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Results for "

Effective antagonists

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (13) Adrenergic Receptor (11) Akt (1) Androgen Receptor (3) Angiotensin Receptor (2) Antibiotic (5) Apoptosis (16) Aryl Hydrocarbon Receptor (1) Autophagy (1) Bacterial (5) Bradykinin Receptor (1) Calcium Channel (5) Cannabinoid Receptor (2) Casein Kinase (1) CCR (1) CFTR (5) CGRP Receptor (1) Cholecystokinin Receptor (2) Cholinesterase (ChE) (3) COX (3) Cytochrome P450 (2) Dopamine Receptor (10) EGFR (1) Endogenous Metabolite (2) Environmental Pollutants (1) Estrogen Receptor/ERR (3) FXR (1) GCGR (2) Glycoprotein VI (1) GnRH Receptor (7) Histamine Receptor (12) IAP (1) IFNAR (1) iGluR (1) IKK (1) Integrin (1) Interleukin Related (1) Isotope-Labeled Compounds (11) Leukotriene Receptor (5) LPL Receptor (1) mAChR (2) MCHR1 (GPR24) (3) mGluR (2) mTOR (1) nAChR (6) Neurokinin Receptor (7) Neuropeptide Y Receptor (1) NF-κB (2) NO Synthase (3) Nuclear Factor of activated T Cells (NFAT) (6) Opioid Receptor (3) P-glycoprotein (2) PI3K (1) Potassium Channel (2) PPAR (2) Progesterone Receptor (1) Protease Activated Receptor (PAR) (1) RAR/RXR (4) Reference Standards (17) Ser/Thr Protease (1) Sodium Channel (2) STING (1) TSH Receptor (1) Vasopressin Receptor (1) VD/VDR (1) Wnt (1)
By Research Areas:	Cancer (29) Cardiovascular Disease (17) Endocrinology (21) Infection (6) Inflammation/Immunology (24) Metabolic Disease (23) Neurological Disease (40)
Click Chemistry:	Tetrazine (1) Alkynes (4)

126

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

GMP Molecules

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-U00449

AGN 193109 5+ Cited Publications	RAR/RXR	Cancer
AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with K_ds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively. AGN 193109 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. AGN 193109 is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity.

HY-12870

AZD9496 Maximum Cited Publications 28 Publications Verification	Estrogen Receptor/ERR	Cancer
AZD9496 is an effective, selective estrogen receptor (ERα) antagonist with an IC₅₀ of 0.28 nM. AZD9496 is an orally active, selective estrogen receptor degrader (SERD).

HY-106301

Devazepide 5+ Cited Publications L-364,718; MK-329	Cholecystokinin Receptor	Metabolic Disease
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC₅₀s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .

HY-B0349

Meclizine dihydrochloride 4 Publications Verification Meclozine dihydrochloride	Histamine Receptor Apoptosis	Neurological Disease Endocrinology Cancer
Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .

HY-14369

Elagolix sodium NBI-56418 sodium	GnRH Receptor Nuclear Factor of activated T Cells (NFAT)	Metabolic Disease Cancer
Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K_D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

HY-N0925

Tetrahydroberberine 2 Publications Verification Canadine	Dopamine Receptor	Neurological Disease
Tetrahydroberberine is a different kind of living thing that can be extended and divided into parts. Tetrahydroberberine is a kind of effective D2 receptor antagonistic force. Tetrahydroberberine has the ability to strengthen the stomach and relieve the pressure on the stomach .

HY-14789

(R)-Elagolix NBI-56418	GnRH Receptor Nuclear Factor of activated T Cells (NFAT)	Endocrinology Cancer
Elagolix is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K_D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

HY-107601

UBP316 ACET	iGluR	Neurological Disease
UBP316 (ACET) is a highly potent and selective kainate receptor GluK1 (GluR5) antagonist, with a K_b value of 1.4 nM. UBP316 is effective at blocking the depression of both field excitatory postsynaptic potentials (fEPSPs) and monosynaptically-evoked GABAergic transmission induced by ATPA, a GluK1 selective agonist .

