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Results for "

Inverse Agonists

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (19) Adenosine Receptor (3) Adrenergic Receptor (2) Angiotensin Receptor (1) Apoptosis (7) Autophagy (1) Cannabinoid Receptor (19) CMV (1) Complement System (1) CXCR (2) Dengue virus (2) Dopamine Receptor (5) Drug Metabolite (1) EBI2/GPR183 (1) Endogenous Metabolite (1) ERK (1) Estrogen Receptor/ERR (8) Flavivirus (2) Free Fatty Acid Receptor (3) FXR (1) GABA Receptor (15) GHSR (8) GPR6 (1) GPR84 (2) Histamine Receptor (32) Interleukin Related (2) Isotope-Labeled Compounds (7) LXR (6) Mas-related G-protein-coupled Receptor (MRGPR) (1) Melanocortin Receptor (2) Melatonin Receptor (1) mGluR (1) Nuclear Hormone Receptor 4A/NR4A (1) Parasite (1) PPAR (9) RAR/RXR (1) Reactive Oxygen Species (2) REV-ERB (1) ROR (41) TSH Receptor (1)
By Research Areas:	Cancer (37) Cardiovascular Disease (6) Endocrinology (21) Infection (9) Inflammation/Immunology (57) Metabolic Disease (22) Neurological Disease (75)
Click Chemistry:	Azide (3)

186

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-160039

GAC0001E5	LXR	Cancer
GAC0001E5 is an LXR inverse agonist. GAC0001E5 has antiproliferative activity and can be used in cancer research .

HY-137434

Cedirogant ABBV-157	ROR	Inflammation/Immunology
Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research .

HY-122737

*RORγt Inverse* agonist 8**	ROR	Inflammation/Immunology
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC₅₀ of 19 nM for human RORγt-LBD .

HY-118336

VUF10497	Histamine Receptor	Inflammation/Immunology
VUF10497 is a potent histamine H4 receptor (H4R) inverse agonist with anti-inflammatory activity .

HY-124225

RU 33965	GABA Receptor	Neurological Disease
RU 33965 is an orally active benzodiazepine receptor weak partial inverse agonist .

HY-160161

BAY-5094	PPAR	Cancer
BAY-5094 is a PPAR gamma (PPARG) inverse agonist. BAY-5094 has oral activity. BAY-5094 can be used in the research of luminal bladder cancer .

HY-168179

*RORγt inverse* agonist 32**	ROR	Inflammation/Immunology
RORγt inverse agonist 32 (compound b14) is orally active. RORγt inverse agonist 32 can be used in inflammation research .

HY-135280

MRL-650 CB1 Inverse agonist 1	Cannabinoid Receptor	Metabolic Disease
MRL-650 (CB1 inverse agonist 1) is a highly potent, orally active, and specific inverse agonist of CB1 receptor with IC₅₀s of 7.5 nM and 4100 nM for CB1 and CB2 receptors, respectively. Anorexigenic effects .

HY-143271

*RORγt inverse* agonist 29**	ROR	Inflammation/Immunology
RORγt inverse agonist 29 is a potent, orally active and selective RORγt inverse agonist (IC₅₀: 21 nM). RORγt inverse agonist 29 can be used in the research of skin inflammation and autoimmune diseases like psoriasis .

HY-119010

UCM 549	Melatonin Receptor	Neurological Disease
UCM 549 is a melatonin MT2 receptor inverse agonist and a MT1 receptor antagonist .

HY-147533

*RORγt inverse* agonist 30**	ROR	Inflammation/Immunology
RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist with the IC₅₀ of 46 nM. Targeting the nuclear receptor RORγt is effective in autoimmune disorders .

HY-137061

AZ-GHS-22	GHSR	Metabolic Disease
AZ-GHS-22 is a potent, non-CNS penetrant GHS-R1a inverse agonist (IC₅₀=0.77 nM) .

HY-111273

AR244555	Mas-related G-protein-coupled Receptor (MRGPR)	Cardiovascular Disease
AR244555 is a malate-aspartate shuttle (MAS) inverse agonist with IC₅₀s of 186 nM and 348 nM in human and rat inositol phosphatase (IP) Gq coupling assays respectively. AR244555 has cardioprotective effects .

HY-116247

ST247	PPAR	Metabolic Disease Inflammation/Immunology
ST247 a potent PPARβ/δ inverse agonist. ST247 has a higher affinity to PPARβ/δ. ST247 modulates expression of the activation marker CCL2 in the opposite direction. ST247 efficiently induces the interaction with corepressors. ST247 inhibits the agonist-induced transcriptional activity of PPARβ/δ .

