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Results for "

Desensitization

" in MedChemExpress (MCE) Product Catalog:

59

Inhibitors & Agonists

9

Peptides

1

Inhibitory Antibodies

11

Natural
Products

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-103045
    CMPD101
    4 Publications Verification

    		 ROCK PKC G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure .
    CMPD101
  • HY-W004049
    3-Hydroxybenzoic acid

    		Endogenous Metabolite Hydroxycarboxylic Acid Receptor (HCAR) Neurological Disease Metabolic Disease Inflammation/Immunology
    3-Hydroxybenzoic acid is an orally active endogenous metabolite. 3-Hydroxybenzoic acid is an agonist for GPR81 and GPR109A. 3-Hydroxybenzoic acid acts as stress response desensitizers. 3-Hydroxybenzoic acid can be used for anti-inflammatory and analgesic study .
    3-Hydroxybenzoic acid
  • HY-W001160
    5-Hydroxyindole

    		Endogenous Metabolite Calcium Channel nAChR Neurological Disease Endocrinology Cancer
    5-Hydroxyindole is an orally active hydroxylated indole and tryptophan metabolite. 5-Hydroxyindole activates α7 nicotinic acetylcholine receptors and acts on intestinal L-type calcium channels. 5-Hydroxyindole slows down the desensitization of 5-HT3 receptor-mediated ion currents in cells. 5-Hydroxyindole causes convulsions and loss of consciousness. 5-Hydroxyindole is used in the study of neuroblastoma, schizophrenia, and diseases related to intestinal motility disorders .
    5-Hydroxyindole
  • HY-101165
    Cyclothiazide
    2 Publications Verification

    		 iGluR GABA Receptor Neurological Disease
    Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .
    Cyclothiazide
  • HY-100903
    Norbinaltorphimine dihydrochloride
    Maximum Cited Publications
    7 Publications Verification

    nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride

    		 Opioid Receptor Neurological Disease
    Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain .
    Norbinaltorphimine dihydrochloride
  • HY-117040
    nor-Binaltorphimine
    Maximum Cited Publications
    7 Publications Verification

    Norbinaltorphimine; NorBNI

    		 Opioid Receptor Neurological Disease
    nor-Binaltorphimine (Norbinaltorphimine; NorBNI) is a selective, long-acting competitive antagonist of the κ-opioid receptor. nor-Binaltorphimine blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. nor-Binaltorphimine suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. nor-Binaltorphimine is applicable to research related to neurological disorders such as pain .
    nor-Binaltorphimine
  • HY-12509
    PEPA

    		iGluR Neurological Disease
    PEPA is an AMPA receptor allosteric potentiator. PEPA shows preferential action of PEPA on the flop form of AMPA receptors. PEPA is a more potent suppressor of desensitization of receptors containing GluR3 and GluR4 as opposed to those containing GluR1. PEPA has antianxiety effects .
    PEPA
  • HY-N2071
    Cedrol
    1 Publications Verification

    (+)-Cedrol; α-Cedrol

    		 Environmental Pollutants Cytochrome P450 Apoptosis Fungal Caspase Platelet-activating Factor Receptor (PAFR) Infection Neurological Disease Inflammation/Immunology Cancer
    Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties .
    Cedrol
  • HY-N4323
    14-Deoxyandrographolide
    1 Publications Verification

    		 Calcium Channel Apoptosis Caspase Neurological Disease Metabolic Disease
    14-Deoxyandrographolide is a diterpene with calcium channel blocking activity and acts as a uterine smooth muscle relaxant. 14-Deoxyandrographolide stimulates the release of nitric oxide (NO) in endothelial cells. 14-Deoxyandrographolide gradually desensitizes liver cells to TNF-α mediated apoptosis by inducing the release of TNFRSF1A .
    14-Deoxyandrographolide
  • HY-121027
    Anagyrine

