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Results for "

Inverse Agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (34) Adenosine Receptor (4) Adrenergic Receptor (6) Angiotensin Receptor (1) ANGPTL (1) Antibiotic (1) Apoptosis (10) Arrestin (2) Autophagy (2) Bacterial (1) Bcl-2 Family (1) Cannabinoid Receptor (26) Caspase (1) CDK (1) CMV (1) Complement System (1) CXCR (2) Cytochrome P450 (3) Dengue Virus (4) Dopamine Receptor (7) Drug Derivative (2) Drug Isomer (1) Drug Metabolite (4) EBI2/GPR183 (3) Endogenous Metabolite (4) ERK (2) Estrogen Receptor/ERR (10) Ferroptosis (1) Flavivirus (4) Free Fatty Acid Receptor (5) FXR (2) G protein-coupled Bile Acid Receptor 1 (3) GABA Receptor (24) GHSR (10) Glutathione Peroxidase (1) GPR6 (3) GPR84 (4) Histamine Receptor (42) Interleukin Related (5) Isotope-Labeled Compounds (12) Ligands for Target Protein for PROTAC (2) LXR (10) Mas-related G-protein-coupled Receptor (MRGPR) (1) Melanocortin Receptor (2) Melatonin Receptor (1) mGluR (1) MMP (2) mTOR (1) Nuclear Hormone Receptor 4A/NR4A (3) Orphan GPCR (4) Orphan Nuclear Receptor (1) Parasite (1) Phosphodiesterase (PDE) (1) Potassium Channel (1) PPAR (10) Pregnane X Receptor (PXR) (1) RAR/RXR (2) Reactive Oxygen Species (ROS) (3) Reference Standards (30) REV-ERB (3) ROR (55) Transferrin Receptor (1) TRP Channel (1) TSH Receptor (1) VEGFR (1)
By Research Areas:	Cancer (48) Cardiovascular Disease (12) Endocrinology (26) Infection (12) Inflammation/Immunology (82) Metabolic Disease (43) Neurological Disease (111)
Click Chemistry:	Azide (3)

267

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14557

Pimavanserin 10+ Cited Publications ACP-103	5-HT Receptor	Neurological Disease
Pimavanserin is a selective, brain-penetrant, inverse agonist of the 5-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

HY-13421

SR1001 5+ Cited Publications	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-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 .

HY-12584

PF-5190457 PF-05190457	GHSR	Metabolic Disease Endocrinology
PF-5190457 (PF-05190457) is a potent and selective ghrelin receptor inverse agonist with a pK_i of 8.36 .

HY-12199

Pitolisant 2 Publications Verification Tiprolisant	Histamine Receptor	Neurological Disease Endocrinology
Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (K_i=0.16 nM).

HY-12199B

Pitolisant hydrochloride 2 Publications Verification Ciproxidine; BF 2649	Histamine Receptor	Neurological Disease Endocrinology
Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (K_i=0.16 nM).

HY-16972

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

HY-16998

SR2211 1 Publications Verification	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-14426

L-655708 4 Publications Verification	GABA Receptor	Neurological Disease
L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (K_i=0.45 nM).

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-12664

AF64394 1 Publications Verification	Orphan GPCR	Others
AF64394 is a GPR3 inverse agonist, with a pIC₅₀ of 7.3.

HY-10013

Taranabant 2 Publications Verification MK-0364	Cannabinoid Receptor	Metabolic Disease
Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding K_i of 0.13 nM for the human CB1R in vitro.

HY-101192

GSK682753A 3 Publications Verification	EBI2/GPR183	Inflammation/Immunology
GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC₅₀ of 53.6 nM.

HY-101442

SR9238 2 Publications Verification	LXR	Metabolic Disease
SR9238 is a synthetic liver X receptor (LXR) inverse agonist with IC₅₀s of 214 nM and 43 nM for LXRα and LXRβ, respectively.

HY-153344

FX-909 1 Publications Verification	PPAR	Cancer
FX-909 is a covalent peroxisome proliferator-activated receptor gamma (PPARG) inverse agonist. FX-909 can be used for the research of cancer .

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-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-156354

*GPR61 Inverse* agonist 1**	Orphan GPCR	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-116622

α5IA L-822179	GABA Receptor	Neurological Disease
α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential .

HY-147400

Sipagladenant KW-6356	Adenosine Receptor	Neurological Disease
Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist . Sipagladenant can be used in frontal lobe dysfunction research .

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-114411

*ERRγ inverse* agonist 1**	Estrogen Receptor/ERR	Cancer
ERRγ inverse agonist 1 (Compound 12) is a selective ERRγ inverse agonist with an IC₅₀ value of 0.040 μM against ERRγ. ERRγ inverse agonist 1 inhibits the activity of ERRγ at the functional level. ERRγ inverse agonist 1 can be used in the research of anaplastic thyroid cancer .

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-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-102075A

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

HY-148352

BAY-4931 1 Publications Verification	PPAR	Cancer
BAY-4931 is a potent, covalent and selective PPARγ inverse-agonist with an IC₅₀ of 0.17 nM .

HY-101232

Tiotidine 2 Publications Verification ICI 125211	Histamine Receptor	Cardiovascular Disease
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA₂=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors .

HY-160039

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

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-131338

*RORγt inverse* agonist 13** 1 Publications Verification	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-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-175306

*GPR183 inverse* agonist-1**	EBI2/GPR183 Arrestin	Inflammation/Immunology Cancer
GPR183 inverse agonist-1 (Compound 78) is a GPR183 inverse agonist. GPR183 inverse agonist-1 inhibits the GPR183-mediated Gi activation and β-arrestin2 recruitment, and blocks PBMC migration. GPR183 inverse agonist-1 can be used for inflammatory, autoimmune and neoplastic disorders research .

