Search Result
Results for "
APD
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-17504
-
|
Rosuvastatin hemicalcium; ZD 4522 Calcium
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
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- HY-17504A
-
Rosuvastatin
Maximum Cited Publications
24 Publications Verification
ZD 4522
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
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- HY-12789
-
|
APD334
|
LPL Receptor
|
Inflammation/Immunology
|
|
Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
|
-
-
- HY-17504B
-
|
ZD 4522 Sodium; X-Plended Sodium; Crestor Sodium
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
-
- HY-103175
-
PSB36
1 Publications Verification
|
Adenosine Receptor
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
PSB36 is a highly selective A1 adenosine receptor antagonist, with a Ki of 0.12 nM and a Kd of 0.7 nM. Systemic administration of PSB36 reduces formalin- and Carrageenan (HY-125474)-induced edema in mice and decreases pain-related behaviors, with no local paw activity. PSB36 prolongs the APD90 of rat and human atria, produces a frequency-dependent prolongation of rat atrial ERP, increases the diastolic threshold of rat atria, and shortens the duration of atrial fibrillation episodes. PSB36 can be used in research related to inflammatory pain, inflammatory hyperalgesia, edema and atrial fibrillation .
|
-
-
- HY-16751
-
-
-
- HY-15793
-
|
(+)-DTBZ; (+)-α-Dihydrotetrabenazine; (+)-α-DHTBZ
|
Monoamine Transporter
|
Neurological Disease
|
|
NBI-98782 is a high affinity and selectivity vesicular monoamine transporter 2 (VMAT2) inhibitor with a Ki of 3 nM. NBI-98782 has antipsychotic activity .
|
-
-
- HY-B1194
-
|
(±)-Tetramisole hydrochloride; DL-Tetramisole hydrochloride; R-829
|
Potassium Channel
Parasite
PKA
|
Infection
Cardiovascular Disease
|
|
Tetramisole hydrochloride is an orally active, selective inward rectifier potassium channel agonist with an EC50 of approximately 30 μM for the Kir2.1 subunit. Tetramisole hydrochloride is also an anti-nematode agent that blocks neuromuscular transmission by non-competitive depolarization. Tetramisole hydrochloride promotes the forward transport of Kir2.1 channels, hyperpolarizes the resting potential (RP), shortens the action potential duration (APD), inhibits intracellular calcium overload and the PKA signaling pathway, and exerts anti-arrhythmic and anti-myocardial remodeling activities. Tetramisole hydrochloride can be used in cardiac electrophysiology research and research related to myocardial ischemia and heart failure .
|
-
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- HY-15565
-
APD668
2 Publications Verification
|
GPR119
Cytochrome P450
Potassium Channel
|
Metabolic Disease
|
|
APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes .
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- HY-10559
-
|
APD125
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
|
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- HY-148804
-
|
APD418
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Vemtoberant is a β3-adrenergic receptor inhibitor with a human Ki of 8.2 nM, and exhibits 400- to 600-fold selectivity over human β1-AR and β2-AR. Vemtoberant attenuates β3-AR-mediated cardiac inhibition. Vemtoberant can be used for the research of systolic heart failure .
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- HY-N0747
-
-
-
- HY-15566
-
APD597
1 Publications Verification
JNJ-38431055
|
GPR119
|
Metabolic Disease
|
|
APD597 (JNJ-38431055) is an orally active agonist of GPR119. APD597 exhibits reduced CYP2C9 inhibition with an IC50 of 5.8 μM. APD597 can be studied in research for type 2 diabetes .
|
-
-
- HY-111110
-
-
-
- HY-10560
-
-
-
- HY-125772
-
|
Acetylpodocarpic dimer; APD
|
LXR
|
Cardiovascular Disease
|
|
Acetyl podocarpic acid anhydride is a potent, semisynthetic liver X receptor(LXR) agonist derived from extracts of the mayapple. Acetyl podocarpic acid anhydride has the potential to be useful for the prevention and research of atherosclerosis, especially in the context of low HDL levels .
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- HY-17504AS1
-
|
ZD 4522-d6
|
Isotope-Labeled Compounds
Autophagy
Bacterial
HMG-CoA Reductase (HMGCR)
Potassium Channel
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
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- HY-12789S
-
|
APD334-d9
|
Isotope-Labeled Compounds
LPL Receptor
|
Inflammation/Immunology
|
|
Etrasimod-d9 (APD334-d9) is a deuterium labeled Etrasimod (HY-12789). Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells. .