HY-B1161A

S-Methoprene 2 Publications Verification (+)-Methoprene; (7S)-Methoprene	Environmental Pollutants Cannabinoid Receptor	Others
S-Methoprene is an insect juvenile hormone analog and effective insecticide that blocks the transition from pupa to adult. S-Methoprene is also a CB(1) receptor ligand and inhibits the binding of the CB1 receptor antagonist [ ³H]CP-55940 to the CB1 receptor (IC₅₀: 19.31 μM) .

HY-B0905

Tilmicosin 5 Publications Verification LY-177370; EL-870	Bacterial Antibiotic Apoptosis Calcium Channel	Infection Inflammation/Immunology
Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects .

HY-12407

ZK168281 1 Publications Verification	VD/VDR	Metabolic Disease
ZK168281 is a 25-carboxylic ester 1α,25(OH)₂D₃ analog and a pure VDR antagonist with a K_d value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor .

HY-133017

Amcenestrant 3 Publications Verification SAR439859	Estrogen Receptor/ERR	Cancer
SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC₅₀ of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER ⁺ breast cancer.

HY-B0905A

Tilmicosin phosphate 5 Publications Verification LY-177370 phosphate; EL-870 phosphate	Bacterial Antibiotic Apoptosis NO Synthase COX	Infection Inflammation/Immunology
Tilmicosin (LY-177370) phosphate is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin phosphate mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin phosphate is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin phosphate has immunomodulatory and anti-inflammatory effects .

HY-15009

Fuscoside 1 Publications Verification OPC-21268	Vasopressin Receptor	Cardiovascular Disease Endocrinology
Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC₅₀ of 0.4 μM.

HY-P1023

VIP(6-28)(human, rat, porcine, bovine) 1 Publications Verification	GCGR	Metabolic Disease
VIP(6-28)(human, rat, porcine, bovine) is an effective antagonist of the actions of exogenous vasoactive intestinal peptide (VIP) on cAMP.

HY-B0780

Fimasartan 4 Publications Verification BR-A-657	Angiotensin Receptor Apoptosis NF-κB	Cardiovascular Disease Neurological Disease Inflammation/Immunology Endocrinology
Fimasartan (BRA-657) is an orally effective angiotensin receptor AT1 non-peptide antagonist. Fimasartan has antihypertensive effects. Fimasartan improves neuroinflammation and brain injury mediated by NLRP3 inflammatome after intracerebral hemorrhage, and has neuroprotective effect. Fimasartan inhibits the expression of inducible nitric oxide synthase through the inactivation of NF-κB and activator protein-1 .

HY-120084

BTX161 1 Publications Verification	Casein Kinase	Cancer
BTX161, a thalidomide analog, is an effective CKIα degrader. BTX161 mediates human AML cell CKIα degradation more effectively than lenalidomide and activates the DNA damage response (DDR) and p53, while stabilizing p53 antagonist MDM2.

HY-N6969

Dicentrine	Adrenergic Receptor	Endocrinology
Dicentrine is a natural product isolated from the plant Stephania epigaea Lo with antihypertensive effect. Dicentrine is an α₁-adrenoceptor antagonist which has effective against human hyperplastic prostates .

HY-B0971

Pheniramine maleate Prophenpyridamine maleate; Tripoton maleate	Histamine Receptor Apoptosis	Inflammation/Immunology Endocrinology
Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .

HY-B1164

Bromopride 2 Publications Verification	Dopamine Receptor	Neurological Disease
Bromopride is a selective, irreversible, competitive, and orally effective dopamine D2 receptor antagonist. Bromopride can pass through the blood-brain barrier, inhibit the vomiting center, and enhance gastrointestinal motility, exerting antiemetic and gastrointestinal motility effects. Bromopride antagonizes dopamine-mediated vomiting reflexes and promotes gastrointestinal smooth muscle contraction, and has no adverse effects on abdominal wall healing in rats with postoperative abdominal infection. Bromopride can be used for the study of digestive system diseases (such as gastric hypomotility, nausea and vomiting) .

HY-111480

Propionylpromazine	Dopamine Receptor	Neurological Disease
Propionylpromazine is a dopamine receptor DRD2 antagonist. Propionylpromazine also is an effective tranquillizer. Propionylpromazine can be used in veterinary studies .

HY-18641

Ki16198	LPL Receptor	Cancer
Ki16198 is a potent and orally active LPA receptor antagonist, the methyl ester of Ki16425 (HY-13285). Ki16198 inhibits LPA₁ and LPA₃-induced inositol phosphate production with?K_i?values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo .

