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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
94 Results for "
agonist potency
" in MedChemExpress (MCE) Product Catalog:
Products (94)
94 Results for "agonist potency" in MCE Product Catalog:
8
8 Publications Verification
Synonyms: ACT-128800
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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 .
6
6 Cited Publications
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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 .
4
4 Cited Publications
Synonyms: LY3502970; GLP-1 receptor agonist 1; OWL-833
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Cardiovascular Disease Metabolic Disease Inflammation/Immunology
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 .
4
4 Cited Publications
Synonyms: LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate; OWL-833 hemicalcium hydrate
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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 .
3
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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 .
3
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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 Cited Publications
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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 Cited Publications
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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 .
1
1 Cited Publications
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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 .
1
1 Cited Publications
Synonyms: (±)-Carazolol; DL-Carazolol; Suacron
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Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist .
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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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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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NS 9283 (A-969933) is a α4β2 nicotinic acetylcholine receptor (α4β2 nAChR) positive allosteric modulator that preferentially targets the (α4)3 (β2)2 stoichiometric conformation. NS 9283 increases the potency of ACh-induced currents without enhancing the maximal effect of ACh. NS 9283 also enhances prefrontal glutamate release, modulates attention-related electrophysiological responses, and potentiates the antinociceptive effects associated with α4β2 nAChR agonists. NS 9283 can be used in research related to inflammatory pain, postoperative pain, osteoarthritis pain, and Parkinson's disease .
Cat. No.: HY-110168R
CAS No.: 913830-15-6
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NS 9283 (Standard) is the analytical standard of NS 9283 (HY-110168). This product is intended for research and analytical applications. NS 9283 (A-969933) is a α4β2 nicotinic acetylcholine receptor (α4β2 nAChR) positive allosteric modulator that preferentially targets the (α4)3 (β2)2 stoichiometric conformation. NS 9283 increases the potency of ACh-induced currents without enhancing the maximal effect of ACh. NS 9283 also enhances prefrontal glutamate release, modulates attention-related electrophysiological responses, and potentiates the antinociceptive effects associated with α4β2 nAChR agonists. NS 9283 can be used in research related to inflammatory pain, postoperative pain, osteoarthritis pain, and Parkinson's disease .
Cat. No.: HY-W270810
CAS No.: 360778-55-8
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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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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) .
Cat. No.: HY-P2249
CAS No.: 2245073-05-4
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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 .
Cat. No.: HY-P11320
CAS No.: 863919-85-1
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Cat. No.: HY-P10716
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
