Search Result

Results for "

biased

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (6) Angiotensin Receptor (5) Apelin Receptor (APJ) (3) Arrestin (4) Biochemical Assay Reagents (1) Bombesin Receptor (1) Cannabinoid Receptor (1) CXCR (2) Dopamine Receptor (7) G protein-coupled Bile Acid Receptor 1 (2) GABA Receptor (1) GCGR (1) GPR84 (3) Histamine Receptor (1) Interleukin Related (1) JNK (1) LPL Receptor (1) mGluR (1) nAChR (1) Opioid Receptor (2) PERK (1) Protease Activated Receptor (PAR) (2) RXFP Receptor (1)
By Research Areas:	Cancer (6) Cardiovascular Disease (9) Endocrinology (2) Inflammation/Immunology (11) Metabolic Disease (1) Neurological Disease (18)

By Targets:

5-HT Receptor (6)

Angiotensin Receptor (5)

Apelin Receptor (APJ) (3)

Arrestin (4)

Biochemical Assay Reagents (1)

Bombesin Receptor (1)

Cannabinoid Receptor (1)

CXCR (2)

Dopamine Receptor (7)

G protein-coupled Bile Acid Receptor 1 (2)

GABA Receptor (1)

GCGR (1)

GPR84 (3)

Histamine Receptor (1)

Interleukin Related (1)

JNK (1)

LPL Receptor (1)

mGluR (1)

nAChR (1)

Opioid Receptor (2)

PERK (1)

Protease Activated Receptor (PAR) (2)

RXFP Receptor (1)

By Research Areas:

Cancer (6)

Cardiovascular Disease (9)

Endocrinology (2)

Inflammation/Immunology (11)

Metabolic Disease (1)

Neurological Disease (18)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-128121

MLS1547	Dopamine Receptor	Neurological Disease
MLS1547 is a highly efficacious *G protein-biased* dopamine D2 receptor (D2R) agonist (K_i=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC₅₀**=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC₅₀=9.9 μM) .

HY-W040201

CHAPSO 3-[3-(Cholamidopropyl)dimethylammonio]-2-hydroxy-1-propanesulfonate	Biochemical Assay Reagents	Others
CHAPSO is a zwitterionic detergent that is thermally stable. CHAPSO is able to broaden the particle orientation distribution, enabling single-particle cryo-electron microscopy (cryo-EM) to produce isotropically uniform maps. CHAPSO can eliminate the directional bias of bacterial transcription complexes and help determine the structure of bacterial transcription complexes under cryo-electron microscopy .

HY-138951

AY77	Protease Activated Receptor (PAR)	Inflammation/Immunology Cancer
AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC₅₀ of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca ²⁺ release .

HY-P3259

AY254	Protease Activated Receptor (PAR)	Inflammation/Immunology Cancer
AY254 is an analogue of AY77 (HY-138951). AY254 is ERK-biased PAR2 agonist with an EC₅₀ of 2 nM. AY254 relieves cytokine-induced caspase 3/8 activation. AY254 also promotes scratch-wound healing and induced IL-8 secretion via PAR2-ERK1/2 signaling

HY-156025

HCAR2 agonist 1	Others	Inflammation/Immunology
HCAR2 agonist 1 (Compound 9n) is a G_i protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the G_i protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis .

HY-P3136

TRV055	Angiotensin Receptor	Cardiovascular Disease
TRV055, a G-protein-biased agonist, is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling .

HY-P3136A

TRV055 hydrochloride	Angiotensin Receptor	Cardiovascular Disease
TRV055 hydrochloride, a G-protein-biased agonist, is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 hydrochloride is efficacious in stimulating cellular Gq-mediated signaling .

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-108003

MM 07

Apelin Receptor (APJ) Cardiovascular Disease

MM 07 is a biased apelin receptor agonist, with a K_D of 300 nM in CHO-K1 cells and a K_D of 172 nM in human heart.
HY-19863

F-15599

2 Publications Verification

NLX-101
5-HT Receptor Neurological Disease

F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with K_i of 3.4 nM.