HY-107322A

Barnidipine Mepirodipine; YM-09730-5 Free base	Calcium Channel	Cardiovascular Disease
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ ³H] initrendipine binding sites (K_i = 0.21 nmol/L), has selective action against CaA receptors. Barnidipine is an orally effective antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .

HY-119832B

(S)-Setastine (S)-EGIS-2062 free acid; (S)-EGYT-2062 free acid	Histamine Receptor	Inflammation/Immunology
(S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly potent antagonist of H1 receptor-mediated responses. (S)-Setastine has a long-lasting antihistamine effect and good oral efficacy. (S)-Setastine can be used in the research of allergic diseases .

HY-138937

NDB	FXR	Metabolic Disease
NDB is a selective human FXRα (hFXRα) antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research .

HY-101676

RG-12525 NID 525	Leukotriene Receptor PPAR Cytochrome P450	Metabolic Disease
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC₅₀s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC₅₀ of appr 60 nM and a potent inhibitor of CYP3A4, with a K_i value of 0.5 µM.

HY-127115

Sulukast LY 170680	Leukotriene Receptor	Inflammation/Immunology
Sulukast (LY 170680) is a selective leukotriene D₄ (LTD₄) antagonist. Sulukast exerts an effective antagonistic effect on bronchoconstriction induced by LTD₄. Sulukast can be used in the research of diseases such as asthma .

HY-152524

Androgen receptor antagonist 7	Androgen Receptor	Cancer
Androgen receptor antagonist 7 is an effective androgen receptor (AR) antagonist with an IC₅₀ value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI₅₀ value of 7.9 µM .

HY-12073

WAY-255348	Progesterone Receptor	Endocrinology Cancer
W-255348 is an effective non-steroidal progesterone receptor (PR) antagonist that acquires antagonist activity by binding to and subsequently blocking progesterone induced nuclear accumulation, phosphorylation, and PR promoter interactions. WAY-255348 can be used in the research of reproductive disorders or PR-positive breast cancer .

HY-P4745

hMCH-1R antagonist 1	MCHR1 (GPR24)	Metabolic Disease
hMCH-1R antagonist 1 (Compound 30) is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an K_B value of 3.6 nM. HMCH-1R antagonist 1 can bind to hMCHR1 and hMCHR2 with IC₅₀ values of 65 nM and 49 nM, respectively. HMCH-1R antagonistist 1 can be used for metabolic research .

HY-19501

DPC-168	CCR	Inflammation/Immunology
DPC-168 is an orally effective CCR3 antagonist (IC₅₀ = 41 nM). DPC-168 exhibits a significant ability to inhibit eosinophil chemotaxis and pulmonary inflammation. DPC-168 can be used for research on airway inflammation .

HY-B0971A

Pheniramine Prophenpyridamine; Tripoton; Pheniramine solution	Histamine Receptor Apoptosis	Inflammation/Immunology Cancer
Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .

HY-B0905R

Tilmicosin (Standard) LY-177370 (Standard); EL-870 (Standard)	Reference Standards Bacterial Antibiotic Apoptosis Calcium Channel	Infection Inflammation/Immunology
Tilmicosin (Standard) is the analytical standard of Tilmicosin. This product is intended for research and analytical applications. Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects .

HY-B0349A

Meclizine Meclozine	Histamine Receptor Apoptosis	Neurological Disease Inflammation/Immunology
Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease .

HY-U00207

MEN11467	Neurokinin Receptor	Neurological Disease Endocrinology
MEN11467 is a selective and orally- effective peptidomimetic tachykinin NK₁ receptor antagonist.

HY-129995

TSHR antagonist S37b	TSH Receptor	Endocrinology
TSHR antagonist S37b is the less effective enantiomer of TSHR antagonist S37a (HY-129995A). TSHR antagonist S37b shows only a minor effect for thyrotropin receptor (TSHR) inhibition. TSHR antagonist S37b can be used for the research of thyroid function .

HY-144127

AR antagonist 3	Androgen Receptor	Cancer
AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC₅₀ of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC₅₀= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .

HY-19668

SGS-518	5-HT Receptor	Neurological Disease
SGS-518 is a selective 5-HT₆R antagonist. SGS518 can be used for the research of cognitive impairments such as amnesia, anxiety and depression, and it is effective in protecting mouse retina at high doses .

