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Pharmacodynamic activity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Anaplastic lymphoma kinase (ALK) (1) Antibiotic (2) Apoptosis (1) ATP Synthase (1) Bacterial (3) CD20 (1) Complement System (1) Cytochrome P450 (2) DNA/RNA Synthesis (1) Endogenous Metabolite (1) Factor Xa (1) Fungal (2) Histamine Receptor (1) Histone Methyltransferase (1) HSV (1) Indoleamine 2,3-Dioxygenase (IDO) (1) Influenza Virus (2) Isotope-Labeled Compounds (1) JAK (1) Orexin Receptor (OX Receptor) (1) Phosphodiesterase (PDE) (1) PI3K (1) Sodium Channel (1) TNF Receptor (1) β-glucuronidase (1)
By Research Areas:	Cancer (5) Cardiovascular Disease (3) Endocrinology (1) Infection (8) Inflammation/Immunology (5) Neurological Disease (1)

By Targets:

Akt (1)

Anaplastic lymphoma kinase (ALK) (1)

Antibiotic (2)

Apoptosis (1)

ATP Synthase (1)

Bacterial (3)

CD20 (1)

Complement System (1)

Cytochrome P450 (2)

DNA/RNA Synthesis (1)

Endogenous Metabolite (1)

Factor Xa (1)

Fungal (2)

Histamine Receptor (1)

Histone Methyltransferase (1)

HSV (1)

Indoleamine 2,3-Dioxygenase (IDO) (1)

Influenza Virus (2)

Isotope-Labeled Compounds (1)

JAK (1)

Orexin Receptor (OX Receptor) (1)

Phosphodiesterase (PDE) (1)

PI3K (1)

Sodium Channel (1)

TNF Receptor (1)

β-glucuronidase (1)

By Research Areas:

Cancer (5)

Cardiovascular Disease (3)

Endocrinology (1)

Infection (8)

Inflammation/Immunology (5)

Neurological Disease (1)

Inhibitors & Agonists

Fluorescent Dye

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-A0147A

Grepafloxacin hydrochloride OPC-17116 hydrochloride; dl-Grepafloxacin hydrochloride	Antibiotic Bacterial	Infection
Grepafloxacin (OPC-17116) hydrochloride is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin hydrochloride has high tissue penetration and a promising pharmacodynamic profile .

HY-18030A

CEP-28122 mesylate salt	Anaplastic lymphoma kinase (ALK)	Cancer
CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK inhibitor, with an IC₅₀ value of 1.9 nM for recombinant ALK kinase activity. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity .

HY-101560

Linrodostat 5 Publications Verification BMS-986205; ONO-7701	Indoleamine 2,3-Dioxygenase (IDO)	Cancer
Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC₅₀ value of 1.1 nM in IDO1-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers .

HY-117290

BMS-962212	Factor Xa	Cardiovascular Disease
BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity .

HY-177123

Refinicopan	Complement System	Inflammation/Immunology
Refinicopan is a complement factor D inhibitor with an IC₅₀ of 10 nM. Refinicopan inhibits rabbit erythrocyte hemolysis with an IC₅₀ of 41 nM. Refinicopan exhibits excellent pharmacokinetic and pharmacodynamic activity .

HY-A0147

Grepafloxacin OPC-17116; dl-Grepafloxacin	Antibiotic Bacterial	Infection
Grepafloxacin (OPC-17116) is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin has high tissue penetration and a promising pharmacodynamic profile .

HY-170435

PDE5-IN-13	Phosphodiesterase (PDE)	Cardiovascular Disease
PDE5-IN-13 (Compound 14b) inhibits phosphodiesterase 5 (PDE5A) with an IC₅₀ of 3 nM. PDE5-IN-13 is a potential candidate for PAH (pulmonary arterial hypertension) research. PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 is orally active .

HY-174353S

CYP51-IN-23-d3	Isotope-Labeled Compounds Cytochrome P450 Fungal	Infection
CYP51-IN-23-d₃ is a potent and broad-spectrum CYP51 inhibitor with a MIC₈₀ of 1 μg/mL against Aspergillus fumigatum. CYP51-IN-23-d₃ can prevent fungal phase transformation and biofilm formation. CYP51-IN-23-d₃ exhibits anti-drug resistance activity and fungal activity, and shows excellent safety for cells and significant pharmacological activity in mice. CYP51-IN-23-d₃ can be used for the study of invasive fungal infections (IFIs) .

