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Results for "

Preclinical efficacy

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Payload (1) Akt (1) Amyloid-β (2) Annexin A (1) Apoptosis (1) Bacterial (1) DNA Alkylator/Crosslinker (1) EGFR (1) Fungal (1) GPR119 (1) Histamine Receptor (1) IFNAR (1) Integrin (1) Interleukin Related (2) JAK (1) MetAP (1) nAChR (1) Opioid Receptor (1) Parasite (1) Phosphodiesterase (PDE) (1) Potassium Channel (2) PSMA (1) Radionuclide-Drug Conjugates (RDCs) (1) ROR (1) Ser/Thr Protease (1) STING (1) Tim3 (1) YAP (1) γ-secretase (2)
By Research Areas:	Cancer (8) Infection (1) Inflammation/Immunology (3) Metabolic Disease (5) Neurological Disease (5)

By Targets:

ADC Payload (1)

Akt (1)

Amyloid-β (2)

Annexin A (1)

Apoptosis (1)

Bacterial (1)

DNA Alkylator/Crosslinker (1)

EGFR (1)

Fungal (1)

GPR119 (1)

Histamine Receptor (1)

IFNAR (1)

Integrin (1)

Interleukin Related (2)

JAK (1)

MetAP (1)

nAChR (1)

Opioid Receptor (1)

Parasite (1)

Phosphodiesterase (PDE) (1)

Potassium Channel (2)

PSMA (1)

Radionuclide-Drug Conjugates (RDCs) (1)

ROR (1)

Ser/Thr Protease (1)

STING (1)

Tim3 (1)

YAP (1)

γ-secretase (2)

By Research Areas:

Cancer (8)

Infection (1)

Inflammation/Immunology (3)

Metabolic Disease (5)

Neurological Disease (5)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-147214

GNE-7883 5 Publications Verification	YAP	Cancer
GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .

HY-163028

ML-T7	Tim3	Cancer
ML-T7 is a potent Tim-3 inhibitor. ML-T7 blocks Tim-3 interactions with PtdSer and CEACAM1. ML-T7 not only enhances the antitumor activity of adoptive transfer therapy with cytotoxic T lymphocytes (CTLs) and CAR T cells but also increases the effector function of T cell. ML-T7 promotes NK cells’ killing activity against tumor cells and DC antigen-presenting capacity. ML-T7 directly exerts antitumor efficacy in preclinical tumor models either alone or in combination with Nivolumab (HY-P9903A). ML-T7 can be used for tumor immunotherapy research .

HY-114196

Aclimostat ZGN-1061	MetAP	Metabolic Disease
Aclimostat (ZGN-1061) is a potent inhibitor of the MetAP2 enzyme and displays favorable efficacy and safety in preclinical studies. ZGN-1061 produced similar efficacy as beloranib for weight loss, improvements in metabolic parameters in a mouse model of obesity and insulin resistance, and concordant changes in gene transcription in HepG2 cells .

HY-16632

ELND 006	γ-secretase Amyloid-β	Metabolic Disease
ELND 006 (Compound 30) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while sparing Notch signaling. It was developed through a synthetic strategy emphasizing diversity and chirality. ELND 006, along with its analog ELND007 (Compound 34), progressed into human clinical trials. In preclinical studies, both compounds demonstrated effective reduction of Aβ levels in vitro and in vivo. Comparisons with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat underscored their potency and specificity in lowering Aβ levels in cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic efficacy in Alzheimer's disease .

HY-136527

BMS-986251	ROR Interleukin Related	Inflammation/Immunology
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC₅₀ of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC₅₀ of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis) .

HY-178780

MKP10241	GPR119	Metabolic Disease
MKP10241 is an orally active GPR119 agonist. MKP10241 elevates cAMP levels in the GPR119 expressing cell line (EC₅₀: 3.7 nM). MKP10241 reduces blood glucose levels and HbA1c in acute models and a chronic diabetic mouse model. MKP10241 also demonstrates excellent preclinical efficacy in acute as well as chronic rodent models of obesity, and MASH .

HY-179004

ONO-9517601 VU6022856	Potassium Channel	Neurological Disease
ONO-9517601 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC₅₀= 0.067 μM, TREK-2 IC₅₀= 0.23 μM). ONO-9517601 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-9517601 can be used for research on neurological and cognitive disorders .

HY-117287A

Deucravacitinib hydrochloride BMS-986165 hydrochloride	Interleukin Related JAK IFNAR	Inflammation/Immunology
Deucravacitinib hydrochloride (BMS-986165 hydrochloride) is a highly selective all-site inhibitor with potent inhibitory activity against TYK2. Deucravacitinib hydrochloride can effectively block IL-12, IL-23 and type I interferon signaling. Deucravacitinib hydrochloride demonstrates significant efficacy in preclinical models of inflammatory bowel disease. Deucravacitinib hydrochloride demonstrated superiority over placebo and apremilast on multiple efficacy endpoints in moderate to severe plaque psoriasis. Deucravacitinib hydrochloride was well tolerated in inhibition .

