587 Results for "

Partial agonists

" in MedChemExpress (MCE) Product Catalog:
Products (587)

587 Results for "Partial agonists" in MCE Product Catalog:

4
4 Cited Publications
Cat. No.: HY-A0007
CAS No.: 125572-93-2
Synonyms: N-0923 Hydrochloride
Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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4
4 Cited Publications
Cat. No.: HY-12023
CAS No.: 401900-40-1
Purity:  99.61%
Synonyms: S-4
Target:  

Androgen Receptor

Research Areas:  

Cancer

GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity .
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4
4 Cited Publications
Cat. No.: HY-75502
CAS No.: 99755-59-6
Synonyms: N-0923; (-)-N 0437
Rotigotine is a potent dopamine receptor agonist with Ki values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research .
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4 Cited Publications
Cat. No.: HY-N2025
CAS No.: 57396-78-8
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
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3
3 Cited Publications
Cat. No.: HY-P2625
CAS No.: 275801-62-2
Target:  

GCGR

Research Areas:  

Metabolic Disease

GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM) .
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3
3 Cited Publications
Cat. No.: HY-119486
CAS No.: 1643489-24-0
Purity:  99.94%
Synonyms: PF-06649751; CVL-751
Target:  

Dopamine Receptor

Research Areas:  

Neurological Disease

Tavapadon (PF-06649751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist. Tavapadon is effective in enabling movement and reducing disability and has the potential for Parkinson's disease .
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3
3 Cited Publications
Cat. No.: HY-117829
CAS No.: 1354030-51-5
Purity:  98.06%
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 Gi-regulated cAMP production. Antipsychotic Activity .
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3
3 Cited Publications
Cat. No.: HY-14558
CAS No.: 87760-53-0
Purity:  99.41%
Synonyms: SM-3997
Target:  

5-HT Receptor

Research Areas:  

Neurological Disease

Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms .
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3 Cited Publications
Cat. No.: HY-B0061
CAS No.: 112457-95-1
Synonyms: SM-3997 citrate
Target:  

5-HT Receptor

Tandospirone (SM-3997) citrate is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone citrate has anxiolytic and antidepressant activities. Tandospirone citrate can be used for the research of the central nervous system disorders and the underlying mechanisms .
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3
3 Cited Publications
Cat. No.: HY-P0227
CAS No.: 168482-23-3
Target:  

Melanocortin Receptor

Research Areas:  

Metabolic Disease

SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.
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3
3 Cited Publications
Cat. No.: HY-111385
CAS No.: 2108826-33-9
Purity:  98.83%
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 Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity .
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3
3 Cited Publications
Cat. No.: HY-N1951
CAS No.: 27210-57-7
Synonyms: Rosmariquinone
Miltirone is an orally active natural compound found in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC50 of 0.3 μM. Miltirone induces ROS - and-p53 dependent apoptosis. Miltirone inhibits carboxylesterase 2 (CES2; Ki = 0.04 μM) and SARS-CoV main protease (Mpro) .
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3 Cited Publications
Cat. No.: HY-100554
CAS No.: 21102-95-4
Purity:  99.92%
Research Areas:  

Cardiovascular Disease

BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist .
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2
2 Cited Publications
Cat. No.: HY-N0175
CAS No.: 485-35-8
Synonyms: Cytisine; Sophorine; Baptitoxine
Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .
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2
2 Cited Publications
Cat. No.: HY-17622
CAS No.: 263251-78-1
Synonyms: MIM-D3
Target:  

Trk Receptor

Research Areas:  

Inflammation/Immunology

Tavilermide is a selective, partial agonist of TrkA, or a nerve growth factor (NGF) mimetic.
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2
2 Cited Publications
Cat. No.: HY-101384A
CAS No.: 189744-94-3
Purity:  99.86%
Target:  

Dopamine Receptor

Research Areas:  

Others

Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
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2 Cited Publications
Cat. No.: HY-10559
CAS No.: 839713-36-9
Purity:  99.52%
Synonyms: APD125
Target:  

5-HT Receptor

Research Areas:  

Neurological Disease Cancer

Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
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2 Cited Publications
Cat. No.: HY-103524
CAS No.: 3569-10-6
Purity:  ≥99.0%
Synonyms: (-)-Valerenic Acid
Research Areas:  

Neurological Disease

Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .
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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 Cited Publications
Cat. No.: HY-A0087
CAS No.: 6197-30-4
Octocrylene is an organic ultraviolet (UV) filter that absorbs mainly UVB radiation and shorter UVA wavelengths. Octocrylene acts as a partial agonist of PPARγ, which alters the gene transcription profile of lipid metabolism enzymes. In addition, Octocrylene is cytotoxic and genotoxic to human skin fibroblasts and mediates the biosynthesis of estrogens such as estriol in zebrafish larvae, while affecting antioxidant pathways including glutathione transferase and peroxisomes .
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