MM 07	Apelin Receptor (APJ)	Cardiovascular Disease
MM 07 is a biased apelin receptor agonist, with a K_D of 300 nM in CHO-K1 cells and a K_D of 172 nM in human heart.

F-15599 2 Publications Verification NLX-101	5-HT Receptor	Neurological Disease
F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with K_i of 3.4 nM.

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-16642A

LY2828360	Cannabinoid Receptor	Neurological Disease
LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB₂) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.

HY-139677

5-HT7R antagonist 1

G protein-coupled Bile Acid Receptor 1 Neurological Disease

5-HT7R antagonist 1 is a G protein-biased antagonist against 5-HT₇R (K_i = 6.5 nM).

5-HT7R antagonist 1	G protein-coupled Bile Acid Receptor 1	Neurological Disease
5-HT7R antagonist 1 is a G protein-biased antagonist against 5-HT₇R (K_i = 6.5 nM).

HY-P3347

NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal)	Apelin Receptor (APJ)	Cardiovascular Disease
NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) (compound 40), a macrocyclic analogue of Ape13, is a potent APJ agonist (K_i=5.7 nM). NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) exhibits a favorable Gα12-biased signaling and an increased in vivo half-life .

HY-128901

F 13714 fumarate F 14679 fumarate	5-HT Receptor	Neurological Disease
F13714 fumarate, a selective 5-HT1A receptor biased agonist, shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress .

HY-139677A

5-HT7R antagonist 1 free base	G protein-coupled Bile Acid Receptor 1	Neurological Disease
5-HT7R antagonist 1 (free base) is a G protein-biased antagonist against 5-HT₇R (K_i = 6.5 nM).

HY-P3366

Ecnoglutide XW003	GCGR	Metabolic Disease
Ecnoglutide (XW003) is a long-acting, cAMP-biased glucagon-like peptide 1 (GLP-1) receptor agonist. Ecnoglutide can be used for research of T2DM and obesity .

HY-161106

OX04528	GPR84	Inflammation/Immunology Cancer
OX04528 (compound 68) is a potent, G-protein biased, and orally active GPR84 agonist. OX04528 no cytotoxicity. OX04528 inhibits cAMP production with an EC₅₀ value of 0.00598 nM .

HY-120920

UNC9995	Dopamine Receptor	Inflammation/Immunology
UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions .

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-112606

ML-290	RXFP Receptor	Others
ML-290 is a first-in-class and potent relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes, with an EC₅₀ of 94 nM . ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.

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-161107

OX04529	GPR84	Inflammation/Immunology
OX04529 (compound 69) is a potent, selective and orally active agonist of GPR84. OX04529 inhibits FSK-induced cAMP production with an EC₅₀ of 0.0185 nM. OX04529 displayed excellent potency, high G-protein signaling bias .

HY-145869

Anti-inflammatory agent 12	Others	Inflammation/Immunology
Anti-inflammatory agent 12 (Compound 2) is a pentacyclic triterpene compound. Anti-inflammatory agent 12 shows a significant bias in the LPS-induced inflammatory response with an IIC₅₀ value of 2.22 μM. Anti-inflammatory agent 12 has the potential for the research of inflammation disease .

HY-110302

6'-GNTI dihydrochloride	Opioid Receptor	Neurological Disease
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .

HY-145698

UCSF678	5-HT Receptor	Neurological Disease
UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT_5AR with a more restricted off-target profile and decreased assay liabilities. UCSF678 is a selective probe with which to study the function of the 5-HT_5AR .

HY-126346

DL-175	GPR84	Inflammation/Immunology
DL-175 (compound 13) is a selective GPR84 agonist with biased agonistic activity. DL-175 can selectively activate functional responses in immune cells and induce enhanced chemotaxis and phagocytosis of human bone marrow cells. DL-175 is a potential chemical probe .

HY-P2141A

TRV-120027 TFA 3 Publications Verification	Angiotensin Receptor Arrestin	Cardiovascular Disease
TRV120027 TFA, a *β-arrestin-1*-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment .

HY-P2141

TRV-120027 3 Publications Verification	Angiotensin Receptor Arrestin	Cardiovascular Disease
TRV120027, a *β-arrestin-1*-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment .

HY-157429

25N-N1-Nap	5-HT Receptor	Neurological Disease
25N-N1-Nap (compound 16) is a β-arrestin-biased 5-HT2A agonist. 25N-N1-Nap antagonizes phencyclidine induced hyperactivity in Male C57BL/6?J mice .

HY-101121

NI-42
NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC₅₀s of BRPF1/2/3=7.9/48/260 nM; K_ds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins .

HY-P5839

α-Conotoxin MrIC	nAChR	Neurological Disease
α-Conotoxin MrIC is an α7nAChR biased agonist. α-Conotoxin MrIC exclusively activates α7nAChR regulated by type II positive allosteric modulators, including PNU120596. α-Conotoxin MrIC can be used to study neurological diseases and also to probe the pharmacological properties of α7nAChR .

HY-103080

CMF019	Apelin Receptor (APJ)	Cardiovascular Disease
CMF019 is a potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents . Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin .

HY-117829

UNC9994	Dopamine Receptor 5-HT Receptor Histamine Receptor Arrestin	Neurological Disease
UNC9994, an analog of Aripiprazole, is a functionally selective *β-arrestin-biased* dopamine D2 receptor (D2R) agonist with EC₅₀** <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of G_i-regulated cAMP production. Antipsychotic Activity .

HY-111385

UNC9994 hydrochloride 1 Publications Verification	Dopamine Receptor 5-HT Receptor Arrestin	Neurological Disease
UNC9994 hydrochloride is a functionally selective, *β-arrestin–biased* dopamine D₂ receptor (D₂R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a K_i of 79 nM for D₂R. UNC9994 hydrochloride is also an antagonist of G_i-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity .

HY-125751

UCSF924	Dopamine Receptor	Neurological Disease
UCSF924 is a potent and specific dopamine D4 receptor (DRD4) partial agonist with a EC₅₀ of 4.2 nM. UCSF924 has a high-affinity with a K_i value of 3 nM for DRD4 and shows no measurable affinity for D2, D3 or the F261V/L328F D4 mutant. UCSF924 is a 7.4-fold bias toward arrestin over Gαi/o signaling, referenced to quinpirole .

HY-115831

SAR247799 S1P1 agonist 3	LPL Receptor	Cardiovascular Disease
SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC₅₀s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome .

HY-P0172A

ATI-2341 TFA 2 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-P0172

ATI-2341	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-114978

VU0424465	mGluR PERK	Neurological Disease
VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu₅ mediated iCa ²⁺ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a K_i value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons .

HY-103475

GS39783	GABA Receptor	Neurological Disease
GS39783 is a positive allosteric modulator (PAM) of GABA_BR. Positive modulation of the GABA_BR can be used for the research of Nicotine addiction .

HY-103544

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P	JNK Interleukin Related Bombesin Receptor	Inflammation/Immunology Cancer
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P, a Substance P derivative, is a biased agonist toward neuropeptide and chemokine receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P activates G12. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P binds to IL-8 and GRP receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P inhibits ERK-2 activation, activates JNK activity. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P stimulates an increase in neutrophil migration and Ca ²⁺ mobilization. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P is also a bombesin antagonist, and inhibits the growth of small cell lung cancer

Allosteric Modulators (AMs) Compound Library	174 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 174 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

CHAPSO 3-[3-(Cholamidopropyl)dimethylammonio]-2-hydroxy-1-propanesulfonate	Surfactants
CHAPSO is a zwitterionic detergent that is thermally stable. CHAPSO is able to broaden the particle orientation distribution, enabling single-particle cryo-electron microscopy (cryo-EM) to produce isotropically uniform maps. CHAPSO can eliminate the directional bias of bacterial transcription complexes and help determine the structure of bacterial transcription complexes under cryo-electron microscopy .

Cat. No.	Product Name	Target	Research Area