    (-)-Anagyrine; Monolupine; Rhombinine

    		 mAChR nAChR Neurological Disease
    Anagyrine ((-)-Anagyrine) is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine is a potent and effective desensitizer of nAChR, and Anagyrine can directly, without metabolism, desensitize nAChR .
    Anagyrine
  • HY-110023
    Zimelidine dihydrochloride

    		Serotonin Transporter Neurological Disease
    Zimelidine dihydrochloride is an orally active selective serotonin reuptake inhibitor. Zimelidine dihydrochloride competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine dihydrochloride time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine dihydrochloride strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine dihydrochloride exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine dihydrochloride is used for the study of depressive disorders and analgesic tolerance .
    Zimelidine dihydrochloride
  • HY-P1831
    Proadrenomedullin (1-20), human

    ProAM N20, Human; PAMP-20, human

    		 nAChR Sodium Channel Calcium Channel Cardiovascular Disease Neurological Disease
    Proadrenomedullin (1-20), human is a potent hypotensive and catecholamine release–inhibitory peptide released from chromaffin cells. Proadrenomedullin (1-20) inhibits catecholamine secretion in PC12 pheochromocytoma cells (IC50 ≈ 350 nM) by suppressing Na +/Ca 2+ influx and blocking desensitization. Proadrenomedullin (1-20), human specifically acts on nicotinic cholinergic receptors in a non competitive manner. Proadrenomedullin (1-20), human can be used for research on conditions such as hypertension .
    Proadrenomedullin (1-20), human
  • HY-100939
    4-Chlorophenylguanidine hydrochloride

    		Sodium Channel Neurological Disease
    4-Chlorophenylguanidine hydrochloride is an urokinase-type plasminogen activator inhibitor. 4-Chlorophenylguanidine hydrochloride is a potent ASIC3 positive allosteric modulator and reverses the effects of ASIC3 desensitization. 4-Chlorophenylguanidine hydrochloride influences ASIC3 activity through directly activating the channel and increasing proton sensitivity. 4-Chlorophenylguanidine hydrochloride offers a chemical backbone for the design of new ASIC3 ligands to study ASIC3 in vivo .
    4-Chlorophenylguanidine hydrochloride
  • HY-103229
    Cl-HIBO

    		iGluR Neurological Disease
    Cl-HIBO is a highly subtype-selective GluR1/2 agonist (EC50=4.7 and 1.7 μM, respectively). Cl-HIBO is a potent AMPA receptor agonist (IC50=0.22 μM). Cl-HIBO has desensitizing properties .
    Cl-HIBO
  • HY-W004049R
    3-Hydroxybenzoic acid (Standard)

    		Reference Standards Endogenous Metabolite Hydroxycarboxylic Acid Receptor (HCAR) Neurological Disease Metabolic Disease Inflammation/Immunology
    3-Hydroxybenzoic acid (Standard) is the analytical standard of 3-Hydroxybenzoic acid. This product is intended for research and analytical applications. 3-Hydroxybenzoic acid is an orally active endogenous metabolite. 3-Hydroxybenzoic acid is an agonist for GPR81 and GPR109A. 3-Hydroxybenzoic acid acts as stress response desensitizers. 3-Hydroxybenzoic acid can be used for anti-inflammatory and analgesic study.
    3-Hydroxybenzoic acid (Standard)
  • HY-121082
    (-)-Dihydroalprenolol

    L-Dihydroalprenolol

    		 Adrenergic Receptor Endocrinology
    (-)-Dihydroalprenolol (L-Dihydroalprenolol) is a β-adrenergic antagonist that inhibits the activity of β-adrenergic receptors. (-)-Dihydroalprenolol can cause desensitization of approximately 60% of β-adrenergic receptor binding sites. (-)-Dihydroalprenolol has also been shown to reduce the binding capacity of specific β-adrenergic ligands. (-)-Dihydroalprenolol may affect the ability to stimulate membrane-bound adenylate acylase .
    (-)-Dihydroalprenolol
  • HY-W040176
    N-PTyrosine PA ammonium

