88 Results for "

agonist potency

" in MedChemExpress (MCE) Product Catalog:
Products (88)

88 Results for "agonist potency" in MCE Product Catalog:

7
7 Publications Verification
Cat. No.: HY-10569
CAS No.: 854107-55-4
Purity:  99.78%
Synonyms: ACT-128800
Target:  

LPL Receptor

Research Areas:  

Inflammation/Immunology

Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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6
6 Cited Publications
Cat. No.: HY-131615
CAS No.: 2804595-86-4
Purity:  99.79%
Target:  

Sodium Channel

Research Areas:  

Others

TPC2-A1-P is a powerful and membrane permeable agonist of two pore channel 2 (TPC2) with an EC50 of 10.5 μM. TPC2-A1-P plays its role by mimicking the physiological actions of PI(3,5)P2. TPC2-A1-P also shows higher potency to induce Na 2+ mobilisation from TPC2 than TPC-A1-N (HY-131614). TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells .
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3
3 Cited Publications
Cat. No.: HY-14229
CAS No.: 1197300-24-5
Purity:  99.71%
Synonyms: CCDC
TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca 2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity .
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3
3 Cited Publications
Cat. No.: HY-100677
CAS No.: 1378524-41-4
Purity:  94.56%
Target:  

CXCR

Research Areas:  

Endocrinology

VUF11207 (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7 .
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2
2 Cited Publications
Cat. No.: HY-112185
CAS No.: 2212020-52-3
Purity:  99.80%
Synonyms: LY3502970; GLP-1 receptor agonist 1
Target:  

GCGR

Orforglipron (LY3502970) (Compound 67) is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorates the type 2 diabete .
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2
2 Cited Publications
Cat. No.: HY-112185A
CAS No.: 3008544-96-2
Purity:  99.71%
Synonyms: LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate
Target:  

GCGR

Orforglipron hemicalcium hydrate (LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate) is the calcium salt hydrate form of Orforglipron (HY-112185). Orforglipron is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorating the type 2 diabete .
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2
2 Cited Publications
Cat. No.: HY-109009
CAS No.: 1294000-61-5
Purity:  99.65%
Synonyms: UCB-0942
Target:  

GABA Receptor

Research Areas:  

Neurological Disease

Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .
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2
2 Cited Publications
Cat. No.: HY-110238
CAS No.: 1062271-24-2
Purity:  98.27%
Target:  

TRP Channel

Research Areas:  

Metabolic Disease

MK6-83 is a new candidate agonist of TRPML1 with an improved efficacy and potency. MK6-83 has the potential for Mucolipidosis type IV study .
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2
2 Cited Publications
Cat. No.: HY-121885
CAS No.: 950195-51-4
Purity:  99.35%
Target:  

CCR

Research Areas:  

Metabolic Disease Endocrinology

LMD-009 is a selective CCR8 nonpeptide agonist. LMD-009 mediates chemotaxis, inositol phosphate accumulation, and calcium release in high potencies with EC50s from 11 to 87 nM .
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1
1 Cited Publications
Cat. No.: HY-10624
CAS No.: 312637-48-2
Purity:  98.28%
Target:  

Melanocortin Receptor

Research Areas:  

Metabolic Disease

THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants .
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1
1 Cited Publications
Cat. No.: HY-107327
CAS No.: 57775-29-8
Purity:  99.71%
Synonyms: (±)-Carazolol; DL-Carazolol; Suacron
Target:  

Adrenergic Receptor

Research Areas:  

Cardiovascular Disease

Carazolol is a β12 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist .
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Cat. No.: HY-147637
CAS No.: 2611459-57-3
Purity:  99.32%
Target:  

Ephrin Receptor

Research Areas:  

Cancer

EphA2 agonist 1 (Compound 7bg) is a potent EphA2 receptor agonist. EphA2 agonist 1 shows great potency and selectivity toward EphA2 overexpressed glioblastoma cells and stimulates EphA2 phosphorylation .
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Cat. No.: HY-128865
CAS No.: 2059904-66-2
Purity:  98.32%
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects .
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Cat. No.: HY-W270810
CAS No.: 360778-55-8
Research Areas:  

Cancer

NR4A agonist-1, a fatty acid mimetic (FAM), is a potent NR4A agonist. NR4A agonist-1 exhibits high agonist potency on NR4A receptors Nurr1, Nur77, and NOR-1, with EC50s of 0.09 μM, 0.04 μM, and 0.15 μM, respectively .
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Cat. No.: HY-108258
CAS No.: 388575-52-8
Purity:  99.96%
Target:  

GPR119

Research Areas:  

Endocrinology

PSN 375963 is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 shows similar potency to the endogenous agonist oleoylethanolamide (OEA) .
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Cat. No.: HY-P2249
CAS No.: 2245073-05-4
Research Areas:  

Cardiovascular Disease

ELA-21 (human) is an apelin receptor agonist with a pKi 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 .
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Cat. No.: HY-129683
CAS No.: 213182-22-0
Purity:  ≥98.0%
Target:  

PPAR

Research Areas:  

Metabolic Disease

AM3102 is an oleoylethanolamide (OEA) analog. AM3102 is an endogenous high-affinity PPAR-alpha agonist. AM3102 resists enzymatic hydrolysis, activates PPAR-alpha with high potency in vitro, and persistently reduces feeding when administered in vivo either parenterally or orally .
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Cat. No.: HY-P11320
CAS No.: 863919-85-1
Research Areas:  

Metabolic Disease

Davalintide is an Amylin (HY-P1464)-mimetic peptide with greater potency and longer-lasting effects. Davalintide is a potent agonist of amylin receptor (IC50 = 0.04 nM), calcitonin receptor (IC50 = 0.06 nM) and calcitonin related peptide receptor (CGRP receptor) (IC50 = 3.1 nM). Davalintide shows stronger potency to Amylin to activate cyclic AMP production through the calcitonin receptor (EC50 = 1.4 nM). Davalintide regulates blood sugar and weight through various mechanisms such as delaying gastric emptying, inhibiting glucagon secretion, and reducing food intake. Davalintide can be used for the studies of anti-obesity and anti-diabetes .
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Cat. No.: HY-P10716
Target:  

GLP Receptor

Research Areas:  

Metabolic Disease

Exendin-P5 is a selective agonist that targets the GLP-1R. Exendin-P5 promotes rapid activation of G proteins by transient interactions with the transmembrane domain of GLP-1R, enhancing its potency in G protein-mediated signaling and accelerating cAMP production. This mechanism suggests the potential application of Exendin-P5 in the study of metabolic diseases .
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Cat. No.: HY-106481
CAS No.: 54867-56-0
Purity:  95.16%
Research Areas:  

Inflammation/Immunology

Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide .
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