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Results for "

low clearance

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Autophagy (1) BCRP (1) Casein Kinase (1) CDK (1) Cyclic GMP-AMP Synthase (1) Epigenetic Reader Domain (1) Estrogen Receptor/ERR (1) Glucosidase (1) HCV (1) HIV (2) HIV Integrase (2) IRAK (2) mAChR (1) p38 MAPK (1) Parasite (1) PDI (1) Phosphodiesterase (PDE) (2) Prostaglandin Receptor (1) Wnt (1)
By Research Areas:	Cancer (9) Cardiovascular Disease (2) Infection (6) Inflammation/Immunology (6) Metabolic Disease (2) Neurological Disease (2)

Targets Recommended: LDLR LOX-1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12839

p38 MAPK-IN-1 Maximum Cited Publications 11 Publications Verification	p38 MAPK Autophagy	Inflammation/Immunology
p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC₅₀ of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.

HY-139875

JH-XVI-178 1 Publications Verification	CDK	Cancer
JH-XVI-178 is a highly efficient and selective CDK8/19 inhibitor, with IC₅₀ values of 1 and 2 nM for CDK8 and CDK19, respectively. JH-XVI-178 has a low clearance rate and moderate oral pharmacokinetic properties .

HY-100432

LOC14 2 Publications Verification	PDI	Neurological Disease Inflammation/Immunology
LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC₅₀ and K_d values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding . LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .

HY-153241

GSK737	Epigenetic Reader Domain	Cancer
GSK737 is a BRD4 BD1 and BD2 inhibitor, with pIC₅₀ *values of 5.3 and 7.3 respectively. GSK737 has low* clearance and good solubility and permeability in rat .**

HY-143255

Enpp-1-IN-11	Phosphodiesterase (PDE)	Cancer
Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an K_i value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer .

HY-128060

PDE5-IN-42	Phosphodiesterase (PDE)	Cardiovascular Disease
PDE5-IN-42 (Compound 42) is a potent and orally active PDE5 inhibitor with an IC₅₀ of 0.04 nM. PDE5-IN-42 maintains selectivity over PDE6 and PDE11 .

HY-163040

DOTA-Tyr-Lys-DOTA	Others	Inflammation/Immunology
DOTA-Tyr-Lys-DOTA is a DOTA-based small molecule hapten. DOTA-Tyr-Lys-DOTAexhibits rapid clearance and low whole-body retention. DOTA-Tyr-Lys-DOTA can used in study pretargeted radioimmunotherapy .

HY-120004

PF-06827443	mAChR	Infection
PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .

HY-112047

GSK8175 GSK2878175	HCV	Infection
GSK8175 is a non-nucleoside polymerase (NS5B) inhibitor of hepatitis C virus (HCV). GSK8175 is a sulfonamide- N-benzoxaborole analog with low in vivo clearance across preclinical species and broad-spectrum activity against HCV replicons .

HY-116494

ML753286	BCRP	Cancer
ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC₅₀ of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .

HY-162459

cGAS-IN-3	Cyclic GMP-AMP Synthase	Inflammation/Immunology
cGAS-IN-3 (compound 30d-S) is an orally active cyclic GMP-AMP synthase (Cyclic GMP-AMP Synthase/cGAS) inhibitor with good plasma exposure and low clearance. cGAS-IN-3 has anti-inflammatory activity and can significantly reduce lung inflammation in rats .

HY-153256

EP3 antagonist 4	Prostaglandin Receptor	Metabolic Disease
EP3 antagonist 4 (Compound 28) is an EP3 antagonist, with a K_i value of 2 nM for hEP. EP3 antagonist 4 shows low in vivo clearance, high oral AUC, and good bioavailability in the rat full PK studies. EP3 antagonist 4 can be used for research of beta cell dysfunction in diabetes .

HY-154823

Gcase activator 2	Glucosidase	Metabolic Disease
Gcase activator 2 (compound 14), a pyrrolo[2,3-b]pyrazine, is alos a β-Glucocerebrosidase (GCase) activator (EC₅₀=3.8 μM). Gcase activator 2 induces GCase dimerizatio (both K-type and V-type). And Gcase activator 2 has low metabolic clearance in human and mouse .