    N-Palmitoyl-tyrosine phosphoric acid ammonium

    		 LPL Receptor Cardiovascular Disease Neurological Disease Inflammation/Immunology
    N-PTyrosine PA (N-Palmitoyl-tyrosine phosphoric acid) ammonium is a lysophosphatidic acid (LPA) receptor modulator, which exhibits weak inhibitory activity against LPA1 and partial agonist properties towards LPA5. N-PTyrosine PA ammonium inhibits the activation of LPA receptors and downstream responses by competing with agonists for binding sites. N-PTyrosine PA ammonium can induce morphological changes and aggregation, and also inhibit LPA-induced morphological changes through receptor desensitization caused by pre-incubation. N-PTyrosine PA ammonium can be used in the research of related diseases such as atherosclerosis and acute ischemic syndromes (e.g., unstable angina, myocardial infarction, stroke) .
    N-PTyrosine PA ammonium
  • HY-137988
    Palvanil

    		TRP Channel Neurological Disease Inflammation/Immunology
    Palvanil is a Capsaicin (HY-10448) analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects .
    Palvanil
  • HY-B0822S1
    Fipronil-13C6

    		GABA Receptor Cytochrome P450 Inflammation/Immunology
    Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
    Fipronil-13C6
  • HY-119943B
    (R)-PF-06256142

    		Dopamine Receptor Neurological Disease
    (R)-PF-06256142 is the R enantiomer of PF-06256142 with low active. PF-06256142 is a potent and selective orthosteric D1 receptor agonist that can reduce receptor desensitization relative to dopamine and other catechol-containing agonists .
    (R)-PF-06256142
  • HY-N4323R
    14-Deoxyandrographolide (Standard)

    		Reference Standards Calcium Channel Apoptosis Caspase Neurological Disease Metabolic Disease
    14-Deoxyandrographolide (Standard) is the analytical standard of 14-Deoxyandrographolide. 14-Deoxyandrographolide is a diterpene with calcium channel blocking activity and acts as a uterine smooth muscle relaxant. 14-Deoxyandrographolide stimulates the release of nitric oxide (NO) in endothelial cells. 14-Deoxyandrographolide gradually desensitizes liver cells to TNF-α mediated apoptosis by inducing the release of TNFRSF1A .
    14-Deoxyandrographolide (Standard)
  • HY-P11313
    Catestatin (rat)

    Rat chromogranin A367–387

    		 nAChR Akt Cardiovascular Disease
    Catestatin (rat) (Rat chromogranin A367–387) is a potent, reversible, noncompetitive, and noncooperative nicotinic cholinergic antagonist derived from chromogranin A (A367-387). Catestatin (rat) inhibits norepinephrine release in rat PC12 pheochromocytoma cells (IC50 = 1.2 μM), and blocks desensitization of norepinephrine release (IC50 = 0.62 μM). Catestatin (rat) exerts antiadrenergic effects through the endothelial PI3K-AKT-eNOS pathway in rat papillary muscles and isolated cardiomyocytes. Catestatin (rat) maintains mitochondrial membrane potential in I/R cardiomyocytes and increases phosphorylation of AKT at S473, GSK3β at S9, PLB at T17, and eNOS at S1179. Catestatin (rat) reverses desensitization of 22Na + uptake. Catestatin (rat) can be used for the study of nicotinic cholinergic receptor regulation and catecholamine release control mechanisms .
    Catestatin (rat)
  • HY-118835
    Zimelidine

    		Serotonin Transporter Neurological Disease
    Zimelidine is an orally active selective serotonin reuptake inhibitor. Zimelidine competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine is used for the study of depressive disorders and analgesic tolerance .
    Zimelidine
  • HY-118646
    NS-6740

    		nAChR TNF Receptor Neurological Disease Inflammation/Immunology
    NS-6740 is a partial agonist of α7 nicotinic acetylcholine receptor (α7 nAChR) with an IC50 of 3 nM. NS-6740 also acts as a potent modulator of the cholinergic anti-inflammatory pathway. NS-6740 alters the signaling pattern of α7 in an ion channel-independent manner, thereby reducing synaptic function. NS-6740 induces the desensitized state of α7 nAChR. NS-6740 generates robust nAChR-mediated currents. NS-6740 reduces LPS (HY-D1056)-induced TNF-α release from microglia. NS-6740 can be used in the research of neuroinflammation and neuropathic pain .
    NS-6740
  • HY-121027A
    Anagyrine hydrochloride

