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Results for "

β-arrestins

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Arrestin (25) 5-HT Receptor (5) Adenosine Receptor (3) Adrenergic Receptor (6) Angiotensin Receptor (2) Apelin Receptor (APJ) (9) Apoptosis (1) Cannabinoid Receptor (5) CCR (1) CXCR (7) Dopamine Receptor (10) ERK (2) Free Fatty Acid Receptor (1) G Protein-coupled Receptor Kinase (GRK) (1) GHSR (2) GPR35 (3) GPR55 (3) Histamine Receptor (2) HIV (2) mAChR (1) Opioid Receptor (4) Oxytocin Receptor (1) P2Y Receptor (2) PKC (1) Protease Activated Receptor (PAR) (1) RXFP Receptor (1) Thyroid Hormone Receptor (2)
By Research Areas:	Cancer (17) Cardiovascular Disease (17) Endocrinology (8) Infection (2) Inflammation/Immunology (18) Metabolic Disease (7) Neurological Disease (26)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Peptides

Click Chemistry

Targets Recommended: Arrestin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-117829

UNC9994 1 Publications Verification	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-119706

Barbadin Maximum Cited Publications 10 Publications Verification	Apoptosis Arrestin	Others
Barbadin is a novel and selective *β-arrestin/β2-adaptin* interaction inhibitor, has IC₅₀ values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors. Barbadin can induce apoptosis .

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-123813

CCX-777	Arrestin	Cancer
CCX-777 is a partial agonist of *β-arrestin-2* recruitment to ACKR3 (atypical chemokine receptor 3) .

HY-119486A

(Rac)-Tavapadon (Rac)-PF-06649751; (Rac)-CVL-751	Dopamine Receptor Arrestin	Neurological Disease
(Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the *β-arrestin2* recruitment assay (GS-cAMP, EC₅₀=0.8 nM; β-arrestin2, EC₅₀=68 nM). (Rac)-Tavapadon has antiparkinsonian activity .

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-116445

UNC9975	Others	Neurological Disease
UNC9975 is a D₂R agonist that displays signaling bias via β-arrestin–ergic signaling and a simultaneously antagonist of Gi-regulated cAMP production and partial agonist for D₂R/β-arrestin-2 interactions. UNC9975 can be utilized in antipsychotic research .

HY-149336

D1R antagonist 1	Dopamine Receptor	Neurological Disease
D1R antagonist 1 (compound 12a) is a D1R antagonist, involved in G-protein- and β-arrestin-based signaling .

HY-159177

M4 mAChR Modulator-1	mAChR	Neurological Disease
M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment .

HY-155099

FGH31	Dopamine Receptor Arrestin G Protein-coupled Receptor Kinase (GRK)	Neurological Disease
FGH31 (Compound 24) is a potent, selective, GRK2 dependency dopamine D4 agonist, with the K_i of 1.6 nM. FGH31 partial activates *β- arrestin* .

HY-125020

NCGC00135472	Others	Inflammation/Immunology
NCGC00135472 is a potent agonist of resolvin D1 receptor (DRV1), with the EC₅₀ of 0.37 nM and 0.05 μM for β-arrestin and cAMP activities, respectively .

HY-122246

ML192	GPR55 PKC ERK Arrestin	Metabolic Disease
ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the *β-arrestin* trafficking, ERK1/2 phosphorylation and PKCβII translocation .

HY-15705

GPR35 agonist 2	GPR35 Arrestin	Metabolic Disease Inflammation/Immunology
GPR35 agonist 2 (compound 11) is a potent agonist of GPR35, with EC₅₀s of 26 and 3.2 nM in the *β-arrestin* and Ca ²⁺ release assay, respectively .

HY-160187

AAA	Others	Cardiovascular Disease
AAA is a potent blocker of 20-Hydroxyeicosatetraenoic acid (20-HETE) receptor that binds directly to GPR75 and prevents the increases in intracellular Ca2+, IP-1 and β-arrestin .

HY-117295A

7-Fluorotryptamine hydrochloride	Arrestin	Inflammation/Immunology Cancer
7-Fluorotryptamine hydrochloride is a potent agonist of GPRC5A. 7-Fluorotryptamine hydrochloride induces GPRC5A-mediated β-arrestin recruitment. 7-Fluorotryptamine hydrochloride can be used for research of immune and cancer signaling .