HY-101946

AS-35	Leukotriene Receptor	Inflammation/Immunology
AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC₅₀ values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.

HY-10053S

Maropitant-d3	Isotope-Labeled Compounds Neurokinin Receptor	Neurological Disease Endocrinology
Maropitant-d₃ is the deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .

HY-107725A

BIBO3304 diTFA	Wnt Neuropeptide Y Receptor	Metabolic Disease
BIBO3304 (diTFA) is an orally effective and selective neuropeptide Y (NPY) Y1 receptor antagonist. BIBO3304 (diTFA) has a high affinity for both human and rat Y1 receptors, with IC₅₀ values of 0.38 and 0.72 nM, respectively. BIBO3304 (diTFA) promotes bone-tendon healing through the Wnt/β-catenin signaling pathway .

HY-B0905S

Tilmicosin-d3 LY-177370-d₃; EL-870-d₃	Isotope-Labeled Compounds Bacterial Antibiotic Apoptosis NO Synthase COX	Infection Inflammation/Immunology
Tilmicosin-d3 is the deuterium labeled Tilmicosin. Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects .

HY-107129

MK-3577	GCGR	Metabolic Disease
MK-3577 is an orally effective glucagon receptor (GCGR) antagonist that reduces hepatic glucose production and lowers blood glucose levels by blocking glucagon receptors on target organs, primarily the liver. Pharmacokinetic analysis in domestic cats indicates that MK-3577 reaches peak levels 3 to 4 hours after oral administration, with a half-life of approximately 15 hours. MK-3577 can be used in diabetes research .

HY-19429A

SLV-317	Neurokinin Receptor	Neurological Disease
SLV-317 is an antagonist of the neurokinin-1 receptor with oral activity. SLV-317 can effective antagonist of substance P-induced effects .

HY-19429

SLV-317 free base	Neurokinin Receptor	Metabolic Disease
SLV-317 (free base) is an antagonist of the neurokinin-1 receptor with oral activity. SLV-317 (free base) can effective antagonist of substance P-induced effects .

HY-167946

CP-866087	Opioid Receptor	Others
CP-866087 is a new, highly effective, and selective antagonist of the mu-opioid receptor designed for exploring female sexual dysfunction.

HY-161899

MCHR1 antagonist 4	MCHR1 (GPR24)	Others
MCHR1 antagonist 4 (Compound 2m) is a blood-brain barrier permeable MCHR1 antagonist with K_i values of 0.74 nM and 0.76 nM for hMCHR1 and rMCHR1, respectively. MCHR1 antagonist 4 is also an effective anti-obesity agent .

HY-19053

NP-252	Calcium Channel	Cardiovascular Disease
NP-252 is a calcium channel antagonist with an 20% effective dose (ED20) of 2.55 mg/kg in spontaneously hypertensive rats .

HY-P2118

NPC-567	Bradykinin Receptor	Inflammation/Immunology
NPC-567 is a bradykinin B2 receptor antagonist. NPC-567 is effective in inhibiting the acute response to allergen in the airways .

HY-129826

J-104129	mAChR	Others
J-104129 is a selective and orally active muscarinic M3 receptor antagonist (K_i = 4.2 nM). J-104129 is effective in promoting bronchodilation .

Cat. No.	Product Name	Type

HY-U00449G

AGN 193109

Fluorescent Dye

AGN 193109 (GMP) is AGN 193109 (HY-U00449) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AGN 193109 is a specific and highly effective retinoic acid receptor (RAR) antagonist . AGN 193109 (GMP) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. AGN 193109 is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity.

Cat. No.	Product Name	Type

HY-U00449G

AGN 193109

Biochemical Assay Reagents

Cat. No.	Product Name	Target	Research Area

HY-P1023

VIP(6-28)(human, rat, porcine, bovine) 1 Publications Verification	GCGR	Metabolic Disease
VIP(6-28)(human, rat, porcine, bovine) is an effective antagonist of the actions of exogenous vasoactive intestinal peptide (VIP) on cAMP.

HY-P4745

hMCH-1R antagonist 1	MCHR1 (GPR24)	Metabolic Disease
hMCH-1R antagonist 1 (Compound 30) is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an K_B value of 3.6 nM. HMCH-1R antagonist 1 can bind to hMCHR1 and hMCHR2 with IC₅₀ values of 65 nM and 49 nM, respectively. HMCH-1R antagonistist 1 can be used for metabolic research .