    (-)-Anagyrine hydrochloride; Monolupine hydrochloride; Rhombinine hydrochloride

    		 mAChR nAChR Neurological Disease
    Anagyrine ((-)-Anagyrine) hydrochloride is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine hydrochloride binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine hydrochloride is a potent and effective desensitizer of nAChR, and Anagyrine hydrochloride can directly, without metabolism, desensitize nAChR .
    Anagyrine hydrochloride
  • HY-124906
    JAMI1001A

    		iGluR Neurological Disease
    JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms .
    JAMI1001A
  • HY-P3785
    PKI(5-22)amide

    		PKA Neurological Disease
    PKI(5-22)amide is the active inhibitory fragment of the inhibitor of the cyclic AMP-dependent protein kinase (PKA). PKI(5-22)amide inhibits PKA activation, but fails to attenuate homologous desensitization of CRF1 receptors .
    PKI(5-22)amide
  • HY-P10594
    Myr-Arf1(2–17)

    		Ras Endocrinology
    Myr-Arf1(2–17) is a sarcosinated peptide that mimics the localization and function of Arf1 protein on the cell membrane. Myr-Arf1(2–17) can be used to study the desensitization mechanism of luteinizing hormone/chorionic gonadotropin receptor (LH/CGR) .
    Myr-Arf1(2–17)
  • HY-101165R
    Cyclothiazide (Standard)

    		Reference Standards iGluR GABA Receptor Neurological Disease
    Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .
    Cyclothiazide (Standard)
  • HY-P5876
    Proadrenomedullin (N-20) (bovine, porcine)

    ProADM N20(bovine, porcine); PAMP-20(bovine, porcine)

    		 nAChR Neurological Disease
    Proadrenomedullin (N-20) (ProADM N20) (bovine, porcine) is a potent and noncompetitive hypotensive and catecholamine release-inhibitory peptide released from chromaffin cells. Proadrenomedullin (N-20) (bovine, porcine) inhibits catecholamine secretion with an IC50 of 350 nM in PC12 pheochromocytoma cells. Proadrenomedullin (N-20) (bovine, porcine) also blocks (EC50≈270 nM) nicotinic cholinergic agonist desensitization of catecholamine release, as well as desensitization of nicotinic signal transduction ( 22Na + uptake) .
    Proadrenomedullin (N-20) (bovine, porcine)
  • HY-173471
    TRPA1 agonist-1

    		TRP Channel Neurological Disease
    TRPA1 agonist-1 (compound 21) is a potent and selective TAAR1 agonist with an EC50 of 25.47 μM. TRPA1 agonist-1 shows effective analgesic properties without irritation in mice .
    TRPA1 agonist-1
  • HY-120946
    VMY-2-95

    		nAChR Neurological Disease
    VMY-2-95 is an oral active and blood-brain barrier (BBB) penetrant α4β2 nicotinic acetylcholine receptor desensitizer. VMY-2-95 can be used for study of depression or addiction .
    VMY-2-95
  • HY-172588
    GABAA receptor modulator-7

    		GABA Receptor Neurological Disease
    GABAA receptor modulator-7 (compound 1m), a spiro-Barbiturate, is a GABAA receptor modulator. GABAA receptor modulator-7 reverses the action of anesthetics without affecting GABA-induced desensitization and can be used for study of antiepileptics and anxiolytics .
    GABAA receptor modulator-7
  • HY-161118
    MB327

    		nAChR Neurological Disease
    MB327 is a bipyridine nonoxime compound that restores neuromuscular function. MB327 restores the activity of nicotinamide acetylcholine receptors (nAChRs) for carbachol desensitization in a typical type II PAM manner. MB327 can neutralize nerve agent poisoning .
    MB327
  • HY-P3041
    Chromostatin (bovine)

