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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
35 Results for "
biased signaling
" in MedChemExpress (MCE) Product Catalog:
Products (35)
35 Results for "biased signaling" in MCE Product Catalog:
3
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3 Cited Publications
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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 Cited Publications
Cat. No.: HY-P2141A
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1 Cited Publications
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MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=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) .
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1 Cited Publications
Cat. No.: HY-16642A
CAS No.: 1231220-79-3
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LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
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1 Cited Publications
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KNT-127 is a selective and BBB-penetrant δ-opioid receptor (DOR) agonist (Ki = 0.16 nM). KNT-127 is highly selective to the δ receptor, with Ki values of 0.16, 21.3 and 153 nM for δ, μ and κ receptors, respectively. KNT-127 acts as a biased ligand that mainly activates cyclic adenosine monophosphate (cAMP) signaling with lower beta-arrestin signaling activation. KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 exhibits antidepressant- and anxiolytic-like effects. KNT-127 can be studied in research on neurological diseases .
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1 Cited Publications
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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 .
Cat. No.: HY-164899
CAS No.: 2765091-45-8
Synonyms: 2-aminopyridine-3-carboxylic acid imidazolide
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2A3 (2-aminopyridine-3-carboxylic acid imidazolide) is a covalent probe reagent for Selective 2'-Hydroxyl Acylation analyzed by Primer Extension (SHAPE) that targets the RNA ribose 2'-OH group. 2A3 efficiently permeates the biological membranes of Gram-negative bacteria, Gram-positive bacteria, and mammalian cells. 2A3 exhibits no base bias and specifically labels conformationally flexible, unpaired regions within RNA.
2A3 forms covalent adducts by acylating the 2'-OH groups of flexible RNA residues. When combined with SHAPE-MaP (mutational profiling) sequencing technology, these modification sites are converted into detectable mutational signals, thereby accurately reflecting local RNA backbone flexibility and base-pairing status. 2A3 is primarily utilized in molecular biology and transcriptomics research, including the resolution of RNA structuromes in living cells, the study of RNA folding regulatory mechanisms, and the investigation of non-coding RNA functions .
Cat. No.: HY-P3137
CAS No.: 812644-79-4
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Cat. No.: HY-171978
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LM-189 is a β2-adrenergic receptor (β2AR) ligand and G protein-biased modulator with a human β2AR Ki of 0.063 nM.LM-189 promotes β2AR coupling to Gαs and Gαi heterotrimers, stabilizes distinct β2AR conformations including a TM6 outward state, and increases β2AR ICL2 dynamics.LM-189 restricts β2AR ligand-binding pocket conformational heterogeneity, stabilizes polar ligand-receptor interaction networks, and exhibits bias toward Gαi signaling over Gαs signaling.LM-189 enabled cryo-EM structural characterization of the β2AR-Gi complex.LM-189 can be used for the research of congestive heart failure .
Cat. No.: HY-16639
CAS No.: 1448895-09-7
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ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC50 = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions .
Cat. No.: HY-P3136
CAS No.: 25849-90-5
Synonyms: TRV120055
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GS39783 is a positive allosteric modulator (PAM) of GABABR. Positive modulation of the GABABR can be used for the research of Nicotine addiction .
Cat. No.: HY-P3136A
Synonyms: TRV120055 hydrochloride
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Cat. No.: HY-163671
CAS No.: 2767348-36-5
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PW0729 is a selective GPR52 agonist. PW0729 activates G protein/cAMP signaling pathway, with bias toward this pathway over β-arrestin recruitment, and induces GPR52 desensitization. PW0729 can be used for the research of neuropsychiatric and neurological diseases .
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HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi 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 .
Cat. No.: HY-110302
CAS No.: 2410327-94-3
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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 .
Cat. No.: HY-P11235
CAS No.: 3028974-74-2
Synonyms: PF-08653944; MET-097
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Cat. No.: HY-P11540
CAS No.: 2923120-30-1
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Cat. No.: HY-P11237
CAS No.: 2869147-44-2
Synonyms: CT-388
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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