HY-P2118

NPC-567	Bradykinin Receptor	Inflammation/Immunology
NPC-567 is a bradykinin B2 receptor antagonist. NPC-567 is effective in inhibiting the acute response to allergen in the airways .

HY-P2446

ORG 30276 APTAA-LHRH	GnRH Receptor	Endocrinology
ORG 30276 (APTAA-LHRH) is a potent GnRH antagonist that effectively reduces serum LH and FSH levels in male rats. ORG 30276 significantly decreases unoccupied pituitary GnRH receptors, leading to suppressed gonadotropin secretion. ORG 30276 treatment results in a considerable reduction in mRNA levels of gonadotropin beta-subunits in the pituitary gland. ORG 30276's effects on gonadotropin dynamics can be selectively reversed by the replacement of specific sex steroids, with androgens being particularly effective for the FSH beta-subunit mRNA levels.

HY-P0038

MK-852 L-367073	Integrin	Cardiovascular Disease
MK-852 (L-367073) is an effective GPIIb/IIIa receptor antagonist. MK-852 can significantly inhibit the binding of fibrinogen to platelets in vitro. MK-852can be used for the study of thrombosis .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0925

Tetrahydroberberine 2 Publications Verification Canadine	Alkaloids Corydalis yanhusuo W. T. Wang Plants Isoquinoline Alkaloids Papaveraceae Source Classification	Dopamine Receptor
Tetrahydroberberine is a different kind of living thing that can be extended and divided into parts. Tetrahydroberberine is a kind of effective D2 receptor antagonistic force. Tetrahydroberberine has the ability to strengthen the stomach and relieve the pressure on the stomach .

HY-N6969

Dicentrine	Alkaloids Structural Classification Classification of Application Fields Stephania epigaea Lo Plants Isoquinoline Alkaloids Menispermaceae Disease Research Fields Endocrinology Source Classification	Adrenergic Receptor
Dicentrine is a natural product isolated from the plant Stephania epigaea Lo with antihypertensive effect. Dicentrine is an α₁-adrenoceptor antagonist which has effective against human hyperplastic prostates .

HY-N6932

Voacamine	Alkaloids other families Classification of Application Fields Metabolic Disease Plants Disease Research Fields Indole Alkaloids Source Classification	Cannabinoid Receptor P-glycoprotein PI3K Akt mTOR Apoptosis Autophagy EGFR
Voacamine is an indole alkaloid with cannabinoid 1 (CB1) antagonistic activity. Voacamine can inhibit nuclear translocation. Voacamine is effective in enhancing the effect of Doxorubicin (HY-15142A) as it interferes with the P-glycoprotein (P-gp) function. Voacamine promotes apoptosis-independent autophagic cell death in human osteosarcoma cells. Voacamine activates mitochondrial-associated apoptosis signaling pathway and inhibition of PI3K/Akt/mTOR signaling pathway to suppress breast cancer progression. Voacamine inhibits EGFR to exert oncogenic activity against colorectal cancer .

HY-N1514R

Ganoderenic acid B (Standard)	Triterpenes Structural Classification Human Gut Microbiota Metabolites Microorganisms Terpenoids Polyporaceae Ganoderma lucidum (Leyss. Ex Fr.) Karst. Plants Endogenous metabolite Source Classification	Reference Standards P-glycoprotein
Doxylamine (succinate) (Standard) is the analytical standard of Doxylamine (succinate). This product is intended for research and analytical applications. Doxylamine (succinate), a first generation antihistamine, is a histamine (H1) receptor antagonist. Doxylamine is also a local analgesic agent and effective hypnotic agent .

HY-N0925R

Tetrahydroberberine (Standard) Canadine (Standard)	Alkaloids Structural Classification Corydalis yanhusuo W. T. Wang Plants Isoquinoline Alkaloids Papaveraceae Source Classification	Reference Standards Dopamine Receptor
Tetrahydroberberine (Standard) is the analytical standard of Tetrahydroberberine. This product is intended for research and analytical applications. Tetrahydroberberine is a different kind of living thing that can be extended and divided into parts. Tetrahydroberberine is a kind of effective D2 receptor antagonistic force. Tetrahydroberberine has the ability to strengthen the stomach and relieve the pressure on the stomach .

