Reverse agonist

By Targets:	5-HT Receptor (1) ADC Cytotoxin (2) Adenosine Receptor (1) Apoptosis (2) Cannabinoid Receptor (2) Dopamine Receptor (1) Estrogen Receptor/ERR (2) Glucocorticoid Receptor (3) LXR (2) Melanocortin Receptor (3) nAChR (1) Protease Activated Receptor (PAR) (2) ROR (2) Sigma Receptor (1) Trk Receptor (1)
By Research Areas:	Cancer (6) Endocrinology (2) Inflammation/Immunology (10) Metabolic Disease (1) Neurological Disease (8)
Click Chemistry:	Azide (1)

Targets Recommended: Reverse Transcriptase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-155481

CB2 receptor antagonist 3	Cannabinoid Receptor	Neurological Disease
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 .

HY-154928

GW6340

LXR Metabolic Disease

GW6340 is an intestinal-specific LXR agonist. GW6340 promotes macrophage reverse cholesterol transport (mRCT) .

GW6340	LXR	Metabolic Disease
GW6340 is an intestinal-specific LXR agonist. GW6340 promotes macrophage reverse cholesterol transport (mRCT) .

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-123985

MFN2 agonist-1	Others	Others
MFN2 agonist-1 (B-A/l) potently stimulates mitochondrial fusion in mitofusin 2 (MFN2)-deficient cells. MFN2 agonist-1 reverses mitochondrial “clumping” (formation of static mitochondrial aggregates) and restores mitochondrial motility in cultured mouse neurons expressing the CMT2A mutant MFN2 T105M.

HY-101230

ICI 174864
ICI 174864 is a highly selective, potent δ-receptor antagonist. ICI 174864 is equipotent with naloxone and can not reverse the effect of the μ-agonist [D-Ala2, MePhe4, Gly-Ol5]enkephalin or the κ-agonist-tifluadom .

HY-153189

TrkB-IN-1	Trk Receptor	Neurological Disease
TrkB-IN-1 is a potent and orally active TrkB agonist and has favorable PK properties. TrkB-IN-1 reverses the cognitive defects in an AD mouse model and can be used for alzheimer’s disease research .

HY-118461

PD 120697	Dopamine Receptor	Neurological Disease
PD 120697 is an orally active dopamine (DA) agonist. PD 120697 inhibits striatal DA synthesis, DA neuronal firing, spontaneous locomotor activity, and reverses Reserpine (HY-N0480)-induced depression .

HY-13580

Budesonide 3 Publications Verification	Glucocorticoid Receptor ADC Cytotoxin	Inflammation/Immunology Cancer
Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma .

HY-P1310

VKGILS-NH2 1 Publications Verification	Protease Activated Receptor (PAR)	Inflammation/Immunology
VKGILS-NH2 is a reversed amino acid sequence control peptide for SLIGKV-NH2 (protease-activated receptor 2 (PAR2) agonist). VKGILS-NH2 has no effect on DNA synthesis in cells .

HY-149853

AD186	Sigma Receptor	Neurological Disease
AD186 is a potent and selective S1R agonist with K_is of 2.7, 27 nM for S1R and S2R, respectively. AD186 fully reverses the antiallodynic effect of BD-1063 (HY-18101A) .

HY-P1310A

VKGILS-NH2 TFA	Protease Activated Receptor (PAR)	Inflammation/Immunology
VKGILS-NH2 TFA is a reversed amino acid sequence control peptide for SLIGKV-NH2 (protease-activated receptor 2 (PAR2) agonist). VKGILS-NH2 TFA has no effect on DNA synthesis in cells .

HY-103454B

MPP hydrochloride Maximum Cited Publications 7 Publications Verification	Estrogen Receptor/ERR Apoptosis	Endocrinology Cancer
MPP hydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP hydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP hydrochloride reverses the the positive effects of beta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo .

HY-103454

MPP dihydrochloride Maximum Cited Publications 7 Publications Verification	Estrogen Receptor/ERR Apoptosis	Endocrinology Cancer
MPP dihydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP dihydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP dihydrochloride reverses the positive effects of beta-estradiol. MPP dihydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo .

HY-13580S

Budesonide-d8	Glucocorticoid Receptor	Inflammation/Immunology Cancer
Budesonide-d₈ is the deuterium labeled Budesonide. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma[1][2][3].

HY-147707

CB2 receptor antagonist 1	Cannabinoid Receptor	Others
Hexyl resorcinol derivative 29 has been proved to be a CB2 selective competitive antagonist / reverse agonist with good potency. Olivanol and 5- (2-methyloctane-2-yl) resorcinol derivatives 23 and 24 showed significant antinociceptive activity. Compound 24 was shown to activate cannabinoid and TRPV1 receptors.

HY-13580R

Budesonide (Standard) 3 Publications Verification	Glucocorticoid Receptor ADC Cytotoxin	Inflammation/Immunology Cancer
Budesonide (Standard) is the analytical standard of Budesonide. This product is intended for research and analytical applications. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma .

HY-P1208

PG-931	Melanocortin Receptor	Inflammation/Immunology
PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC₅₀=0.58 nM) agonist and is more selective than for the hMC3R (IC₅₀=55 nM) or the hMC5R (IC₅₀=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo .

HY-P1726A

MSG606 TFA	Melanocortin Receptor
MSG606 TFA is a potent human MC1 receptor antagonist (IC₅₀=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC₅₀ values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.

HY-P1208A

PG-931 TFA	Melanocortin Receptor	Inflammation/Immunology
PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC₅₀=0.58 nM) agonist and is more selective than for the hMC3R (IC₅₀=55 nM) or the hMC5R(IC₅₀=2.4 nM). PG-931 TFA can reverse haemorrhagic shock and prevent multiple organ damage in vivo .

