron(III) citrate; Zerenex
|
Reactive Oxygen Species (ROS)
Antibiotic
|
Metabolic Disease
|
|
Ferric citrate (Iron(III) citrate), an orally active iron supplement, is an efficacious phosphate binder. Ferric citratee can be used for iron deficiency anemia and chronic kidney disease (CKD) research .
|
-
-
- HY-153321
-
|
NX-5948; BTK-IN-24
|
PROTACs
Btk
|
Inflammation/Immunology
Cancer
|
|
Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
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-
-
- HY-10268
-
|
PRT054021
|
Factor Xa
|
Cardiovascular Disease
|
|
Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect .
|
-
-
- HY-15200
-
|
CEP-32496; RXDX-105
|
Raf
|
Cancer
|
|
Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
|
-
-
- HY-112542
-
|
CL-287088; LL-F28249 α
|
Parasite
Antibiotic
|
Infection
|
|
Nemadectin (CL-287088), an orally active broad-spectrum endectocide, is highly efficacious against natural infections of all the major canine gastrointestinal helminthes. Anthelmintic activity .
|
-
-
- HY-12445
-
|
CDKI-73; LS-007
|
CDK
Apoptosis
|
Inflammation/Immunology
Cancer
|
Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. Asnuciclib down-regulates the RNAPII phosphorylation. Asnuciclib is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion .
|
-
-
- HY-107427
-
|
|
MAPKAPK2 (MK2)
p38 MAPK
|
Inflammation/Immunology
|
|
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect .
|
-
-
- HY-141692
-
|
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
IL-17 modulator 4 is a proagent of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator. IL-17 modulator 4 is promising for the research of IL-17A mediated diseases, including inflammation, autoimmune diseases, infectious diseases, cancer, and precancerous syndrome .
|
-
-
- 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-10596
-
|
|
Integrin
|
Inflammation/Immunology
|
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BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC50 of 2.5 nM in the adhesion assay and an IC50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model .
|
-
-
- HY-111745
-
|
|
JAK
|
Inflammation/Immunology
|
|
Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis .
|
-
-
- HY-10268A
-
|
PRT054021 maleate
|
Factor Xa
|
Cardiovascular Disease
|
|
Betrixaban (PRT054021) maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban maleate shows antithrombotic effect .
|
-
-
- HY-47030
-
-
-
- HY-121212
-
|
|
LDLR
|
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-14390
-
-
-
- HY-130253
-
|
|
IRAK
|
Cancer
|
|
IRAK4-IN-6 is an orally efficacious and selective IRAK4 inhibitor with an IC50 of 4 nM, and targetes MyD88 L265P mutant diffuse large B cell lymphoma .
|
-
-
- HY-15199
-
|
CEP-32496 hydrochloride; RXDX-105 hydrochloride
|
Raf
|
Cancer
|
|
Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
|
-
-
- HY-A0287S
-
|
Clomifene-d5 hydrochloride; (Z/E)-Enclomiphene-d5 hydrochloride; (Z/E)-Enclomifene-d5 hydrochloride
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
Clomifene (Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene)-d5 hydrochloride is a deuterium labeled Clomifene hydrochloride (HY-A0287A). Clomiphene hydrochloride is an orally active ovulation-inducing agent. Clomiphene hydrochloride binds to hypothalamic estrogen receptors to elevate FSH levels, and exhibits antiestrogenic or estrogenic properties. Clomiphene hydrochloride can induce erturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes. Clomiphene hydrochloride ameliorates memory impairment in PCOS models. Clomiphene hydrochloride mobilizes cytosolic calcium and reduces viability in prostate cancer cells. Clomiphene hydrochloride can be used for the research of polycystic ovary syndrome (PCOS) and prostate cancer .
|
-
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- HY-10268S
-
|
PRT054021-d6
|
Factor Xa
|
Cardiovascular Disease
|
|
Betrixaban-d6 is a deuterium labeled Betrixaban. Betrixaban is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor .
|
-
-
- HY-10268B
-
|
PRT054021 hydrochloride
|
Factor Xa
|
Cardiovascular Disease
|
|
Betrixaban (PRT054021) hydrochloride is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban hydrochloride shows antithrombotic effect .
|
-
-
- 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-10268R
-
|
PRT054021 (Standard)
|
Reference Standards
Factor Xa
|
Cardiovascular Disease
|
|
Betrixaban (Standard) is the analytical standard of Betrixaban. This product is intended for research and analytical applications. Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect .
|
-
-
- HY-12738
-
-
-
- HY-147642
-
-
-
- HY-111368
-
|
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MEK
|
Cancer
|
|
EBI-1051 is a highly potent and orally efficacious MEK inhibitor with an IC50 of 3.9 nM.