HY-144699

ERRα antagonist-2	Estrogen Receptor/ERR	Cancer
ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC₅₀ of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo .

HY-100369A

DMCM hydrochloride	GABA Receptor	Neurological Disease
DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with K_is of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 ?receptors, respectively .

HY-101198

Clobenpropit dihydrobromide	Histamine Receptor Apoptosis	Neurological Disease Cancer
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC₅₀ of 8.07 for histamine H3LR . Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (K_i 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (K_i 7.4 nM) and α2A/α2C adrenoceptors (K_i 17.4/7.8 nM) . Clobenpropit dihydrobromide increases apoptosis .

HY-100991

FG 7142 ZK 39106; LSU-65	GABA Receptor	Neurological Disease
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (K_i=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC₅₀= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex .

HY-116603

SB-236057	5-HT Receptor	Others
SB-236057 is an inverse agonist of the 5-HT_1B receptor that exhibits strong skeletal teratogenicity in rodents and rabbits. SB-236057 affects gene expression during embryonic development through interference with the Notch signaling pathway and interaction with r-esp1. SB-236057 induces somatic patterning and tail extension defects in rat embryos during early organogenesis .

HY-103476

Ro15-4513	GABA Receptor	Neurological Disease
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-49076

*RORγ inverse* agonist 1**	ROR	Cancer
RORγ inverse agonist 1 is the inverse agonist of RORγ .

HY-132909

*Nurr1 inverse* agonist-1**	Nuclear Hormone Receptor 4A/NR4A	Inflammation/Immunology Cancer
Nurr1 inverse agonist-1 is an inverse agonist tool for the neuroprotective transcription factor Nurr1.

HY-149833

*ERRγ inverse* agonist 2**	Estrogen Receptor/ERR	Infection Metabolic Disease
ERRγ inverse agonist 2 (compound 19) is a potent and selective ERRγ inverse agonist with a K_d value of 6.5 μM. ERRγ inverse agonist 2 inhibits the expression of hepcidin, fibrinogen and gluconeogenic genes. ERRγ inverse agonist 2 has antimicrobial, anti-coagulant and antidiabetic activities .

HY-156354

*GPR61 Inverse* agonist 1**	Others	Metabolic Disease
GPR61 Inverse agonist 1 (Compound 1) is a GPR61 inverse agonist (IC₅₀: 11 nM). GPR61 Inverse agonist 1 can be used for research of disorders of metabolism and body weight, such as obesity and cachexia .

HY-111748

*RORγt Inverse* agonist 2**	ROR	Inflammation/Immunology
RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC₅₀ of 119 nM .

HY-12095

*CB1 inverse* agonist 2**	Cannabinoid Receptor	Neurological Disease
CB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model .

HY-132195

*RORγt inverse* agonist 14**	ROR	Inflammation/Immunology
RORγt inverse agonist 14 (8e) is a potent, orally active and selective RORγt inverse agonist (EC₅₀ of 2.5 nM) with anti-inflammatory activity. RORγt inverse agonist 14 is used in the study for rheumatoid arthritis and psoriasis .

HY-139847

*RORγt inverse* agonist 23**	ROR	Inflammation/Immunology
RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist.

HY-142806

*RORγt inverse* agonist 26**	ROR	Inflammation/Immunology
RORγt inverse agonist 26 is a potent reverse agonist of RORγt. RORγt inverse agonist 26 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 26 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 1) .

HY-142703

*RORγt inverse* agonist 28**	ROR	Inflammation/Immunology
RORγt inverse agonist 28 is a potent reverse agonist of RORγt. RORγt inverse agonist 28 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 28 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 6) .

HY-130243

*RORγt Inverse* agonist 6**	ROR	Inflammation/Immunology
RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo .

HY-114411

*ERRγ inverse* agonist 1**	Estrogen Receptor/ERR	Cancer
ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective and orally bioavailable Estrogen-related Receptor grammar (ERRγ) inverse agonist, with an IC₅₀ of 40 nM .

HY-155548

*RORγt inverse* agonist 31**	ROR	Inflammation/Immunology
RORγt inverse agonist 31 (14g) is a potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist, with an IC₅₀ of 0.428 μM. RORγt inverse agonist 31 can alleviate the severity of Imiquimod (HY-B0180)-induced psoriasis in mice .

HY-10559

Nelotanserin 2 Publications Verification APD125	5-HT Receptor	Neurological Disease Cancer
Nelotanserin is a potent 5-HT_2A inverse agonist, a moderately potent 5-HT_2C partial inverse agonist and a weak 5-HT_2B inverse agonist, with IC₅₀s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

HY-131338

*RORγt inverse* agonist 13**	ROR	Inflammation/Immunology
RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved agent-like properties, with an IC₅₀ of 63.8 nM .

