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D4R

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (1) Dopamine Receptor (11) Endogenous Metabolite (1) Histone Demethylase (1) Isotope-Labeled Compounds (4) Mitochondrial Metabolism (1) PERK (1) Reactive Oxygen Species (ROS) (2) Reference Standards (1) Small Interfering RNA (siRNA) (1) TLK (1)
By Research Areas:	Cancer (3) Inflammation/Immunology (1) Neurological Disease (11)
Oligonucleotides:	Mouse Pre-designed siRNA Sets (1) siRNAs (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-108751

Aripiprazole Lauroxil 2 Publications Verification	Dopamine Receptor	Neurological Disease
Aripiprazole lauroxil, an N-acyloxymethyl proagent of Aripiprazole (HY-14546), is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia and a ligand of dopamine receptor *D2R/D4R*. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity.

HY-163703

D4R antagonist-2	Dopamine Receptor	Neurological Disease
D4R antagonist-2 (compound 33) is a *D4R* antagonist. D4R antagonist-2 has a IC₅₀ value of 210 nM, and a Ki value of 59 nM for D4R. D4R antagonist-2 can be used in the Parkinson's disease research .

HY-149481

D4R agonist-1	Dopamine Receptor	Neurological Disease
D4R agonist-1 (Compound 16f) is a *D4R* partial agonist (K_i: 2.2 nM). D4R agonist-1 is metabolically stable in rat and human liver microsomes. D4R agonist-1 can be used for research of neuropsychiatric disorders .

HY-145905

D4R antagonist-1	Dopamine Receptor	Neurological Disease
D4R antagonist-1 is a potent and selective *D4R* antagonist with an IC₅₀ of 6.87 µM. D4R antagonist-1 has the potential for the research of Parkinson’s disease .

HY-145906

D4R antagonis-2	Dopamine Receptor	Neurological Disease
D4R antagonist-2 is a potent and selective *D4R* antagonist with an IC₅₀ of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease .

HY-175504

MLS6357	Dopamine Receptor PERK	Neurological Disease
MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC₅₀s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC₅₀ > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC₅₀ of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder .

HY-149213

LSD1/TLK1-IN-1 J54; J3-54	Histone Demethylase TLK	Cancer
LSD1/TLK1-IN-1 is an orally active LSD1, TLK1, TLK2, TTK inhibitor with an LSD1 IC₅₀ of 0.247 μM. LSD1/TLK1-IN-1 suppresses phosphorylation of Nek1 at T141 and Rad9 at S328, abrogates the TLK1>Nek1>ATR>Chk1 axis, protects H3K4me1/2 from demethylation, and does not affect LSD2, MAO-A, or MAO-B. LSD1/TLK1-IN-1 induces apoptosis, bypasses cell-cycle arrest, suppresses tumor growth, acts as a weak *D4R* antagonist, downregulates PD-L1 expression, enhances T-cell killing response, inhibits gastric cancer cell proliferation, shows minimal toxicity, and has no significant effect on normal prostate cells. LSD1/TLK1-IN-1 can be used for the research of prostate cancer and gastric cancer .

HY-108751R

Aripiprazole Lauroxil (Standard)	Others Reference Standards	Neurological Disease
Aripiprazole Lauroxil (Standard) is the analytical standard of Aripiprazole Lauroxil. This product is intended for research and analytical applications. Aripiprazole lauroxil, an N-acyloxymethyl proagent of Aripiprazole (HY-14546), is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia and a ligand of dopamine receptor D2R/D4R. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity.

HY-101384

Ro 10-5824	Dopamine Receptor	Neurological Disease
Ro 10-5824 is a potent and selective *D4R* partial agonist with a K_i of 5.2 nM. Ro 10-5824 increases novel object exploration in C57 mice .

HY-B1470S

Azaperone-d4 R-1929-d₄	Isotope-Labeled Compounds Dopamine Receptor Adrenergic Receptor	Neurological Disease
Azaperone-d₄ (R-1929-d₄) is the deuterium labeled Azaperone (HY-B1470). Azaperone is an antagonist of dopamine D2 receptor (Dopamine D2 Receptor) and α-adrenergic receptor (AR). Azaperone reduces vasomotor tone, mean arterial pressure, hematocrit, hemoglobin concentration, and etorphine-induced duration; induces transient tachycardia followed by bradycardia, splenic uptake of red blood cells, and sedation; alters animal behaviors; and produces sedation with distinct onset and duration in foals. Azaperone is used for sedation and tranquilization in various animals to reduce stress and aggressive behaviors, and serves as a preanesthetic agent.

HY-173431

Dopamine D4 receptor ligand 3	Dopamine Receptor Reactive Oxygen Species (ROS)	Cancer
Dopamine D4 receptor ligand 3 (Compound 16) is a dopamine D4 receptor (D4R) antagonist (pK_i: 8.86). Dopamine D4 receptor ligand 3 has pIC₅₀ values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors in HEK-293T cells, respectively. Dopamine D4 receptor ligand 3 inhibits the viability of three human glioma cell lines, U87 MG, T98G, and U251 MG. Dopamine D4 receptor ligand 3 induces ROS production and mitochondrial dysfunction in glioma cells .