HY-174353

CYP51-IN-22	Cytochrome P450 Fungal	Infection
CYP51-IN-22, the non-deuterated analog of CYP51-IN-23-d₃ (HY-174353S), is a potent and broad-spectrum CYP51 inhibitor.CYP51-IN-22 inhibits Aspergillus fumigatum with a MIC₈₀ of 1 μg/mL. CYP51-IN-22 can prevent fungal phase transformation and biofilm formation. CYP51-IN-22 exhibits anti-drug resistance activity and fungal activity, and shows excellent safety for cells and significant pharmacological activity in mice. CYP51-IN-22 can be used for the study of invasive fungal infections (IFIs) .

HY-N8265

Abyssinone V	HSV DNA/RNA Synthesis ATP Synthase	Infection
Abyssinone V is a prenylated flavonoid with predicted anti-viral activity. Abyssinone V can be isolated from the stem bark of Erythrina melanacantha. Abyssinone V possesses good pharmacodynamics properties. Abyssinone V is predicted to be antivirals including anti-herpes (HSV) agent, with mechanisms comprising inhibition of polymerase, ATPase and membrane integrity .

HY-19517

R1663	Endogenous Metabolite	Cardiovascular Disease
R1663 is a factor Xa inhibitor with anticoagulant activity. R1663 does not affect bleeding time. The pharmacodynamic effects (such as inhibition of thrombin generation) and plasma concentrations of R1663 are dose-dependent. R1663 prolongs clotting time in a concentration-dependent manner and inhibits the peak height of thrombin generation and endogenous thrombin potential .

HY-P99812

Ragifilimab INCAGN-1876	TNF Receptor	Inflammation/Immunology Cancer
Ragifilimab (INCAGN-1876) is an agonist monoclonal antibody targeting the glucocorticoid-induced TNFR-related protein (GITR). Ragifilimab binds to and activates GITR on T cells, which stimulates the immune system to enhance its anti-tumor activity. Ragifilimab can be used for advanced or metastatic solid tumors research .

HY-D1460

Fluorescein Di-β-D-Glucuronide	β-glucuronidase Bacterial	Infection
Fluorescein Di-β-D-Glucuronide, a fluorescent probe, can be utilized to non-invasively image the intestinal bacterial β-glucuronidase activity in nude mice. Fluorescein Di-β-D-Glucuronide-based imaging reveals the in vitro and in vivo activity of intestinal bacterial β-glucuronidase, which would facilitate pharmacodynamic studies of specific bacterial β-glucuronidase inhibitors in animal studies .

HY-118374

AM-9635	PI3K Akt	Inflammation/Immunology
AM-9635 is a selective PI3Kδ inhibitor with oral bioavailability, good in vitro and in vivo activity and pharmacodynamic properties. AM-9635 inhibits PI3Kδ-dependent B cell receptor-mediated AKT phosphorylation and suppresses the production of specific IgG and IgM antibodies in rats immunized with Aplysia leocyanin (KLH).

HY-167846

YLIU-4-105-1	JAK	Cancer
YLIU-4-105-1 is a Type II JAK2 inhibitor. YLIU-4-105-1 binds to the ATP-binding pocket of JH1. YLIU-4-105-1 has in vivo pharmacodynamic activity as evidenced by inhibiting pSTAT5, reducing spleen to body weight, and lowering blood reticulocyte counts in a dose-dependent manner .

HY-135495

AM-0466	Sodium Channel Histamine Receptor	Inflammation/Immunology
AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing .

HY-143755

Cap-dependent endonuclease-IN-9	Influenza Virus	Infection
Cap-dependent endonuclease-IN-9 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-9 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-9 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent CN112521386A, compound VI-1) .

HY-143743

Cap-dependent endonuclease-IN-2	Influenza Virus	Infection
Cap-dependent endonuclease-IN-2 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-2 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-2 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent WO2019052565A1, compound 28) .

HY-10900

TCS 1102	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1 receptors, respectively. TCS 1102 demonstrates excellent blood-brain barrier penetrability and moderate bioavailability in rats .

HY-133031A

CSV0C018875 hydrochloride	Histone Methyltransferase	Others
CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .

HY-P991547

Anti-CD20 Antibody (mAb 1.5.3)	CD20 Apoptosis	Inflammation/Immunology Cancer
Anti-CD20 Antibody (mAb 1.5.3) is a fully human IgG1 anti-CD20 antibody. Anti-CD20 Antibody (mAb 1.5.3) evokes enhanced pro-apoptotic activity in vitro. Anti-CD20 Antibody (mAb 1.5.3) mediated both complement-dependent cytotoxicity and antibody-dependent cellular cytotoxicity. Anti-CD20 Antibody (mAb 1.5.3) demonstrates enhanced anti-tumor activity in various tumor xenograft models. Anti-CD20 Antibody (mAb 1.5.3) produces a superior B-cell depletion profile in lymph node organs and bone marrow in a primate pharmacodynamic model. Anti-CD20 Antibody (mAb 1.5.3) can be studied in research for B-cell maglignancies .