HY-163683

EB-PSMA-617	Radionuclide-Drug Conjugates (RDCs) PSMA	Cancer
EB-PSMA-617 is a modified form of PSMA-617 that has enhanced pharmacokinetic properties by conjugating it to Evans Blue (EB) to extend its circulation half-life to improve prostate tumor uptake and radiotherapy efficacy. In preclinical studies using PC3-PIP-loaded mice, EB-PSMA-617 demonstrated prolonged blood half-life, increased accumulation in PSMA-positive tumors, and successful tumor elimination with lower radioactivity .

HY-179005

ONO-7927846 VU6024391	Potassium Channel	Neurological Disease
ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC₅₀= 0.11 μM, TREK-2 IC₅₀= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders .

HY-168151

EGFR-IN-128	EGFR	Cancer
EGFR-IN-128 (compund 28) is a potent and selective molecule targeting wild-type EGFR Ex20Ins that demonstrates efficacy in multiple human xenograft models and can cross the blood-brain barrier in preclinical species .

HY-114584

A-953227	Ser/Thr Protease	Neurological Disease
A-953227 is a highly potent and selective inhibitor with the activity of inhibiting calcium-dependent esterase (calpain). A-953227 has enhanced selectivity for related cysteine proteases (cathepsins) and has shown good efficacy in cell experiments. A-953227 has shown broad efficacy in preclinical models for Alzheimer's disease, suggesting that it has potential benefits in inhibiting Alzheimer's disease .

HY-106752

CI-936 MRS-3310	Annexin A	Neurological Disease
CI-936 (MRS-3310) is an orally active A₂ agonist with 25 nM affinity. CI-936 produces potent and selective effects in preclinical tests predictive of antipsychotic efficacy. CI-936 inhibits exploratory activity in mice .

HY-116149

A-424274	nAChR	Others
A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.

HY-123582

CP-866,087	Opioid Receptor	Neurological Disease
CP-866,087 is a novel, potent and selective μ-opioid receptor antagonist with activity to inhibit opioid effects. CP-866,087 has shown promising preclinical efficacy data in disease models associated with alcohol consumption. CP-866,087 has also been used to study female sexual dysfunction .

HY-135711

PDE8B-IN-1	Phosphodiesterase (PDE)	Metabolic Disease
PDE8B-IN-1 is a selective inhibitor of phosphodiesterase 8B (PDE8B) with the activity of enhancing insulin secretion. PDE8B-IN-1 showed good efficacy in high-throughput screening and optimized its ligand efficiency through rapid deconstruction. PDE8B-IN-1 showed high target selectivity and good bioavailability in preclinical development, providing a basis for exploring its potential inhibitory use .

HY-16469

SR 13668	Akt	Cancer
SR13668 is a potent indole analog derived from indole-3-carbinol (I3C), known for its natural anticancer properties but limited by poor metabolic characteristics. Developed to enhance I3C's anticancer efficacy, SR13668 effectively inhibits growth factor-stimulated Akt activation. It demonstrates strong oral anticancer activity across different cancer types in preclinical studies, showing promise in clinical development due to its favorable safety profile and potent therapeutic effects .

HY-16633

ELND 007	γ-secretase Amyloid-β	Metabolic Disease
ELND 007 (Compound 34) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while minimizing Notch inhibition. Developed alongside ELND 006 (Compound 30), it underwent human clinical trials following a synthetic strategy emphasizing diversity and chirality. In preclinical studies, ELND 007 showed promising in vitro and in vivo characteristics, effectively reducing Aβ levels. Comparative studies with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat highlighted its efficacy in lowering Aβ production, particularly demonstrated by reduced Aβ levels in the cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic benefit for Alzheimer's disease .

HY-12193

A-349821	Histamine Receptor	Others
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .

HY-122023

TBC3486	Integrin	Inflammation/Immunology Cancer
TBC3486 is a highly selective integrin α4β1 inhibitor. TBC3486 acts as a chemosensitizer to enhance the sensitivity of leukemia cells to chemotherapy. TBC3486 exhibits efficacy in preclinical models of integrin α4-dependent inflammatory and autoimmune diseases, including a mouse model of autoimmune encephalomyelitis. TBC3486 can be used for the research of precursor B-cell acute lymphoblastic leukemia .

HY-179626

STING agonist-49	STING ADC Payload	Cancer
STING agonist-49 (Compound 1) is a STING agonist and can be used as a payload for ADCs. STING agonist-49 can be applied in lung cancer research .

HY-126929

Trioxacarcin B TXN-B	DNA Alkylator/Crosslinker Apoptosis Bacterial Parasite Fungal	Infection Cancer
Trioxacarcin B (TXN-B) is a potent cytotoxic agent and DNA-targeted inhibitor. Trioxacarcin B disrupts DNA function and induces apoptosis in cancer cells. Trioxacarcin B not only effectively inhibits the growth of various Gram-positive and Gram-negative bacteria as well as Plasmodium falciparum, but also blocks the colony formation of cancer stem cells, significantly reduces tumor volume and prolongs survival in preclinical in vivo models. The activity of Trioxacarcin B is highly dependent on its intact spiro-epoxide structure; it loses efficacy once this moiety undergoes hydrolysis, and Trioxacarcin B shows no activity against fungi, microalgae and small RNA viruses. Trioxacarcin B can be used for research on bacterial infections, malaria, and various cancers including colon cancer and melanoma .

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Preclinical efficacy

Inhibitors & Agonists