HY-143439

LX-039	Estrogen Receptor/ERR	Cancer
LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC₅₀ value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high C_max and oral exposure. LX-039 has anti-tumor activity .

HY-116494A

(6R)-ML753286	Others	Cancer
(6R)-ML753286 is an isomer of ML753286 (HY-116494). ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC₅₀ of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .

HY-150080

GSK3739936 BMS-986180	HIV HIV Integrase	Infection
GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC₅₀ value of 11.1 nM and an EC₅₀ value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC₅₀>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .

HY-12570

CK2-IN-9	Casein Kinase Wnt	Cancer
CK2-IN-9 is a potent and selective inhibitor of CK2 kinase with an IC₅₀ of 3 nM. CK2-IN-9 reduces Wnt reporter activity with an IC₅₀ of 75 nM. CK2-IN-9 has low exposure (AUC=0.36 μM/h) and high clearance (CL=65 mL/min/kg) properties in rat .

HY-162238

OSM-S-106	Parasite	Infection
OSM-S-106 is a pro-inhibitor and that inhibition of PfAsnRS occurs via enzyme-mediated production of an Asn-OSM-S-106 adduct. OSM-S-106 inhibits protein translation and activates the amino acid starvation response. OSM-S-106 exhibits selective activity against Plasmodium blood and liver stages and low intrinsic clearance by human microsomes .

HY-122229

GS-9822	HIV	Infection
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC₅₀ of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .

HY-155518

IRAK4-IN-25	IRAK	Inflammation/Immunology
IRAK4-IN-25 (compound 38) is an orally acitve and potent IRAK4 inhibitor (IC₅₀=7.3 nM), with low clearance (Cl=12 mL/min/kg). IRAK4-IN-25 inhibits production of pro-inflammatory cytokines, and shows in vitro safety and ADME profiles. IRAK4-IN-25 can be used for research in inflammatory and autoimmune disorders .

HY-146113

IRAK4-IN-15	IRAK	Cancer
IRAK4-IN-15 (compound 35) is a potent and selective IRAK4 inhibitor with an IC₅₀ of 0.002 µM. IRAK4-IN-15 shows good human PK predictions with low intrinsic clearance. IRAK4-IN-15 shows great synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib. .

HY-163476

PIP5K1C-IN-1	Others	Inflammation/Immunology Cancer
PIP5K1C-IN-1 (Compound 30) is a potent PIP5K1C inhibitor, with an IC₅₀ of 0.80 nM. PIP5K1C-IN-1 exhibits low total clearance in mice and high levels of kinase selectivity. PIP5K1C-IN-1 can be used for the research of cancer and chronic pain .

HY-159091

HIV-1 integrase inhibitor 12	HIV Integrase	Infection
HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC₅₀ of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC₅₀ of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .

HY-136659

Ro 04-5595	Others	Others
Ro 04-5595 is a selective antagonist with specific activity against the NR2B subunit of the NMDA receptor. Ro 04-5595 exhibits favorable pharmacokinetic properties in in vitro and in vivo studies, with rapid uptake and clearance. Ro 04-5595 exhibits strong binding in NR2B receptor-enriched regions and low binding in the cerebellum. Ro 04-5595 is able to effectively inhibit specific binding, showing high affinity for the NR2B receptor and a clear ranking of binding affinity with a variety of other compounds .

HY-117912

TRC210258	Others	Cardiovascular Disease
TRC210258 is a TGR5 agonist with activity to improve diabetes-associated hyperglycemia and dyslipidemia. TRC210258 promotes energy expenditure by enhancing the release of glucagon-like peptide-1. TRC210258 is able to improve glucose metabolic control in high-fat diet-induced obese mice. TRC210258 also showed improvement in lipid parameters in high-fat-fed hamsters, including reductions in plasma triglyceride and low-density lipoprotein cholesterol levels. TRC210258 improved emerging lipid-related cardiovascular risk parameters including remnant cholesterol and triglyceride clearance .

HY-162585

5-HT1AR agonist 1	5-HT Receptor	Neurological Disease
5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC₅₀ value of 34 nM, SERT reuptake ihibitor (IC₅₀ =12 nM), NET reuptake inhibitor (IC₅₀ =78 nM) and DAT reuptake inhibitor (IC₅₀ =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs .

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low clearance

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