|
-
-
- HY-145352
-
-
-
- HY-A0287A
-
|
Clomifene hydrochloride; (Z/E)-Enclomiphene hydrochloride; (Z/E)-Enclomifene hydrochloride
|
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
Clomiphene (Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene) hydrochloride is an orally active ovulation-inducing agent. Clomiphene hydrochloride binds to hypothalamic estrogen receptors to elevate FSH levels, and exhibits antiestrogenic or estrogenic properties. Clomiphene hydrochloride can induce erturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes. Clomiphene hydrochloride ameliorates memory impairment in PCOS models. Clomiphene hydrochloride mobilizes cytosolic calcium and reduces viability in prostate cancer cells. Clomiphene hydrochloride can be used for the research of polycystic ovary syndrome (PCOS) and prostate cancer .
|
-
-
- HY-128354
-
|
|
Parasite
|
Infection
|
|
CWHM-1552 is an orally efficacious inhibitor of P. falciparum with IC50s of 51 nM and 53 nM for 3D7 and Dd2 strain, respectively .
|
-
-
- HY-B0477A
-
|
CI-906 free acid
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Quinapril is a potent, orally active, non-peptide and nonsulfhydryl inhibitor of angiotensin-converting enzyme (ACE). Quinapril specifically interrupts the conversion of angiotensin I to angiotensin II in both plasma and tissue. Quinapril is enzymatically hydrolyzed to a pharmacologically active diacid form quinaprilat. Quinapril is efficacious in hypertensive models .
|
-
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- HY-141692B
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
(R)-IL-17 modulator 4 is the R-configure of IL-17 modulator 4 (HY-141692). IL-17 modulator 4 is a proagent of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator. IL-17 modulator 4 is promising for the research of IL-17A mediated diseases, including inflammation, autoimmune diseases, infectious diseases, cancer, and precancerous syndrome .
|
-
-
- HY-141535A
-
|
|
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
IL-17 modulator 1 (disodium) is an orally active, highly efficacious IL-17 modulator extracted from patent WO 2020127685. IL-17 modulator 1 (disodium) can be used for the research of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis .
|
-
-
- HY-141535
-
|
|
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
IL-17 modulator 1 is an orally active, highly efficacious small molecule IL-17 modulators extracted from patent WO 2020127685. IL-17 modulator 1 can be used for the research of preventing, researching or ameliorating a variety of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis .
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-
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- HY-118709
-
-
-
- HY-115721
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 2 is a novel orally efficacious antimalarials that suggests a fast in vitro killing profile.
|
-
-
- HY-122078
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
FR-190809 is a potent, nonadrenotoxic, orally efficacious acyl-CoA:cholesterol O-acyltransferase (ACAT) inhibitor, with an IC50 of 45 nM .
|
-
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- HY-145704
-
|
|
Parasite
|
Infection
|
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Antimalarial agent 8 (Compound 7e) is a novel orally active class of antimalarials. Antimalarial agent 8 is potent in vitro against P. falciparum and is orally efficacious (40 mg/kg) in an in vivo mouse model of malaria .
|
-
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- HY-120608
-
|
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
BMS-814580 is an orally active, highly efficacious MCHR1 inhibitor with a Ki of 16.9 nM against hMCHR1. BMS-814580 shows antiobesity activities .
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-
-
- HY-112542R
-
|
CL-287088 (Standard); LL-F28249 α (Standard)
|
Reference Standards
Parasite
Antibiotic
|
Infection
|
|
Nemadectin (Standard) is the analytical standard of Nemadectin. This product is intended for research and analytical applications. Nemadectin (CL-287088), an orally active broad-spectrum endectocide, is highly efficacious against natural infections of all the major canine gastrointestinal helminthes. Anthelmintic activity .
|
-
-
- HY-10268S1
-
|
PRT054021-dsub>4
|
Isotope-Labeled Compounds
Factor Xa
|
Cardiovascular Disease
|
|
Betrixaban-d4 (PRT054021-d4) is deuterium labeled Betrixaban. Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect .
|
-
-
- HY-115987
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD) .
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-
-
- HY-11051
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .
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-
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- HY-B0477AS2
-
|
CI-906-d4
|
Isotope-Labeled Compounds
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Quinapril-d4 (CI-906-d4) is deuterium labeled Quinapril. Quinapril is a potent, orally active, non-peptide and nonsulfhydryl inhibitor of angiotensin-converting enzyme (ACE). Quinapril specifically interrupts the conversion of angiotensin I to angiotensin II in both plasma and tissue. Quinapril is enzymatically hydrolyzed to a pharmacologically active diacid form quinaprilat. Quinapril is efficacious in hypertensive models .
|
-
-
- HY-141692A
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
IL-17 modulator 4 sulfate is a proagent of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator. IL-17 modulator 4 sulfate is promising for the research of IL-17A mediated diseases, including inflammation, autoimmune diseases, infectious diseases, cancer, and precancerous syndrome .
|
-
-
- HY-146399
-
|
|
Cholinesterase (ChE)
ROS Kinase
|
Neurological Disease
|
|
AChE/BChE-IN-9 (Compound 7a) is a potent, orally active AChE and BChE inhibitor with IC50 values of 5.74 μM and 14.05 μM against hAChE and eqBChE, respectively. AChE/BChE-IN-9 is also an efficacious antioxidant with an IC50 of 57.35 μM. AChE/BChE-IN-9 is able to chelate iron and modulates aggregation of amyloid β1-42. AChE-IN-16 can cross the BBB .
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-
-
- HY-128774
-
|
|
Beta-secretase
|
Neurological Disease
|
|
AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM) . AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
-
- 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 .
|
-
-
- HY-175547
-
|
|
PROTACs
MAP4K
ERK
Interleukin Related
IFNAR
|
Inflammation/Immunology
Cancer
|
|
PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader (DC50 = 5.0 nM; Dmax ≥ 99%). PROTAC HPK1 Degrader-5 significantly inhibits SLP76 phosphorylation and enhanced ERK pathway activation through degrading HPK1, thereby stimulating IL-2 and IFN-γ release. PROTAC HPK1 Degrader-5 exhibits the ability to overcome the immunosuppressive effects imposed by PGE2, NECA or TGF-β. PROTAC HPK1 Degrader-5 alone efficaciously inhibits tumor growth in an MC38 syngeneic mouse model. PROTAC HPK1 Degrader-5 can be used for the study of tumor (such as colorectal cancer) immunotherapy (Pink: Target protein ligand (HY-175549); Blue: E3 ligand (HY-W023573); Black: Linker; E3 ligand + Linker (HY-175551)) .
|
-
-
- HY-10268S2
-
|
PRT054021-13C6
|
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Betrixaban- 13C6 (PRT054021- 13C6) is 13C labeled Betrixaban. Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect .
|
-
-
- HY-107427R
-
|
|
Reference Standards
MAPKAPK2 (MK2)
p38 MAPK
|
Inflammation/Immunology
|
|
PF-3644022 (Standard) is the analytical standard of PF-3644022 (HY-107427). This product is intended for research and analytical applications. PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated Kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect .
|
-
- HY-10596R
-
|
|
Reference Standards
Integrin
|
Inflammation/Immunology
|
|
BMS-688521 (Standard) is the analytical standard of BMS-688521 (HY-10596). This product is intended for research and analytical applications. BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC50 of 2.5 nM in the adhesion assay and an IC50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-47030
-
|
|
Biochemical Assay Reagents
|
|
Ferric citrate hydrate, an orally active iron supplement, is an efficacious phosphate binder. Ferric citrate hydrate can be used for iron deficiency anemia and chronic kidney disease (CKD) research .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-A0287S
-
|
|
|
Clomifene (Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene)-d5 hydrochloride is a deuterium labeled Clomifene hydrochloride (HY-A0287A). Clomiphene hydrochloride is an orally active ovulation-inducing agent. Clomiphene hydrochloride binds to hypothalamic estrogen receptors to elevate FSH levels, and exhibits antiestrogenic or estrogenic properties. Clomiphene hydrochloride can induce erturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes. Clomiphene hydrochloride ameliorates memory impairment in PCOS models. Clomiphene hydrochloride mobilizes cytosolic calcium and reduces viability in prostate cancer cells. Clomiphene hydrochloride can be used for the research of polycystic ovary syndrome (PCOS) and prostate cancer .
|
-
-
- HY-10268S
-
|
|
|
Betrixaban-d6 is a deuterium labeled Betrixaban. Betrixaban is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor .
|
-
-
- HY-10268S1
-
|
|
|
Betrixaban-d4 (PRT054021-d4) is deuterium labeled Betrixaban. Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect .
|
-
-
- HY-B0477AS2
-
|
|
|
Quinapril-d4 (CI-906-d4) is deuterium labeled Quinapril. Quinapril is a potent, orally active, non-peptide and nonsulfhydryl inhibitor of angiotensin-converting enzyme (ACE). Quinapril specifically interrupts the conversion of angiotensin I to angiotensin II in both plasma and tissue. Quinapril is enzymatically hydrolyzed to a pharmacologically active diacid form quinaprilat. Quinapril is efficacious in hypertensive models .
|
-
-
- HY-10268S2
-
|
|
|
Betrixaban- 13C6 (PRT054021- 13C6) is 13C labeled Betrixaban. Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect .
|
-
| Cat. No. |
Product Name |
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Classification |
-
- HY-128774
-
|
|
|
Alkynes
|
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AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM) . AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
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