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- HY-17504AS
-
-
-
- HY-135432
-
|
APD334 arginine
|
LPL Receptor
|
Inflammation/Immunology
|
|
Etrasimod arginine is an orally available S1P receptor modulator that is a potent full agonist of the S1P1 receptor and has partial agonist activity at S1P4. Etrasimod arginine reduces inflammation in a CD4 +CD45RB high T cell-transferred mouse colitis model .
|
-
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- HY-W008628S
-
-
-
- HY-106718
-
|
|
Sodium Channel
|
Cardiovascular Disease
|
|
Barucainide is an Ib-class anti-arrhythmic agent (moderately blocking sodium channel). Barucainide exhibits concentration-dependent inhibitory effects on the maximum upstroke velocity (Vmax) of Purkinje fibers and ventricular muscle in dogs. Barucainide significantly shortens the action potential duration (APD). Barucainide significantly inhibits the pacemaker activity frequency of atrial tissue in rabbits and the enhanced automaticity of Purkinje fibers under normal resting potential in response to isoproterenol. Barucainide cannot inhibit the abnormal automaticity emission frequency of canine Purkinje fibers induced by barium. Barucainide can be used for research on arrhythmias .
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- HY-172617
-
|
|
BMI1
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
APD-94 is a dual inhibitor targeting tubulin and Bmi-1. APD-94 interfers tubulin normal polymerization. APD-94 suppresses the expression of Bmi-1. APD-94 causes cell cycle arrest at the G2/M phase in cancer cells and induces apoptosis, thus inhibiting cancer cell proliferation. APD-94 represses the growth of HT29 cell xenografts in NOD/SCID mice. APD-94 can be used for colorectal cancer study .
|
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- HY-19899
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
APD-916 is an H3 receptor antagonist. APD-916 shows good pharmacokinetic properties, and oral administration of APD-916 has been shown to enhance wakefulness in various animal models .
|
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- HY-15565R
-
|
|
GPR119
Cytochrome P450
Potassium Channel
|
Metabolic Disease
|
|
APD668 (Standard) is the analytical standard of APD668. This product is intended for research and analytical applications. APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes .
|
-
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- HY-17504BR
-
|
ZD 4522 Sodium (Standard); X-Plended Sodium (Standard); Crestor Sodium (Standard)
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
Bacterial
Reference Standards
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin (Sodium) (Standard) is the analytical standard of Rosuvastatin (Sodium). This product is intended for research and analytical applications. Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
-
- HY-17504BS2
-
|
ZD 4522-13C,d3 sodium; X-Plended-13C,d3 sodium; Crestor-13C,d3 sodium
|
Autophagy
Bacterial
HMG-CoA Reductase (HMGCR)
Potassium Channel
Isotope-Labeled Compounds
|
Cardiovascular Disease
Metabolic Disease
|
|
Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
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- HY-12789R
-
|
APD334 (Standard)
|
LPL Receptor
Reference Standards
|
Inflammation/Immunology
|
|
Etrasimod (Standard) is the analytical standard of Etrasimod. This product is intended for research and analytical applications. Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
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- HY-10560A
-
-
-
- HY-148804A
-
|
APD418 mesylate
|
Adrenergic Receptor
|
Endocrinology
|
|
Vemtoberant mesylate is an β3 Adrenergic Receptor antagonist. Vemtoberant mesylate can be used for research of β3 adrenergic receptor-mediated disorder, such as, heart failure .
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-
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- HY-10560R
-
|
APD791 (Standard)
|
Reference Standards
5-HT Receptor
|
Neurological Disease
|
|
Temanogrel (Standard) is the analytical standard of Temanogrel. This product is intended for research and analytical applications. Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM.
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- HY-10082S1
-
|
3-AP-d3; PAN-811-d3; OCX191-d3
|
Isotope-Labeled Compounds
DNA/RNA Synthesis
|
Cancer
|
|
Triapine-d3 (3-AP-d3) is deuterium labeled Triapine. Triapine (3-AP; PAN-811) is a potent inhibitor of the M2 subunit of ribonucleotide reductase (RR), and is a potent radiosensitizer.
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-
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- HY-182341
-
|
|
Drug Derivative
|
Infection
|
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APD-209 is a sialic acid conjugate with a PEG4 polar linker and a PDA non-polar tail. APD-209 aggregates adenovirus type 37 particles, blocks the binding of viral particles to human corneal epithelial cells, and inhibits cellular entry of adenovirus type 37. APD-209 can be used for the research of epidemic keratoconjunctivitis .
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- HY-14924
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
Inakalant is an atrial specific potassium channel blocker with antiarrhythmic activity. Inakalant works by selectively blocking potassium channels in heart cells, thereby prolongs the action potential duration (APD) of cardiomyocytes and increases the effective refractory period of the atria and ventricles, which helps to terminate and prevent the occurrence of arrhythmias such as atrial fibrillation (AF). Inakalant can be used in the study of arrhythmia and cardiac electrophysiology .
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- HY-118148
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
UK-66914, is a class III antiarrhythmic agent that specifically acts on the delayed rectifier potassium current (I_K). UK-66914 is designed to prolong action potential duration (APD) and increase cardiac refractory period, thereby potentially terminating the reentry mechanism in arrhythmias without affecting the serious side effects of antiarrhythmic drugs associated with other ion channels such as Na+ and Ca2+ currents .
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- HY-N0747R
-
-
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- HY-107036
-
|
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Potassium Channel
|
Cardiovascular Disease
|
|
BMS-394136 (compound 1) is a potent inhibitor of Kv 1.5, with an IC50 of 0.05 μM. BMS-394136 is a selective IKur inhibitor. BMS-394136 dose-dependently prolongs atrial effective refractory period (AERP) and action potential duration (APD) without effecting ventricular effective refractory period (VERP). BMS-394136 can be used for acute atrial ischemia research .