    		Calcium Channel Endocrinology
    Chromostatin bovine is a chromogranin A (CGA) derivative peptide, which inhibits postassium or carbamoylcholine induced catecholamine release with an ID50 of 5 nM. Chromostatin bovine reduces calcium flux, enhances the desensitization process of the cholinergic-evoked secretory response and modulates the endocrine response associated with catecholamine .
    Chromostatin (bovine)
  • HY-P2307
    Tat-NR2Baa

    		iGluR NO Synthase Neurological Disease
    Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .
    Tat-NR2Baa
  • HY-P2307A
    Tat-NR2Baa TFA

    		iGluR NO Synthase Neurological Disease
    Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .
    Tat-NR2Baa TFA
  • HY-130176
    UFP-512

    		Opioid Receptor ERK Adenylate Cyclase Neurological Disease
    UFP-512 is a selective and potent σ-opioid receptor (DOP receptor) peptidic agonist with antidepressant- and anxiolytic-like effects. UFP-512 exhibits as a potent agonist on adenylyl cyclase inhibition and Erk1/2 activation. UFP-512 induces phosphorylation of DOP receptors on Ser 363 with a low desensitization of the cAMP pathway. UFP-512 is promising for research of mood disorders .
    UFP-512
  • HY-N2071R
    Cedrol (Standard)

    (+)-Cedrol (Standard); α-Cedrol (Standard)

    		 Reference Standards Cytochrome P450 Fungal Apoptosis Caspase Infection Neurological Disease Inflammation/Immunology Cancer
    Cedrol (Standard) is the analytical standard of Cedrol. This product is intended for research and analytical applications. Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties.
    Cedrol (Standard)
  • HY-110023R
    Zimelidine dihydrochloride (Standard)

    		Reference Standards Serotonin Transporter Neurological Disease
    Zimelidine dihydrochloride (Standard) is the analytical standard of Zimelidine dihydrochloride (HY-110023). This product is intended for research and analytical applications. Zimelidine dihydrochloride is an orally active selective serotonin reuptake inhibitor. Zimelidine dihydrochloride competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine dihydrochloride time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine dihydrochloride strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine dihydrochloride exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine dihydrochloride is used for the study of depressive disorders and analgesic tolerance .
    Zimelidine dihydrochloride (Standard)
  • HY-118835S
    Zimeldine-d6

    		Isotope-Labeled Compounds Serotonin Transporter Neurological Disease
    Zimeldine-d6 is the deuterium labeled Zimeldine (HY-118835) . Zimelidine is an orally active selective serotonin reuptake inhibitor. Zimelidine competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine is used for the study of depressive disorders and analgesic tolerance .
    Zimeldine-d6
  • HY-W001160R
    5-Hydroxyindole (Standard)

    		Reference Standards Endogenous Metabolite nAChR Calcium Channel Neurological Disease Endocrinology Cancer
    5-Hydroxyindole (Standard) is the analytical standard of 5-Hydroxyindole (HY-W001160). This product is intended for research and analytical applications. 5-Hydroxyindole is an orally active hydroxylated indole and tryptophan metabolite. 5-Hydroxyindole activates α7 nicotinic acetylcholine receptors and acts on intestinal L-type calcium channels. 5-Hydroxyindole slows down the desensitization of 5-HT3 receptor-mediated ion currents in cells. 5-Hydroxyindole causes convulsions and loss of consciousness. 5-Hydroxyindole is used in the study of neuroblastoma, schizophrenia, and diseases related to intestinal motility disorders .
    5-Hydroxyindole (Standard)
  • HY-P11275
    TC4

    		GLP Receptor GCGR Neuropeptide Y Receptor Metabolic Disease
    TC4 is a highly balanced single-molecule quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC50 values of 0.95, 31, 81, and 1100 nM respectively. TC4 exhibits extremely strong signal bias on GLP-1R and has very low recruitment efficacy for β-inhibitor protein 2 (βArr2) and this strong cAMP preference is believed to maximize metabolic benefits (such as weight loss and hypoglycemia) while possibly minimizing side effects mediated by β-inhibitor protein recruitment (such as receptor desensitization). TC4 can be used for research on obesity and diabetes .
    TC4
  • HY-178144
    FPR2 agonist 5