HY-175822

*5-HT2A inverse* agonist-1**	5-HT Receptor	Neurological Disease
5-HT2A inverse agonist-1 is a 5-HT_2A receptor inverse agonist with a IC₅₀ of 5.5 nM. 5-HT2A inverse agonist-1 shows minimal hERG inhibition. 5-HT2A inverse agonist-1 can be used for the research of neurological disease, such as Parkinson’s disease .

HY-150308

SR10221	PPAR	Cancer
SR10221, a noncovalent inverse agonist of PPARγ, represses downstream PPARγ target genes leading to growth inhibition in bladder cancer cell lines .

HY-175490

*RORγ inverse* agonist 2**	ROR	Inflammation/Immunology
RORγ inverse agonist 2 (Compound 15) is a potent inverse agonist of the retinoic acid receptor-related orphan receptor RORγ, with IC₅₀ values of 0.4 and 0.9 μM for Gal4-RORγ and full-length RORγ, respectively. RORγ inverse agonist 2 is useful in the study of autoimmune diseases .

HY-177712

*RORγt inverse* agonist 36**	ROR	Inflammation/Immunology
RORγt inverse agonist 36 (S configuration of Compound 16) is a RORγt inverse agonist. RORγt inverse agonist 36 can be used for the research of inflammation and immunology .

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-128604

XY101	ROR	Cancer
XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC₅₀ of 30 nM and a K_d of 380 nM .

HY-12199A

Pitolisant oxalate Tiprolisant oxalate	Histamine Receptor	Neurological Disease Endocrinology
Pitolisant oxalate is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (K_i=0.16 nM).

HY-160160

BAY-5516	PPAR	Cancer
BAY-5516 is a inverse-agonist o PPARG, with the IC₅₀ value of 6.1±3.6 nM that has anti-tumor effect .

HY-143259

BE1218	LXR	Cancer
BE1218 is a liver X receptor (LXR) inverse agonist with IC₅₀ values of 9 nM and 7 nM against LXRα and LXRβ, respectively .

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-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-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-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-135280

MRL-650 CB1 Inverse Agonist 1	Cannabinoid Receptor	Metabolic Disease
MRL-650 (CB1 inverse agonist 1), a chemical probe, 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-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-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 .

Cat. No.	Product Name	Target	Research Area

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-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-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-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-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-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-N0049

Nuciferine 5+ Cited Publications	Alkaloids Aporphine Alkaloids other families Plants Isoquinoline Alkaloids Source Classification	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-143712

Allolithocholic acid 1 Publications Verification	Structural Classification Classification of Application Fields Metabolic Disease Endogenous metabolite Disease Research Fields Steroids Source Classification	Drug Metabolite G protein-coupled Bile Acid Receptor 1 ROR
Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC₅₀ = 2.7 μM) and RORγt inverse agonist (IC₅₀ = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .

HY-116711

11-cis-Retinal 11-cis Retinaldehyde; 11-cis Vitamin A aldehyde	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Other Diseases Endogenous metabolite Disease Research Fields Source Classification	Drug Derivative Endogenous Metabolite
11-cis-Retinal (11-cis Retinaldehyde; 11-cis Vitamin A aldehyde), oxidized form of 11-cis-Retinol (HY-W587807), is a naturally occurring visual component. 11-cis-Retinal binds to opsin in the mammalian visual system as an inverse agonist forming the inactive conformation of rhodopsin. 11-cis-Retinal plays a crucial role in vision, growth and development. 11-cis-Retinal can restore visual function in moths with visual impairments. 11-cis-Retinal can restore retinal function in an early-age LCA2 retinal degeneration 12 mouse model .

HY-124717

YC-001	Natural Products Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Source Classification	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-N0049R

Nuciferine (Standard)	Alkaloids other families Plants Source Classification	Reference Standards 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.

HY-143712R

Allolithocholic acid (Standard)	Structural Classification Endogenous metabolite Steroids Source Classification	Reference Standards Drug Metabolite G protein-coupled Bile Acid Receptor 1 ROR
Allolithocholic acid (Standard) is the analytical standard of Allolithocholic acid (HY-143712). This product is intended for research and analytical applications. Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC₅₀ = 2.7 μM) and RORγt inverse agonist (IC₅₀ = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .

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-14546S

Aripiprazole-d8

Aripiprazole-d₈ (OPC-14597-d₈) is the deuterium labeled Aripiprazole (HY-14546). Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.

HY-143712S1

Allolithocholic Acid-d4

Allolithocholic Acid-d₄ (3α-hydoxy-5α-Cholaoic Acid-d₄, allo-LCA-d₄) is deuterium labeled Allolithocholic acid (HY-143712). Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC₅₀ = 2.7 μM) and RORγt inverse agonist (IC₅₀ = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .

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 K_i of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity .

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 .

HY-12199S1

Pitolisant-d6
Pitolisant-d₆ (Tiprolisant-d₆) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (K_i=0.16 nM).

HY-12199S

Pitolisant-d10
Pitolisant-d₁₀ (Tiprolisant-d₁₀) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (K_i=0.16 nM) .

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-23188

Loratadine-d5-1
Loratadine-d₅-1 is a deuterated labeled Loratadine (HY-17043). 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-17043S2

Loratadine-d4-1
Loratadine-d₄-1 (Loratidine-d₄-1) is 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-17043S3

Loratadine-13C6
Loratadine- ¹³C₆ (SCH 29851- ¹³C₆) is ¹³C 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 .

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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