Cat. No.	Product Name	Type

HY-D1460

Fluorescein Di-β-D-Glucuronide	Fluorescent Dyes/Probes
Fluorescein Di-β-D-Glucuronide, a fluorescent probe, can be utilized to non-invasively image the intestinal bacterial β-glucuronidase activity in nude mice. Fluorescein Di-β-D-Glucuronide-based imaging reveals the in vitro and in vivo activity of intestinal bacterial β-glucuronidase, which would facilitate pharmacodynamic studies of specific bacterial β-glucuronidase inhibitors in animal studies .

Fluorescein Di-β-D-Glucuronide

Fluorescent Dyes/Probes

Fluorescein Di-β-D-Glucuronide, a fluorescent probe, can be utilized to non-invasively image the intestinal bacterial β-glucuronidase activity in nude mice. Fluorescein Di-β-D-Glucuronide-based imaging reveals the in vitro and in vivo activity of intestinal bacterial β-glucuronidase, which would facilitate pharmacodynamic studies of specific bacterial β-glucuronidase inhibitors in animal studies .

Cat. No.	Product Name	Target	Research Area

HY-P99812

Ragifilimab INCAGN-1876	TNF Receptor	Inflammation/Immunology Cancer
Ragifilimab (INCAGN-1876) is an agonist monoclonal antibody targeting the glucocorticoid-induced TNFR-related protein (GITR). Ragifilimab binds to and activates GITR on T cells, which stimulates the immune system to enhance its anti-tumor activity. Ragifilimab can be used for advanced or metastatic solid tumors research .

HY-P991547

Anti-CD20 Antibody (mAb 1.5.3)	CD20 Apoptosis	Inflammation/Immunology Cancer
Anti-CD20 Antibody (mAb 1.5.3) is a fully human IgG1 anti-CD20 antibody. Anti-CD20 Antibody (mAb 1.5.3) evokes enhanced pro-apoptotic activity in vitro. Anti-CD20 Antibody (mAb 1.5.3) mediated both complement-dependent cytotoxicity and antibody-dependent cellular cytotoxicity. Anti-CD20 Antibody (mAb 1.5.3) demonstrates enhanced anti-tumor activity in various tumor xenograft models. Anti-CD20 Antibody (mAb 1.5.3) produces a superior B-cell depletion profile in lymph node organs and bone marrow in a primate pharmacodynamic model. Anti-CD20 Antibody (mAb 1.5.3) can be studied in research for B-cell maglignancies .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N8265

Abyssinone V	Flavonoids Leguminosae Flavonones Erythrina melanacantha Taub. ex Harms Source classification Plants	HSV DNA/RNA Synthesis ATP Synthase
Abyssinone V is a prenylated flavonoid with predicted anti-viral activity. Abyssinone V can be isolated from the stem bark of Erythrina melanacantha. Abyssinone V possesses good pharmacodynamics properties. Abyssinone V is predicted to be antivirals including anti-herpes (HSV) agent, with mechanisms comprising inhibition of polymerase, ATPase and membrane integrity .

Cat. No.	Product Name	Chemical Structure

HY-174353S

CYP51-IN-23-d3
CYP51-IN-23-d₃ is a potent and broad-spectrum CYP51 inhibitor with a MIC₈₀ of 1 μg/mL against Aspergillus fumigatum. CYP51-IN-23-d₃ can prevent fungal phase transformation and biofilm formation. CYP51-IN-23-d₃ exhibits anti-drug resistance activity and fungal activity, and shows excellent safety for cells and significant pharmacological activity in mice. CYP51-IN-23-d₃ can be used for the study of invasive fungal infections (IFIs) .

CYP51-IN-23-d3

CYP51-IN-23-d₃ is a potent and broad-spectrum CYP51 inhibitor with a MIC₈₀ of 1 μg/mL against Aspergillus fumigatum. CYP51-IN-23-d₃ can prevent fungal phase transformation and biofilm formation. CYP51-IN-23-d₃ exhibits anti-drug resistance activity and fungal activity, and shows excellent safety for cells and significant pharmacological activity in mice. CYP51-IN-23-d₃ can be used for the study of invasive fungal infections (IFIs) .

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