HY-P2197

ELA-11(human)	Apelin Receptor (APJ) Arrestin	Inflammation/Immunology
ELA-11(human), a peptide, is a full agonist of human apelin receptor, with a pK_i of 7.85. ELA-11(human) completely inhibits Forskolin-induced cAMP production and stimulates *β-arrestin* recruitment .

HY-156157

GPR55 agonist 4	GPR55	Cancer
GPR55 agonist 4 (Compound 28) is a GPR55 agonist (EC₅₀: 131 nM, and 1.41 nM for hGPR55 and rGPR55). GPR55 agonist 4 induces β-arrestin recruitment to human GPR55 .

HY-161717

MRS5663	Adenosine Receptor	Cardiovascular Disease
MRS5663 (Compound 3a) is an A3AR agonist, with an EC₅₀ of 5.62 nM for β-arrestin2 recruitment assay. MRS5663 has a cytoprotective effect on skeletal muscle ischemia-reperfusion injury/claudication model .

HY-160628

GPR120 Agonist 4	Free Fatty Acid Receptor	Metabolic Disease
GPR120 Agonist 4 (example 1) is a GPR120 agonist，with the EC₅₀ values of 1 μM and 0.35 μM for β-arrestin A and Calcium A. GPR120 Agonist 4 can be used for the research of type II diabetes mellitus .

HY-122197

ML339	CXCR Apelin Receptor (APJ) Arrestin	Cancer
ML339 is a selective CXCR6 antagonist with an IC₅₀ of 140 nM. ML339 antagonizes *β-arrestin* recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC₅₀ of 0.3 μM and 1.4 μM, respectively. ML339 shows weaker activity against the recruitment of *β-arrestin* in mouse CXCR6 receptors, with an IC₅₀ of 18 μM. ML339 has no inhibitory effect on CXCR5，CXCR4，CXCR6 and apelin receptor (APJ), with IC₅₀ >79 μM. ML339 has the potential to promote the development of prostate cancer research .

HY-156107

GPR55 agonist 3	GPR55	Cancer
GPR55 agonist 3 (Compound 26) is a GPR55 agonist (EC₅₀: 0.239 nM, and 1.76 nM for hGPR55 and rGPR55). GPR55 agonist 3 induces β-arrestin recruitment to human GPR55 (EC₅₀: 6.2 nM) .

HY-100677

VUF11207	CXCR	Endocrinology
VUF11207 (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pK_i of 8.1) ligand that induces recruitment of *β-arrestin2* (pEC₅₀ of 8.8) and subsequent internalization (pEC₅₀ of 7.9) of CXCR7 .

HY-147751

APJ receptor agonist 6	Arrestin Apelin Receptor (APJ)	Cardiovascular Disease
APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with K_i of 1.3 μM. APJ receptor agonist 6 has EC₅₀ values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and *β-arrestin*, respectively .

HY-103254

ML221 5+ Cited Publications	Arrestin Apelin Receptor (APJ)	Neurological Disease
ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC₅₀s of 0.70 μM in the cAMP assay, and 1.75 μM in the *β-arrestin* assay, and EC₈₀ of 10 nM in both assays.

HY-150056

CB1R Allosteric modulator 3	Cannabinoid Receptor Arrestin	Neurological Disease
CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and *β-Arrestin* with EC₅₀ values of 0.018 μM and 1.241 μM, respectively .

HY-P5017

(Val3,Pro8)-Oxytocin	Oxytocin Receptor	Endocrinology
(Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. (Val3,Pro8)-Oxytocin is also a weaker agonist for the *β-arrestin* engagement and endocytosis toward the oxytocin receptor (OXTR) .

HY-P2249

ELA-21 (human)	Arrestin Apelin Receptor (APJ)	Cardiovascular Disease
ELA-21 (human) is an apelin receptor agonist with a pK_i of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates *β-arrestin* recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways .

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-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-149337

D3R ligand 1	Dopamine Receptor	Neurological Disease
D3R ligand 1 (compound 23b) is a potent and selective ligand of dopamine receptor D3R (Ki=66 nM), containing a THPB template. D3R ligand 1 is also an antagonist for both G-protein- and β-arrestin-based signaling .

HY-150057

CB1R Allosteric modulator 4	Cannabinoid Receptor	Others
CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .

HY-113689

GAT211	Cannabinoid Receptor	Neurological Disease
GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC₅₀ values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research .