HY-123148

IMB-808	LXR	Inflammation/Immunology
IMB-808 is a potent LXRα/β dual agonist with EC₅₀ values of 0.53 μM and 0.15 μM (0.15 μM, using GAL4-pGL4-luc reporter plasmid) for LXRβ and LXRα, respectively. IMB-808 promotes expression of genes related to reverse cholesterol transport (ABCA1 and ABCG1). IMB-808 can be used as a promising agent for the prospective treatment of atherosclerosis research .

HY-109139

Taminadenant 1 Publications Verification NIR178; PBF509	Adenosine Receptor	Neurological Disease Cancer
Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A_2A receptor (A_2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with K_B values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response .

HY-14565

Pozanicline ABT-089	nAChR	Neurological Disease
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (K_i=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (K_i, rat) for Pozanicline to [ ³H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction .

HY-110291

A-971432	Others	Neurological Disease
A-971432 is a potent, selective and orally active sphingosine-1-phosphate (S1P) receptor 5 agonist with IC₅₀s of .362, >10, 0.006 µM for S1P1, S1P3, S1P5 respectively. A-971432 protects blood–brain barrier (BBB) homeostasis. A-971432 reverses age-related cognitive decline. A-971432 has the potential for the research of alzheimer’s disease or multiple sclerosis .

HY-103142

AS19	5-HT Receptor	Neurological Disease
AS19 is a potent, selective 5-HT₇ receptor agonist with an IC₅₀ value of 0.83 nM and a K_i of 0.6 nM. AS19 is selective for 5-HT₇ over 5-HT_1A, 5-HT_1B, 5-HT_1D, and 5-HT_5A receptors (K_is = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia .

Cat. No.	Product Name

HY-L070

Neuroprotective Compound Library	1058 compounds
Neurodegenerative diseases are characterised by progressive dysfunction and death of neurons, such as Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis (MS). Neuroprotection is an approach to preserve neurons so that neurons cannot be hurt by different pathological factors in neurodegenerative diseases. Neuroprotectors are some agonists and antagonists targeting some key targets in neuroprotactive signal pathways, such as calcium and sodium channel blockers, GABA receptor agonists, NMDA receptor Antagonists, etc. Current neuroprotectors cannot reverse existing damage, but they may protect against further nerve damage and slow down any degeneration of the central nervous system (CNS) and still play important roles in the treatment of neurodegenerative diseases. MCE offers a unique collection of 1058 compounds with potential neuroprotective activities. These compounds mainly act on some key targets in neuroprotetive signal pathways, such as calcium channel, sodium channel, adenosine A1 receptor, etc. MCE Neuroprotective Compopund Library is a useful tool in neuroprotective drug discovery.

Neuroprotective Compound Library

1058 compounds

Neurodegenerative diseases are characterised by progressive dysfunction and death of neurons, such as Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis (MS). Neuroprotection is an approach to preserve neurons so that neurons cannot be hurt by different pathological factors in neurodegenerative diseases. Neuroprotectors are some agonists and antagonists targeting some key targets in neuroprotactive signal pathways, such as calcium and sodium channel blockers, GABA receptor agonists, NMDA receptor Antagonists, etc. Current neuroprotectors cannot reverse existing damage, but they may protect against further nerve damage and slow down any degeneration of the central nervous system (CNS) and still play important roles in the treatment of neurodegenerative diseases.

MCE offers a unique collection of 1058 compounds with potential neuroprotective activities. These compounds mainly act on some key targets in neuroprotetive signal pathways, such as calcium channel, sodium channel, adenosine A1 receptor, etc. MCE Neuroprotective Compopund Library is a useful tool in neuroprotective drug discovery.

Cat. No.	Product Name	Target	Research Area

HY-P1310

VKGILS-NH2 1 Publications Verification	Protease Activated Receptor (PAR)	Inflammation/Immunology
VKGILS-NH2 is a reversed amino acid sequence control peptide for SLIGKV-NH2 (protease-activated receptor 2 (PAR2) agonist). VKGILS-NH2 has no effect on DNA synthesis in cells .

HY-P1208

PG-931	Melanocortin Receptor	Inflammation/Immunology
PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC₅₀=0.58 nM) agonist and is more selective than for the hMC3R (IC₅₀=55 nM) or the hMC5R (IC₅₀=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo .

HY-P1310A

VKGILS-NH2 TFA	Protease Activated Receptor (PAR)	Inflammation/Immunology
VKGILS-NH2 TFA is a reversed amino acid sequence control peptide for SLIGKV-NH2 (protease-activated receptor 2 (PAR2) agonist). VKGILS-NH2 TFA has no effect on DNA synthesis in cells .

HY-P1726A

MSG606 TFA	Melanocortin Receptor
MSG606 TFA is a potent human MC1 receptor antagonist (IC₅₀=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC₅₀ values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.

HY-P1208A

PG-931 TFA	Melanocortin Receptor	Inflammation/Immunology
PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC₅₀=0.58 nM) agonist and is more selective than for the hMC3R (IC₅₀=55 nM) or the hMC5R(IC₅₀=2.4 nM). PG-931 TFA can reverse haemorrhagic shock and prevent multiple organ damage in vivo .

Cat. No.	Product Name	Chemical Structure

HY-13580S

Budesonide-d8
Budesonide-d₈ is the deuterium labeled Budesonide. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma[1][2][3].

Cat. No.	Product Name		Classification

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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Inhibitors & Agonists

Screening Libraries

Peptides

Isotope-Labeled Compounds

Click Chemistry