HY-N7814R

2-Hydroxypalmitic acid (Standard)	Structural Classification Microorganisms Ketones, Aldehydes, Acids Source Classification	Reference Standards Endogenous Metabolite
Pheniramine (maleate) (Standard) is the analytical standard of Pheniramine (maleate). This product is intended for research and analytical applications. Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .

HY-129482

Detoxin D1	Natural Products Microorganisms Source Classification	Others
Detoxin D1 is a compound with antihistamine activity and a new type of H1 antagonist. In the suppression of seasonal allergic rhinitis, a daily dose of 10-30 mg has an equivalent and highly effective inhibitory effect compared with placebo and has good safety.

Cat. No.	Product Name	Chemical Structure

HY-106901AS

Asoxime-d4 dichloride

1 Publications Verification

Asoxime-d₄ dichloride (HI-6-d₄) is the deuterium labeled Asoxime dichloride. Asoxime dichloride is an orally active thiosemicarbazone-based antidote. Asoxime dichloride is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dichloride significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dichloride is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dichloride can serve as an effective immunomodulator, improving the immune effect of the nervous system.

HY-10053S

Maropitant-d3
Maropitant-d₃ is the deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .

HY-B0905S

Tilmicosin-d3

Tilmicosin-d3 is the deuterium labeled Tilmicosin. Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects .

HY-A0019AS

Paliperidone palmitate-d4

Paliperidone palmitate-d₄ (9-Hydroxyrisperidone palmitate-d₄) is the deuterium labeled Paliperidone palmitate (HY-A0019A). Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .

HY-U00449S

AGN 193109-d7
AGN 193109-d₇ is the deuterium labeled AGN 193109. AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively.

HY-10053S1

Maropitant-13C,d3
Maropitant- ¹³C,d₃ is the ¹³C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .

HY-A0118AS

Naloxegol-d5 oxalate
Naloxegol-d₅ (oxalate) is deuterium labeled Naloxegol (oxalate). Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .

HY-W751574

Elagolix-d6 sodium
Elagolix-d₆ (sodium) (NBI-56418-d₆ (sodium)) is deuterium labeled Elagolix sodium. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K_D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

HY-A0118S1

Naloxegol-13C,d2
Naloxegol- ¹³C,d₂ (NKTR-118- ¹³C,d₂) is ¹³C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .

HY-A0118S

Naloxegol-13C,d3
Naloxegol- ¹³C,d₃ (NKTR-118- ¹³C,d₃) is ¹³C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .

HY-115633S

Elagolix-d9
Elagolix-d₉ is the deuterium labeled Elagolix. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K_D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

Cat. No.	Product Name		Classification

HY-106203

Crinecerfont SSR-125543		Alkynes
Crinecerfont (SSR-125543) is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency . Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-106203A

Crinecerfont hydrochloride SSR-125543 hydrochloride		Alkynes
Crinecerfont (SSR-125543) hydrochloride is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont hydrochloride blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont hydrochloride improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont hydrochloride can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency . Crinecerfont hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-179232

ERα antagonist 2		Tetrazine
ERα antagonist 2 (Compound 5b) is an ER-α antagonist with an IC₅₀ value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer .

HY-106203B

(R)-Crinecerfont (R)-SSR-125543		Alkynes
(R)-Crinecerfont is the R-enantiomer of Crinecerfont (HY-106203). Crinecerfont (SSR-125543) is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency . Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-180120

UM-203		Alkynes
UM-203 is a reversible covalent STING antagonist. UM-203 is effective against both mouse and human STING, and in particular, it inhibits the most common human STING R232 variant. UM-203 can inhibit STING oligomerization and reduce phosphorylation of downstream TBK1 and IRF3, thereby blocking the IRF3 and NF-κB-mediated signaling pathways and inhibiting IFNβ and IL-6 secretion. UM-203 can be used for the research of inflammation and immunology, such as systemic lupus erythematosus .

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-U00449G

AGN 193109	RAR/RXR	Cancer
AGN 193109 (GMP) is AGN 193109 (HY-U00449) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AGN 193109 is a specific and highly effective retinoic acid receptor (RAR) antagonist . AGN 193109 (GMP) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. AGN 193109 is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity.

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