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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
479 Results for "
Inverse
" in MedChemExpress (MCE) Product Catalog:
Products (479)
479 Results for "Inverse" in MCE Product Catalog:
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SB 206553 is a 5-HT2C inverse agonist. SB 206553 can attenuate methamphetamine-seeking in rats. SB 206553 has activity for 5-HT2 receptor ligands in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors with pKi values of 5.6 nM (5-HT2A), 7.7 nM (5-HT2B) and 7.8 nM (5-HT2C), respectively. SB 206553 can be used for the research of psychostimulant abuse disorders .
Cat. No.: HY-U00425
CAS No.: 1264754-13-3
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PROTAC ERRα ligand 1 is a PROTAC target protein ligand. PROTAC ERRα ligand 1 is an orally active ERRα inverse agonist with IC50 values of 0.6 μM for ERRα. PROTAC ERRα ligand 1 shows no significant activity against a panel of other nuclear receptors, including ERα c, ERRγ, ERβ, PPARα, PPARγ, PPARδ, and RXRα. PROTAC ERRα ligand 1 can provide enhanced insulin sensitivity in vivo. PROTAC ERRα ligand 1 can be used for metabolic diseases research, such as type 2 diabetes and obesity .
Cat. No.: HY-151769
CAS No.: 2353409-48-8
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TCO-PEG2-Sulfo-NHS ester-EDC Urea is a click chemistry reagent containing an azide group. TCO-PEG2-Sulfo-NHS ester is a PEG linker containing a TCO moiety and a sulfo-NHS ester moiety. The sulfo group makes this molecule soluble in waqueous buffer. This reagent can be used to label antibodies, proteins and other primary amine-containing macromolecules with TCO moiety. Reagent grade, for research use only . TCO-PEG2-Sulfo-NHS ester-EDC Urea is a click chemistry reagent, it contains a TCO group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing Tetrazine groups.
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JTE-907 is a selective and orally active cannabinoid CB2 receptor inverse agonist and exerts anti-inflammatory effects. JTE-907 upregulates IL-6, MCP-1, IL-1β, VEGF, ANGPTL4, and TRPV1 in mature adipocytes. JTE-907 downregulates CB1, MCP-1, and IL-1β in preadipocytes. JTE-907 inhibits ear swelling in mice. JTE-907 reverses the protective effects of CB2 agonists and Anandamide (HY-10863) against cytokine-evoked colonic mucosal damage. JTE-907 can be used for the research of allergic dermatitis, obesity, and colitis .
Synonyms: JF646, Tetrazine
Cat. No.: HY-179724
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PZ-1657 (Compound 57) is an orally active, blood-brain barrier permeable, highly selective, and metabolically stable 5-HT7 receptor inverse agonist with a Ki value of 5 nM. PZ-1657 inhibits constitutive cyclic adenosine monophosphate (cAMP) production mediated by the Gs signaling pathway (EC50 value of 2.93 nM). PZ-1657 inhibits CYP3A4 P450 (IC50 = 12.2 μM) and hERG channels. PZ-1657 reduces 5-HT7 receptor-mediated MMP-9 activity. PZ-1657 reverses Phencyclidine-induced cognitive impairment. PZ-1657 possesses antidepressant properties .
Cat. No.: HY-179724A
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PZ-1657 hydrochloride (Compound 57) is a potent, selective and orally active 5-HT7 receptor inverse agonist with a Ki of 5 nM. PZ-1657 hydrochloride can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC50 = 2.93 nM). PZ-1657 hydrochloride can significantly reduce the MMP-9 activity mediated by 5-HT7 receptors in the hippocampus of mice, and the effect is comparable to that of SB-269970 (HY-15370). PZ-1657 hydrochloride can reverse the cognitive deficits observed in the rat novel object recognition test induced by Phencyclidine without affecting the animals' spontaneous activities. PZ-1657 hydrochloride can be used for the research of emotional disorders, such as depression and bipolar disorder .
Cat. No.: HY-143712R
CAS No.: 2276-94-0
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Cat. No.: HY-113440R
CAS No.: 712-09-4
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Cat. No.: HY-121837
CAS No.: 2088234-50-6
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β2AR-IN-15 is a selective β2-adrenergic receptor (β2AR) antagonist with a Kd of 1.7 μM. β2AR-IN-15 binds to an intracellular β2AR region overlapping the G-protein binding site, enhancing orthosteric inverse agonist binding while negatively modulating binding of orthosteric agonists with EC50 values of 1.9 and 0.48 μM. β2AR-IN-15 shows inhibitory effect on cAMP production and β-arrestin recruitment to activated β2AR. β2AR-IN-15 can be used for the research of cardiovascular and pulmonary diseases .
Cat. No.: HY-W008820R
CAS No.: 110-94-1
Cat. No.: HY-143712S1
Synonyms: 3α-hydoxy-5α-Cholaoic Acid-d4, allo-LCA-d4
Cat. No.: HY-W048513
CAS No.: 60129-59-1
Cat. No.: HY-103117
CAS No.: 847871-78-7
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S 32212 hydrochloride is an inverse agonist of 5-HT receptors 5-HT2(CINI) and 5-HT2(CVSV) (Kis=6.6, 8.9 nM) and an antagonist of 5-HT2A and α2β-adrenergic receptors (Ki=5.8, 5.8 nM). S 32212 hydrochloride can reduce the binding of GTPγS to Gαq, and reduce the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2(CINI) receptor and CHO cells expressing 5-HT2(CVSV) receptor (EC50=38 and 18.6 nM, respectively). S 32212 hydrochloride (2.5 mg/kg) reduces 5-HT receptor agonist-induced head twitches and penile erections in mice and rats. S 32212 hydrochloride (10, 40 mg/kg) reduces immobility time in the forced swim test and marble burying behavior in mice and rats, exerting antidepressant and anxiolytic activities.
Cat. No.: HY-155887
CAS No.: 474922-26-4
Synonyms: DSPE-PEG-NH2, MW 3400 ammonium
DSPE-PEG-Amine (DSPE-PEG-NH2), MW 3400 ammonium is an amino-functionalized PEGylated phospholipid. It serves not only as a key component for preparing σ receptor-targeted liposomes (such as anisamide-modified lipids) but also as a starting material for synthesizing click chemistry- and tumor-targeted lipids including DSPE-PEG-DBCO (HY-155788) and DSPE-PEG2000-TCO (HY-170704). DSPE-PEG-Amine, MW 3400 ammonium effectively modulates the ζ potential of nanoparticles, enables complexation with nucleic acids or proteins to protect DNA from nuclease degradation, and supports ligand conjugation on the nanoparticle surface. It is used in studies related to DU-145 tumors, breast cancer, and other relevant research .
Cat. No.: HY-134483
CAS No.: 851375-22-9
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5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active, brain-penetrant 5-HT7 and 5-HT2A receptor ligand having a pKi = 8.1 at both receptors. 5-HT7/5-HT2A receptor antagonist 1 behaves as an antagonist in an in vitro functional assay for 5-HT2A and as an inverse agonist in an in vitro functional assay for 5-HT7. 5-HT7/5-HT2A receptor antagonist 1 blockade of 5-Carboxamidotryptamine (5-CT) (HY-135555) induced hypothermia in rats, and blockade of 2,5-dimethoxy-4-iodoamphetamine (DOI) induced head-twitches in mice. 5-HT7/5-HT2A receptor antagonist 1 occupied 5-HT2A receptor binding sites in the frontal cortex of the rat brain. 5-HT7/5-HT2A receptor antagonist 1 can be used for the study of Neurological diseases .
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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