    		Formyl Peptide Receptor (FPR) Calcium Channel Interleukin Related NO Synthase Neurological Disease Inflammation/Immunology
    FPR2 agonist 5 is a selective Formyl Peptide Receptor 2 (FPR2) agonist. FPR2 agonist 5 induces Ca 2+ mobilization in FPR2-HL60 transfected cells with an EC50 of 1.2 μM and causes FPR2 desensitization with an IC50 of 0.32 μM. FPR2 agonist 5 exerts neuroprotective effects by mitigating LDH release, NO production, IL-1β, IL-6, IL-33, and IL-10 levels in LPS (HY-D1056)-induced mouse primary microglial cells. FPR2 agonist 5 can be used for the study of neuroinflammatory-related diseases .
    FPR2 agonist 5
  • HY-121143
    Bis-Q

    		Cholinesterase (ChE) Neurological Disease
    Bis-Q is an acetylcholine (ACh) agonist that targets voltage-clamped muscle fibers of the fish Xenomystus nigris. Bis-Q exists in two forms: cis-Bis-Q (non-agonist) and trans-Bis-Q (agonist). Photoisomerization converts cis-Bis-Q to trans-Bis-Q, which induces agonist-induced currents. Channels activated by trans-Bis-Q and ACh have similar conductances and open times. Flashes increase the ratio of trans-Bis-Q to cis-Bis-Q until light equilibrium is reached. Further flashes transiently increase agonist-induced currents, indicating binding of trans-Bis-Q to desensitized receptors. Higher concentrations of cis-Bis-Q produce larger agonist-induced currents that decay exponentially. .
    Bis-Q
  • HY-150057
    CB1R Allosteric modulator 4

    		Cannabinoid Receptor Others
    CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .
    CB1R Allosteric modulator 4
  • HY-103045R
    CMPD101 (Standard)

    		ROCK PKC G Protein-coupled Receptor Kinase (GRK) Reference Standards Cardiovascular Disease
    CMPD101 (Standard) is the analytical standard of CMPD101 (HY-103045). This product is intended for research and analytical applications. CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure .
    CMPD101 (Standard)
  • HY-W070739
    GABAA receptor modulator-12

    		GABA Receptor Neurological Disease
    GABAA receptor modulator-12 (Compound 5) is a GABAA receptor modulator. GABAA receptor modulator-12 inhibits anesthetic-induced desensitization of GABAA α3β3γ2 receptors with an IC50 of 0.2 μM. GABAA receptor modulator-12 can be used in the research of central nervous system disorders .
    GABAA receptor modulator-12
  • HY-P992154
    Ricefidase

    KJ-103

    		 Human leukocyte immunoglobulin (Ig)-like receptors (LILR) Infection Inflammation/Immunology
    Ricefidase (KJ-103) is a recombinant human immunoglobulin G-degrading enzyme. Ricefidase efficiently cleaves human IgG at the hinge region. Ricefidase rapidly reduces IgG levels. Ricefidase has low immunogenicity and clears AAV neutralizing antibodies. Ricefidase is applicable to research related to desensitization of all IgG subclasses and improvement of the suitability of AAV-based gene therapy .
    Ricefidase
  • HY-165475
    TDPAM02

    		iGluR Neurological Disease
    TDPAM02 is a positive allosteric modulator of AMPA receptor GluA2. TDPAM02 can specifically bind to the ligand-binding domain (LBD) of GluA2 and shows an IC50 of 1.4 nM for the GluA2 flop subtype. TDPAM02 can stabilize the activated conformation of GluA2 receptors, delay the receptor deactivation or desensitization process, maintaining the rapid excitatory synaptic transmission in the central nervous system .
    TDPAM02

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