HY-116521

SR2595	PPAR	Metabolic Disease
SR2595 is an inverse agonist of PPARγ with an IC₅₀ of 30 nM .

HY-128573

*RORγt Inverse* agonist 3**	ROR	Neurological Disease
RORγt Inverse agonist 3 is a potent, selective and orally active RORγ inverse agonist, with EC₅₀s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively .

HY-B0188

Mianserin Mianserine	Histamine Receptor	Neurological Disease Endocrinology
Mianserin is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.

HY-12664

AF64394	Others	Others
AF64394 is a GPR3 inverse agonist, with a pIC₅₀ of 7.3.

HY-119208

VUF11211	CXCR	Others
VUF11211 is an allosteric inverse CXCR3 agonist with a K_d of 0.65 nM .

HY-16972

SR9243 5 Publications Verification	LXR	Cancer
SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.

HY-102075A

TMP778	ROR	Inflammation/Immunology
TMP778 is a potent and selevtive RORγt inverse agonist, with an IC₅₀ of 7 nM in FRET assay.

HY-115777

ARN-6039	ROR	Neurological Disease
ARN-6039 is an orally available inverse agonist of RORγ for autoimmune demyelinating disease.

HY-169001

*5-HT2A/5-HT2C inverse* agonist 1**	5-HT Receptor	Neurological Disease
5-HT2A/5-HT2C inverse agonist 1 is a potent and dual 5-HT2A and 5-HT2C receptor inverse agonist with a hERG inhibitions, thus avoiding cardiovascular risks. 5-HT2A/5-HT2C inverse agonist 1 shows significant antipsychotic efficacy in the MK-801 (HY-15084B)-induced mouse model. 5-HT2A/5-HT2C inverse agonist 1 is promising for research of psychosis .

HY-B0188A

Mianserin hydrochloride Org GB 94	Histamine Receptor	Neurological Disease Endocrinology
Mianserin hydrochloride (Org GB 94) is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.

HY-13421

SR1001 5 Publications Verification	REV-ERB ROR	Inflammation/Immunology
SR1001 is a selective ROR_α and ROR_γt inverse agonist with K_is 172 and 111 nM, respectively.

HY-148237

JNJ-54119936	Others	Others
JNJ-54119936 is a novel RORC inverse agonist (K_d=5.3 nM) .

HY-16998

SR2211	ROR	Inflammation/Immunology
SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a K_i of 105 nM and an IC₅₀ of ~320 nM.

HY-148352

BAY-4931	PPAR	Cancer
BAY-4931 is a potent, covalent and selective PPARγ inverse-agonist with an IC₅₀ of 0.17 nM .

HY-14413

SR3335 10+ Cited Publications ML 176	ROR	Metabolic Disease
SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a K_i of 220 nM .

Cat. No.	Product Name	Target	Research Area

HY-P1091

Hemopressin (human, mouse)	Cannabinoid Receptor	Neurological Disease
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .

HY-P3561A

Agouti-related Protein (AGRP) (83-132) Amide (human) (TFA)	Melanocortin Receptor	Neurological Disease
Agouti-related Protein (AGRP) (83-132) Amide (human) TFA is a fragment of agouti-related protein (AGRP) which is a protein found in abundance in the arcuate nucleus of the hypothalamus. AgRP primarily acts as an inverse agonist for the melanocortin-4 receptor (MC4R) to increase food intake .

HY-P1090

Hemopressin(rat)	Cannabinoid Receptor	Neurological Disease
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .

HY-W140282

Angiotensin II antipeptide	Angiotensin Receptor	Cardiovascular Disease
Angiotensin II antipeptide, a peptide, is an inverse agonist of AR1 receptor. Angiotensin II antipeptide is encoded by mRNA, complementary to that encoding Angiotensin II (HY-13948) itself .

HY-P10673

KwFwLL-NH2	GHSR	Metabolic Disease
KwFwLL-NH2, a hexapeptide, is a ghrelin receptor ligand. KwFwLL-NH2 can act as a specific inverse agonist at the ghrelin receptor but with moderate potency (EC₅₀=45.6 nM) .

HY-P3561

Agouti-related Protein (AGRP) (83-132) Amide (human)	Melanocortin Receptor	Neurological Disease
Agouti-related Protein (AGRP) (83-132) Amide (human) is a fragment of agouti-related protein (AGRP) which is a protein found in abundance in the arcuate nucleus of the hypothalamus. AgRP primarily acts as an inverse agonist for the melanocortin-4 receptor (MC4R) to increase food intake .

