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Results for "

Biased ligand

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (2) Angiotensin Receptor (2) Arrestin (1) CXCR (2) Dopamine Receptor (3) Epigenetic Reader Domain (1) ERK (2) Opioid Receptor (3) Reference Standards (1) Transmembrane Glycoprotein (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (4) Endocrinology (2) Inflammation/Immunology (2) Neurological Disease (7)

Inhibitors & Agonists

Screening Libraries

Peptides

Targets Recommended: Target Protein Ligand-Linker Conjugates E3 Ligase Ligand-Linker Conjugates PD-1/PD-L1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P0172

ATI-2341 4 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

HY-P3137

TRV056	Angiotensin Receptor	Cardiovascular Disease
TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists .

HY-P0172A

ATI-2341 TFA 4 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

HY-171978A

LM-189 free base	Adrenergic Receptor	Cardiovascular Disease
LM-189 free base, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 free base stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 free base can be used to develop the Gαi-biased β2AR agonists .

HY-171978

LM-189	Adrenergic Receptor	Cardiovascular Disease
LM-189 is a β₂-adrenergic receptor (β₂AR) ligand and G protein-biased modulator with a human β₂AR K_i of 0.063 nM.LM-189 promotes β₂AR coupling to Gαs and Gαi heterotrimers, stabilizes distinct β₂AR conformations including a TM6 outward state, and increases β₂AR ICL2 dynamics.LM-189 restricts β₂AR ligand-binding pocket conformational heterogeneity, stabilizes polar ligand-receptor interaction networks, and exhibits bias toward Gαi signaling over Gαs signaling.LM-189 enabled cryo-EM structural characterization of the β₂AR-Gi complex.LM-189 can be used for the research of congestive heart failure .

HY-120511

KNT-127 1 Publications Verification	Opioid Receptor	Neurological Disease
KNT-127 is a selective and BBB-penetrant δ-opioid receptor (DOR) agonist (K_i = 0.16 nM). KNT-127 is highly selective to the δ receptor, with Ki values of 0.16, 21.3 and 153 nM for δ, μ and κ receptors, respectively. KNT-127 acts as a biased ligand that mainly activates cyclic adenosine monophosphate (cAMP) signaling with lower beta-arrestin signaling activation. KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 exhibits antidepressant- and anxiolytic-like effects. KNT-127 can be studied in research on neurological diseases .

HY-104006

CYM51010	Opioid Receptor	Neurological Disease
CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC₅₀ of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms .

HY-P3136

TRV055 TRV120055	Angiotensin Receptor ERK	Cardiovascular Disease
TRV055 (TRV120055) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses ^[1]

HY-117533

UNC0006	Dopamine Receptor	Neurological Disease
UNC0006 is a β-arrestin-biased dopamine D2 ligand. UNC0006 can be used in the study of antipsychotic .

HY-141495

(Rac)-Razpipadon 1 Publications Verification PW0464	Dopamine Receptor	Neurological Disease
PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC₅₀ of 5.8 nM (Gs-cAMP) .

HY-151515

Dopamine D2 receptor agonist-2	Dopamine Receptor	Neurological Disease
Dopamine D2 receptor agonist-2 (compound 36) is a potent dopamine D₂ receptor biased agonism ligand with an K_i value of 11.2 nM. Dopamine D2 receptor agonist-2 can be used to research antipsychosis .

HY-179606

RWT9996	Transmembrane Glycoprotein Arrestin ERK Epigenetic Reader Domain	Neurological Disease
RWT9996 is a balanced GPR17 antagonist. RWT9996 has an inhibitory effect on G protein activation and β-arrestin-2 recruitment induced by MDL-29951. RWT9996 inhibits the phosphorylation of ERK/CREB and the accumulation of inositol phosphate (b IP1) induced by MDL-29951. RWT9996 can be used for the study of neurological diseases .

HY-104006R

CYM51010 (Standard)	Reference Standards Opioid Receptor	Neurological Disease
CYM51010 (Standard) is the analytical standard of CYM51010 (HY-104006). This product is intended for research and analytical applications. CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC₅₀ of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms .

Cat. No.	Product Name

HY-L170

Allosteric Modulators (AMs) Compound Library	250 compounds
An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands. MCE designs a unique collection of 250 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Allosteric Modulators (AMs) Compound Library

250 compounds

An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.

MCE designs a unique collection of 250 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Cat. No.	Product Name	Target	Research Area

HY-P0172

ATI-2341 4 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

HY-P3137

TRV056	Angiotensin Receptor	Cardiovascular Disease
TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists .

HY-P0172A

ATI-2341 TFA 4 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

HY-P3136

TRV055 TRV120055	Angiotensin Receptor ERK	Cardiovascular Disease
TRV055 (TRV120055) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses ^[1]

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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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