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- HY-B1194A
-
|
|
Potassium Channel
Parasite
PKA
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Infection
Cardiovascular Disease
|
|
Tetramisole is an orally active, selective inward rectifier potassium channel agonist with an EC50 of approximately 30 μM for the Kir2.1 subunit. Tetramisole is also an anti-nematode agent that blocks neuromuscular transmission by non-competitive depolarization. Tetramisole promotes the forward transport of Kir2.1 channels, hyperpolarizes the resting potential (RP), shortens the action potential duration (APD), inhibits intracellular calcium overload and the PKA signaling pathway, and exerts anti-arrhythmic and anti-myocardial remodeling activities. Tetramisole can be used in cardiac electrophysiology research and research related to myocardial ischemia and heart failure .
|
-
-
- HY-W705705
-
|
|
Calcium Channel
Potassium Channel
Sodium Channel
|
Cardiovascular Disease
|
|
NIP-142 is a benzopyran derivative with multiple ion channel-blocking effects. NIP-142 selectively blocks the potassium ion channels enriched in atrial muscle, prolonging the effective refractory period (ERP) and action potential duration (APD) of the atrium, while having minimal effect on ventricular repolarization. NIP-142 also inhibits L-type/T-type calcium channels and sodium channels, further contributing to its anti-arrhythmic effect. NIP-142 shows significant efficacy in various atrial fibrillation models. NIP-142 can be used for research on arrhythmias .
|
-
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- HY-B1194R
-
|
(±)-Tetramisole hydrochloride (Standard); DL-Tetramisole hydrochloride (Standard); R-829 (Standard)
|
Reference Standards
Potassium Channel
Parasite
PKA
|
Infection
Cardiovascular Disease
|
|
Tetramisole hydrochloride (Standard) is the analytical standard of Tetramisole (hydrochloride). This product is intended for research and analytical applications. Tetramisole hydrochloride is an orally active, selective inward rectifier potassium channel agonist with an EC50 of approximately 30 μM for the Kir2.1 subunit. Tetramisole hydrochloride is also an anti-nematode agent that blocks neuromuscular transmission by non-competitive depolarization. Tetramisole hydrochloride promotes the forward transport of Kir2.1 channels, hyperpolarizes the resting potential (RP), shortens the action potential duration (APD), inhibits intracellular calcium overload and the PKA signaling pathway, and exerts anti-arrhythmic and anti-myocardial remodeling activities. Tetramisole hydrochloride can be used in cardiac electrophysiology research and research related to myocardial ischemia and heart failure .
|
-
-
- HY-10559R
-
|
APD125 (Standard)
|
Reference Standards
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Nelotanserin (Standard) is the analytical standard of Nelotanserin (HY-10559). This product is intended for research and analytical applications. Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
|
-
-
- HY-180654
-
|
|
Molecular Glues
Drug Derivative
E1/E2/E3 Enzyme
|
Cancer
|
|
JWZ-8-103 is an orally active PRLX-93936 (HY-119264) analog and TRIM21-targeting molecular glue. JWZ-8-103 increases the thermal stability of TRIM21. JWZ-8-103 promotes a robust and rapid interaction between TRIM21 and NUP98 (apparent EC50 = ∼20 μM for TRIM21 PRYSPRY and NUP98 APD). JWZ-8-103 has anti-cancer effects against pancreatic cancer .
|
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- HY-180654A
-
|
|
Molecular Glues
Drug Derivative
E1/E2/E3 Enzyme
|
Cancer
|
|
JWZ-8-103 hydrochloride is an orally active PRLX-93936 (HY-119264) analog and TRIM21-targeting molecular glue. JWZ-8-103 hydrochloride increases the thermal stability of TRIM21. JWZ-8-103 hydrochloride promotes a robust and rapid interaction between TRIM21 and NUP98 (apparent EC50 = ∼20 μM for TRIM21 PRYSPRY and NUP98 APD). JWZ-8-103 hydrochloride has anti-cancer effects against pancreatic cancer .
|
-
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-17504AS1
-
|
|
|
Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
-
- HY-12789S
-
|
|
|
Etrasimod-d9 (APD334-d9) is a deuterium labeled Etrasimod (HY-12789). Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells. .
|
-
-
- HY-17504AS
-
|
|
|
Rosuvastatin-d3 (ZD 4522-d3) is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals .
|
-
-
- HY-W008628S
-
|
|
|
Bisphenol AP-d5 is the deuterium labeled Bisphenol AP .
|
-
-
- HY-17504BS2
-
|
|
|
Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
-
- HY-10082S1
-
|
|
|
Triapine-d3 (3-AP-d3) is deuterium labeled Triapine. Triapine (3-AP; PAN-811) is a potent inhibitor of the M2 subunit of ribonucleotide reductase (RR), and is a potent radiosensitizer.
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