HY-P1091A

Hemopressin(human, mouse) TFA	Cannabinoid Receptor	Neurological Disease
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .

HY-P1432

K-(D-1-Nal)-FwLL-NH2	GHSR	Metabolic Disease
K-(D-1-Nal)-FwLL-NH2 is a high affinity, potent and inverse ghrelin receptor agonist (EC₅₀=3.4 nM, K_i=4.9 nM). K-(D-1-Nal)-FwLL-NH2 can be used for the research of obesity .

HY-P1090A

Hemopressin(rat) TFA	Cannabinoid Receptor	Neurological Disease
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .

HY-P1432A

K-(D-1-Nal)-FwLL-NH2 TFA	GHSR	Cancer
K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (K_i values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B0188A

Mianserin hydrochloride Org GB 94	Alkaloids Structural Classification Neurological Disease Classification of Application Fields Leguminosae Other Alkaloids Source classification Crotalaria pallida Ait. Plants Disease Research Fields Endocrinology	Histamine Receptor
Mianserin hydrochloride (Org GB 94) is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.

HY-152851

Izumerogant IMU-935	Classification of Application Fields Disease Research Fields Cancer	ROR
Izumerogant (IMU-935) is an inverse agonist of retinoid-related orphan receptor-gamma (RORγ). Izumerogant (compound 123) also potently inhibits IL-17A, IL-17F and IFN-γ activity with IC₅₀s <50 nM .

HY-124717

YC-001	Structural Classification Natural Products Classification of Application Fields Source classification Other Diseases Endogenous metabolite Disease Research Fields	Endogenous Metabolite
YC-001 is an inverse agonist and antagonist of rod opsin. YC-001 reversibly binds rod opsin and stabilizes the rod opsin structure. YC-001 protects mice from bright light-induced retinal degeneration. YC-001 has the potential for the research of retinal degeneration .

HY-N0049

Nuciferine 4 Publications Verification	Structural Classification Alkaloids Aporphine Alkaloids other families Source classification Plants Isoquinoline Alkaloids	Parasite 5-HT Receptor Dopamine Receptor
Nuciferine is an antagonist at 5-HT_2A (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-B0188AR

Mianserin hydrochloride (Standard)	Alkaloids Structural Classification Leguminosae Other Alkaloids Source classification Crotalaria pallida Ait. Plants	Histamine Receptor
Mianserin (hydrochloride) (Standard) is the analytical standard of Mianserin (hydrochloride). This product is intended for research and analytical applications. Mianserin hydrochloride (Org GB 94) is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.

HY-N0049R

Nuciferine (Standard)	Structural Classification Alkaloids other families Source classification Plants	5-HT Receptor Dopamine Receptor
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at 5-HT_2A (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

Cat. No.	Product Name	Chemical Structure

HY-17043S1

Loratadine-d5
Loratadine-d₅ is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.

HY-14289S

Cimetidine-d3
Cimetidine-d₃ is the deuterium labeled Cimetidine. Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity[1][2][5].

HY-B0188AS

Mianserin-d3 hydrochloride
Mianserin-d₃ (hydrochloride) is the deuterium labeled Mianserin hydrochloride. Mianserin hydrochloride (Org GB 94) is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.

HY-B0188S

Mianserin-d3
Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin? is a Histamine 1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant .

HY-B0349S

Meclizine-d8
Meclizine-d₈ is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR[1][2][3].

HY-12199BS

Pitolisant-d5 hydrochloride
Pitolisant-d5 hydrochloride (Ciproxidine-d5 hydrochloride) is the deuterium labeled Pitolisant hydrochloride (HY-12199B). Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (K_i=0.16 nM) .

HY-17043S

Loratadine-d4
Loratadine-d₄ is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.

HY-135392S

N-Desmethyl Pimavanserin-d9 hydrochloride
N-Desmethyl Pimavanserin-d9 hydrochloride (AC-279-d9 hydrochloride) is the deuterium labeled N-Desmethyl Pimavanserin (HY-135392). N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively .

HY-32329S

Setiptiline-d3

Setiptiline-d₃ is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine[1][2].

Cat. No.	Product Name		Classification

HY-103476

Ro15-4513		Azide
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-155481A

CB2 receptor antagonist 4		Azide
CB2 receptor antagonist 4 (compound (R)-1) is a CB2R-selective inverse agonist with a K_d value of 39 nM .

HY-155481

CB2 receptor antagonist 3		Azide
CB2 receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptor CB2R with Kd=39 nM. CB2 receptor antagonist 3 can be used as a tool to synthesize a variety of CB2R probes .

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