HY-181049

FMJ-01-054	Dopamine Receptor	Neurological Disease
FMJ-01-054 is a selective dopamine D4 Receptor (D4R) antagonist with a K_i od 77.7 nM. FMJ-01-054 shows subtype selectivity over D2R and D3R. FMJ-01-054 inhibits D4R-mediated β-arrestin recruitment and cAMP production with IC₅₀ values of 3800 nM and 134 nM, respectively. FMJ-01-054 has desirable plasma half-life and brain exposure in rats. FMJ-01-054 can be used for the research of neurological disorders .

HY-RS04004

Drd4 Mouse Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Drd4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Drd4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Drd4 Mouse Pre-designed siRNA Set A Drd4 Mouse Pre-designed siRNA Set A

HY-118634S

trans-Resveratrol-4'-O-D-Glucuronide-d4 R-4G-d₄	Isotope-Labeled Compounds	Others
trans-Resveratrol-4'-O-D-Glucuronide-d₄ (R-4G-d₄) is deuterium labeled trans-Resveratrol-4'-O-D-Glucuronide.

HY-157075S

(Z)-Rilpivirine-d4 R278474-d₄; TMC278-d₄; DB08864-d₄	Isotope-Labeled Compounds	Others
(Z)-Rilpivirine-d₄ (R278474-d₄; TMC278-d₄; DB08864-d₄) is deuterium-labeled (Z)-Rilpivirine .

HY-18733S

Lipoic acid-d4 (R)-(+)-α-Lipoic acid-d₄; R-(+)-Thioctic acid-d₄	Isotope-Labeled Compounds Endogenous Metabolite Mitochondrial Metabolism Reactive Oxygen Species (ROS)	Inflammation/Immunology Cancer
Lipoic acid-d₄ ((R)-(+)-α-Lipoic acid-d₄) is deuterium labeled Lipoic acid. Lipoic acid ((R)-(+)-α-Lipoic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. (R)-(+)-α-Lipoic acid is more effective than racemic Lipoic acid .

HY-181047

FMJ-01-042	Dopamine Receptor	Neurological Disease
FMJ-01-042 is a blood-brain barrier-permeable, low-efficacy partial agonist with high affinity (Kᵢ = 4.33 nM) and exceptional subtype selectivity for the dopamine D4 receptor. FMJ-01-042 exhibits good metabolic stability and is suitable for research on neurological and psychiatric disorders .

Cat. No.	Product Name	Chemical Structure

HY-B1470S

Azaperone-d4
Azaperone-d₄ (R-1929-d₄) is the deuterium labeled Azaperone (HY-B1470). Azaperone is an antagonist of dopamine D2 receptor (Dopamine D2 Receptor) and α-adrenergic receptor (AR). Azaperone reduces vasomotor tone, mean arterial pressure, hematocrit, hemoglobin concentration, and etorphine-induced duration; induces transient tachycardia followed by bradycardia, splenic uptake of red blood cells, and sedation; alters animal behaviors; and produces sedation with distinct onset and duration in foals. Azaperone is used for sedation and tranquilization in various animals to reduce stress and aggressive behaviors, and serves as a preanesthetic agent.

Azaperone-d4

Azaperone-d₄ (R-1929-d₄) is the deuterium labeled Azaperone (HY-B1470). Azaperone is an antagonist of dopamine D2 receptor (Dopamine D2 Receptor) and α-adrenergic receptor (AR). Azaperone reduces vasomotor tone, mean arterial pressure, hematocrit, hemoglobin concentration, and etorphine-induced duration; induces transient tachycardia followed by bradycardia, splenic uptake of red blood cells, and sedation; alters animal behaviors; and produces sedation with distinct onset and duration in foals. Azaperone is used for sedation and tranquilization in various animals to reduce stress and aggressive behaviors, and serves as a preanesthetic agent.

HY-118634S

trans-Resveratrol-4'-O-D-Glucuronide-d4
trans-Resveratrol-4'-O-D-Glucuronide-d₄ (R-4G-d₄) is deuterium labeled trans-Resveratrol-4'-O-D-Glucuronide.

HY-157075S

(Z)-Rilpivirine-d4
(Z)-Rilpivirine-d₄ (R278474-d₄; TMC278-d₄; DB08864-d₄) is deuterium-labeled (Z)-Rilpivirine .

HY-18733S

Lipoic acid-d4
Lipoic acid-d₄ ((R)-(+)-α-Lipoic acid-d₄) is deuterium labeled Lipoic acid. Lipoic acid ((R)-(+)-α-Lipoic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. (R)-(+)-α-Lipoic acid is more effective than racemic Lipoic acid .

Drd4 Mouse Pre-designed siRNA Set A		siRNAs Mouse Pre-designed siRNA Sets
Drd4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Drd4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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