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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC48389 CCR2 antagonist 5 CCR2 antagonist 5 is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). CCR2 antagonist 5 displays a Ki of 9.6 µM for mCCR2 binding. CCR2 antagonist 5 can be used in the research of inflammatory disease.
DC48395 ACT-1004-1239 Featured ACT-1004-1239 is a potent, selective, orally available CXCR7 antagonist with an IC50 value of 3.2 nM.
DC48396 CXCR2 antagonist 2 CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy with an IC50 value of 95 nM.
DC48397 AZD4721 AZD4721 (RIST4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). AZD4721 has the potential for the research of inflammatory disease.
DC48404 Ghrelin receptor full agonist-2 Ghrelin receptor full agonist-2 is a highly potent Ghrelin receptor full agonist.
DC48420 Orexin B, rat, mouse TFA Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexin receptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptors OX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation.
DC48460 L-Glutamine-13C5,15N2 L-Glutamine-13C5,15N2 (L-Glutamic acid 5-amide-13C5,15N2) is the 13C- and 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells.
DC48531 Clorprenaline Clorprenaline is a potent agonist of β2-adrenergic. Clorprenaline promotes animal muscular mass growth and decreases fat accumulation. Clorprenaline is a potential new lean meat-boosting feed additive.
DC48591 Octamylamine Octamylamine is an anticholinergic and antispasmodic agent.
DC48606 UCSF686 UCSF686 is a probe with which to study the function of the 5-HT5AR. UCSF686 loses affinity at 5-HT5AR (>10 000 nM) but not at 5-HT1AR, 5-HT2BR, and 5-HT7R. UCSF686 controls for off-target effects.
DC48611 (R)-Preclamol (R)-Preclamol is a dopamine (DA) agonist with autoreceptor as well as postsynaptic receptor stimulatory properties. (R)-Preclamol inhibits the locomotor activity of mice and rats in low doses.
DC48638 UCSF678 UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT5AR with a more restricted off-target profile and decreased assay liabilities. UCSF678 is a selective probe with which to study the function of the 5-HT5AR.
DC48644 Zacopride hydrochloride Featured Zacopride hydrochloride is a potent antagonist of 5-HT3 receptor with a Ki of 0.38 nM. Zacopride hydrochloride is also a agonist of 5-HT4 receptor with a Ki of 373 nM. Zacopride hydrochloride has anxiolytic activity. Zacopride hydrochloride has the potential for the research of Schizophrenia.
DC48645 5-HT2A receptor agonist-1 5-HT2A receptor agonist-1 shows the agonist activity at the 5-HT2A receptor with an EC50 of 5.54 nM.
DC48667 Tegaserod Tegaserod is a serotonin receptor 4 agonist (HTR4) used in the treatment of irritable bowel syndrome (IBS). Anti-tumor activity.
DC48688 CXCR2 antagonist 3 CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3+ T lymphocytes into the Pan02 tumor tissues.
DC48689 Ro 01-6128 Ro 01-6128 is a positive allosteric modulator of mGluR1.
DC48691 Dioxopromethazine Dioxopromethazine is an orally active antihistamine. Dioxopromethazine inhibits asthmatic symptoms.
DC48710 Ridogrel Ridogrel (R 68070) is an orally active combined thromboxane A2 synthetase inhibitor and thromboxane A2/prostaglandin endoperoxide receptor blocker. Ridogrel is potent antiplatelet agent. Anti-inflammatory activities.
DC48719 Neldazosin Neldazosin is a potent alpha1-adrenoceptor antagonist.
DC48760 Lu AA33810 Lu AA33810 is a potent and selective antagonist of neuropeptide Y5 receptor with a Ki of 1.5 nM for the human receptor. Lu AA33810 exhibts antianxiolytic-like and antidepressant-like effects.
DC48787 LE 300 LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay.
DC48823 SB-328437 Featured SB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC50 of 4.5 nM.
DC48831 GPBAR1-IN-3 GPBAR1-IN-3 (Compound 14) is a selective GPBAR1 agonist (EC50=0.17 μM) and a CysLT1R antagonist.
DC48869 Sequifenadine Sequifenadine is a H1-antihistamine. Sequifenadine has the potential for the research of inflammatory eye disease with allergic symptoms.
DC48870 Prifinium bromide Prifinium bromide is antimuscarinic agent with antispasmodic, antiemetic effect.
DC48907 S-777469 S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism.
DC48913 CM398 Featured CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice.
DC48918 (S)-Butaprost free acid (S)-Butaprost (free acid) is a potent and highly selective agonist of EP2 receptor.
DC48919 Noladin ether Noladin ether is a potent and selective agonist of cannabinoid CB1 receptor, with a Ki of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception.

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