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low hERG

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Akt (1) Antibiotic (1) Apoptosis (1) Autophagy (6) Bacterial (7) CDK (1) GLP Receptor (1) Histamine Receptor (2) HIV (1) HMG-CoA Reductase (HMGCR) (6) HSP (2) Potassium Channel (9) Reverse Transcriptase (1) Somatostatin Receptor (1)
By Research Areas:	Cancer (7) Cardiovascular Disease (7) Infection (4) Metabolic Disease (7) Neurological Disease (3)

Targets Recommended: LDLR LOX-1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17504B

Rosuvastatin Sodium Maximum Cited Publications 9 Publications Verification ZD 4522 Sodium; X-Plended Sodium; Crestor Sodium	HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy Bacterial	Cardiovascular Disease Metabolic Disease
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-17504

Rosuvastatin Calcium Maximum Cited Publications 9 Publications Verification 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 .

HY-147841

HIV-1 inhibitor-41	HIV Reverse Transcriptase	Infection
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC₅₀ values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .

HY-153690

Progranulin modulator-1	Others	Others
Progranulin modulator-1 (Compound 60) is an orally active enhancer of progranulin (PGRN) secretion. Progranulin modulator-1 enhances the potency of BV-2 cell to increase PGRN levels, has inhibitory effect on *hERG* and Low cytotoxicity, the PGRN EC₅₀ and hERG IC₅₀ were 83 and 3100 nM, respectively .

HY-17504A

Rosuvastatin 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 .

HY-17504R

Rosuvastatin Calcium (Standard) 3 Publications Verification Rosuvastatin hemicalcium (Standard); ZD 4522 Calcium (Standard)	HMG-CoA Reductase (HMGCR) Autophagy Potassium Channel Bacterial	Cardiovascular Disease Metabolic Disease Cancer
Rosuvastatin (Calcium) (Standard) is the analytical standard of Rosuvastatin (Calcium). This product is intended for research and analytical applications. 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 .

HY-149013

Anti-MRSA agent 5	Bacterial	Infection
Anti-MRSA agent 5 (B14) is a potent MRSA agent with MIC₅₀ values of 0.38 μg/mL and has low hERG activity with an IC₅₀ values of >40 μM. Anti-MRSA agent 5 (B14) also has low cytotoxicity to mammal cells and unlikely to acquire bacterial resistance .

HY-17504D

(3S,5R)-Rosuvastatin	HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy	Cardiovascular Disease Metabolic Disease
(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin 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 . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-17504C

(3R,5R)-Rosuvastatin	HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy	Cardiovascular Disease Metabolic Disease
(3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin 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 . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-144341

DprE1-IN-1	Bacterial	Infection
DprE1-IN-1 is a potent, orally active DprE1 inhibitor with favorable hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 displays potent activity against both agent-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs10 CFU reduction in macrophages.

HY-160031

GLP-1R agonist 19	GLP Receptor	Metabolic Disease
GLP-1R agonist 19 (M3190) is a potent and selective GLP-1R agonist. GLP-1R agonist 19 has excellent plasma stability, liver microsomal stability, and low hERG toxicity .

HY-149431

NDNA4	HSP Potassium Channel	Cancer
NDNA4 (compound 17) is a selective inhibitor of Hsp90α (IC₅₀: 0.34 μM). NDNA4 is a permanently charged analog with low membrane permeability and low cytotoxicity against Ovcar-8 and MCF-10A ((IC₅₀ >100 μM)). NDNA4 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .

HY-149432

NDNA3	HSP Potassium Channel	Cancer
NDNA3 (compound 14) is a selective inhibitor of Hsp90α (IC₅₀: 0.51 μM). NDNA3 is a permanently charged analog with low membrane permeability and low toxicity to Ovcar-8 (IC₅₀: 12.66 μM) and MCF-10A (IC₅₀: 11.72 μM) cells. NDNA3 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .

HY-157303

SSTR5 antagonist 3	Somatostatin Receptor	Cardiovascular Disease
SSTR5 antagonist 3 (Compound 23) is an orally active somatostatin receptor subtype 5 (SSTR5) antagonist with low hERG inhibition. SSTR5 antagonist 3 exhibits potency with IC₅₀ values of 2.8 nM and 1.4 nM in human and mouse, respectively. SSTR5 antagonist 3 can be used for the research of anti-gallstone .

HY-146158

WX-081	Bacterial Potassium Channel Antibiotic	Infection
WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. WX-081 exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for agent susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. WX-081 also inhibits hERG channel with the IC50 of 1.89 μM.

HY-150562

CDK9-IN-19	CDK	Cancer
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC₅₀ value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .

HY-126257

AKT-IN-3	Akt Apoptosis	Cancer
AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells .

HY-109968A

Irdabisant hydrochloride CEP-26401 hydrochloride	Histamine Receptor	Neurological Disease
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with K_i values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC₅₀ of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .

HY-109968

Irdabisant CEP-26401	Histamine Receptor	Neurological Disease
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with K_i values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC₅₀ of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .

HY-157425

5-HT2CR agonist 1	5-HT Receptor	Neurological Disease
5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective 5-HT_2CR partial agonist (E_max=71.09%) with an EC₅₀ value of 121.5 nM and no observed activity toward 5-HT_2AR or 5-HT_2BR. 5-HT2CR agonist 1 exhibits no recruitment activity for β-arrestin and shows low inhibition of hERG at 10 μM .

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low hERG

Inhibitors & Agonists