HY-108742

Abaloparatide 1 Publications Verification BA 058; BIM 44058	Thyroid Hormone Receptor Arrestin	Metabolic Disease
Abaloparatide (BA 058) is a parathyroid hormone receptor 1 (PTHR1) analog. Abaloparatide also is a selective PTHR1 activator. Abaloparatide enhances Gs/cAMP signaling and *β-arrestin* recruitment. Abaloparatide enhances bone formation and cortical structure in mice. Abaloparatide has the potential for the research of osteoporosis .

HY-108656A

MRS2365 trisodium	P2Y Receptor Arrestin	Cardiovascular Disease
MRS2365 trisodium is a potent and selective P2Y1 receptor (EC₅₀=0.4 nM)/[ ³⁵S]GTPγS binding/β-arrestin 2 recruitment agonist. MRS2365 trisodium relieves mechanical allodynia and increases mechanical sensitivity .

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-163277

PIPE-3297	Opioid Receptor	Inflammation/Immunology
PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC₅₀ of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .

HY-162728

RO-76	Opioid Receptor	Neurological Disease
RO-76 is a mu opioid receptor (μOR) selective partial agonist. RO-76 binds to μOR-G-protein complex with an EC₅₀ value of 454 nM. RO-76 reduces β-Arrestin-1/2 recruitment. RO-76 shows antinociception activity .

HY-W010907

Pamoic acid disodium 2 Publications Verification	GPR35 ERK	Neurological Disease
Pamoic acid disodium is a potent GPR35 agonist with an EC₅₀ value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC₅₀ values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect .

HY-P1102

TC14012 2 Publications Verification	CXCR HIV	Infection Cancer
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC₅₀ of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC₅₀ of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity .

HY-P2197A

ELA-11(human) TFA	Apelin Receptor (APJ)	Inflammation/Immunology
ELA-11(human) TFA is a high affinity apelin receptor agonist (K_i=14 nM). ELA-11(human) TFA is a bioactive fragment of ELA-32. ELA-11(human) TFA inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.

HY-108742A

Abaloparatide TFA 1 Publications Verification BA 058 TFA; BIM 44058 TFA	Thyroid Hormone Receptor Arrestin	Metabolic Disease Endocrinology
Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue. Abaloparatide TFA also is a selective PTHR1 activator. Abaloparatide TFA enhances Gs/cAMP signaling and *β-arrestin* recruitment. Abaloparatide TFA enhances bone formation and cortical structure in mice. Abaloparatide TFA has the potential for the research of osteoporosis .

HY-P1102A

TC14012 TFA	CXCR HIV	Infection Cancer
TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC₅₀ of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC₅₀ of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity .

HY-145278

RXFP3/4 agonist 2	RXFP Receptor	Neurological Disease
RXFP3/4 agonist 2 is a potent, nonpeptide dual RXFP3/4 agonist (EC₅₀=3.1 and 2.7 nM). RXFP3/4 agonist 2 also potently promotes interactions between RXFP3 and β-arrestin-2 with EC₅₀ values in the range of 10-22 nM .

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-119234

CX4338	Others	Inflammation/Immunology
CX4338 is a CXCL8-mediated chemokine inhibitor with the activity of inhibiting CXCR2-mediated cell migration. CX4338 selectively inhibits CXCR2-mediated β-arrestin-2 recruitment and receptor internalization while enhancing CXCR2-mediated MAPK activation. CX4338 also inhibited CXCL8-induced chemotaxis, showing efficacy in CXCR2-overexpressing cells and human neutrophils. In vivo, CX4338 significantly reduced LPS-induced neutrophil numbers in mouse bronchoalveolar lavage fluid. The mechanism of action of CX4338 is to selectively inhibit CXCR2-mediated β-arrestin-2 activation, which is sufficient to inhibit CXCL8-mediated chemotaxis .

HY-155183

A3AR agonist 1	Adenosine Receptor	Inflammation/Immunology Cancer
A3AR agonist 1 (Compound 12) is an A3AR agonist (K_i: 25.8 nM). A3AR agonist 1 stimulates β-arrestin2 recruitment, with an EC₅₀ value of 5.17 nM. A3AR agonist 1 can be used for research of inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, etc .

HY-162495

IDOR-1117-2520	CCR	Inflammation/Immunology
IDOR-1117-2520 is a potent and selective antagonist of CCR6. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC₅₀ = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC₅₀ = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 can be used for research of autoimmune diseases .

HY-14299

Indacaterol 4 Publications Verification	Adrenergic Receptor	Cardiovascular Disease Endocrinology Cancer
Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol inhibits NF-κB activity in a *β-arrestin2*-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research .

Cat. No.	Product Name	Target	Research Area

HY-P2197

ELA-11(human)	Apelin Receptor (APJ) Arrestin	Inflammation/Immunology
ELA-11(human), a peptide, is a full agonist of human apelin receptor, with a pK_i of 7.85. ELA-11(human) completely inhibits Forskolin-induced cAMP production and stimulates *β-arrestin* recruitment .

HY-P2249

ELA-21 (human)	Arrestin Apelin Receptor (APJ)	Cardiovascular Disease
ELA-21 (human) is an apelin receptor agonist with a pK_i of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates *β-arrestin* recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways .

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-108742

Abaloparatide 1 Publications Verification BA 058; BIM 44058	Thyroid Hormone Receptor Arrestin	Metabolic Disease
Abaloparatide (BA 058) is a parathyroid hormone receptor 1 (PTHR1) analog. Abaloparatide also is a selective PTHR1 activator. Abaloparatide enhances Gs/cAMP signaling and *β-arrestin* recruitment. Abaloparatide enhances bone formation and cortical structure in mice. Abaloparatide has the potential for the research of osteoporosis .

HY-P1102

TC14012 2 Publications Verification	CXCR HIV	Infection Cancer
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC₅₀ of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC₅₀ of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity .

HY-P10333

LIH383	Peptides	Neurological Disease Inflammation/Immunology
LIH383 is an agonist of ACKR3 (CXCR7) (EC₅₀=0.61 nM). LIH383 efficiently induces the recruitment of β-arrestin to ACKR3 but does not trigger typical G protein signaling .

HY-P5017

(Val3,Pro8)-Oxytocin	Oxytocin Receptor	Endocrinology
(Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. (Val3,Pro8)-Oxytocin is also a weaker agonist for the *β-arrestin* engagement and endocytosis toward the oxytocin receptor (OXTR) .

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-P2197A

ELA-11(human) TFA	Apelin Receptor (APJ)	Inflammation/Immunology
ELA-11(human) TFA is a high affinity apelin receptor agonist (K_i=14 nM). ELA-11(human) TFA is a bioactive fragment of ELA-32. ELA-11(human) TFA inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.

HY-108742A

Abaloparatide TFA 1 Publications Verification BA 058 TFA; BIM 44058 TFA	Thyroid Hormone Receptor Arrestin	Metabolic Disease Endocrinology
Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue. Abaloparatide TFA also is a selective PTHR1 activator. Abaloparatide TFA enhances Gs/cAMP signaling and *β-arrestin* recruitment. Abaloparatide TFA enhances bone formation and cortical structure in mice. Abaloparatide TFA has the potential for the research of osteoporosis .

HY-P1102A

TC14012 TFA	CXCR HIV	Infection Cancer
TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC₅₀ of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC₅₀ of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity .

HY-P2106

Elabela(19-32) 3 Publications Verification	Arrestin Apelin Receptor (APJ)	Cardiovascular Disease
Elabela(19-32) is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) activates the G_αi1 and *β-arrestin-2* signaling pathways with EC₅₀s of 8.6 nM and 166 nM. Elabela(19-32) induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .

HY-P3910

[Val4] Angiotensin III	Peptides	Cardiovascular Disease
[Val4] Angiotensin III is an angiotension III peptide. [Val4] Angiotensin III is a potent full agonist of Gα_q and βarr2 response, with pEC₅₀ values of 8.31 and 8.44, respectively .

HY-P2106A

Elabela(19-32) TFA 3 Publications Verification	Apelin Receptor (APJ) Arrestin	Cardiovascular Disease
Elabela(19-32) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the G_αi1 and *β-arrestin-2* signaling pathways with EC₅₀s of 8.6 nM and 166 nM. Elabela(19-32) TFA induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .

HY-P1682

Balixafortide POL6326	CXCR Arrestin	Cancer
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC₅₀ < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks *β-arrestin* recruitment and calcium flux with IC₅₀s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .

HY-P1682A

Balixafortide TFA 1 Publications Verification POL6326 TFA	CXCR Arrestin	Cancer
Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC₅₀ < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks *β-arrestin* recruitment and calcium flux with IC₅₀s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .

Cat. No.	Product Name		Classification

HY-155480

PSB-22034		Alkynes
PSB-22034 (compound 30d) is a selective agonist of MRGPRX4 with EC₅₀s of 11.2 nM and 30.0 nM in Ca ²⁺ and β-arrestin experiments, respectively .

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