Search Result
Results for "
Effective antagonists
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-119832B
-
|
(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-15009
-
-
-
- HY-111480
-
|
|
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-129995
-
|
|
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
-
|
|
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-U00207
-
-
-
- HY-U00363
-
-
-
- HY-19429A
-
-
-
- HY-167946
-
|
|
Others
|
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 (GPR24)
|
Others
|
|
MCHR1 antagonist 4 (Compound 2m) is a blood-brain barrier permeable MCHR1 antagonist with Ki 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-P1023
-
|
|
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-110292
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
A-425619, a potent and selective TRPV1 receptor antagonist, is effective in alleviating acute and chronic inflammatory pain and postoperative pain .
|
-
-
- HY-19053
-
-
-
- HY-P2118
-
-
-
- HY-152524
-
|
|
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-A0069A
-
-
-
- HY-12870
-
AZD9496
Maximum Cited Publications
25 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-131041
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Ned-K is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist. Ned-K is effective at dampening simulated ischaemia and reperfusion (sIR)-induced Ca 2+ oscillations in cardiomyocytes .
|
-
-
- HY-129826
-
|
|
mAChR
|
Others
|
|
J-104129 is a selective and orally active muscarinic M3 receptor antagonist (Ki = 4.2 nM). J-104129 is effective in promoting bronchodilation .
|
-
-
- HY-A0069
-
-
-
- HY-138937
-
|
|
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-167866
-
-
-
- HY-159896
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
PAR4 antagonist 8 (Compound 20f) is an effective, orally active, and selective PAR4 antagonist with an IC50 value of 15.32 nM. PAR4 antagonist 8 exhibits favorable pharmacokinetic properties. PAR4 antagonist 8 not only effectively inhibits human platelet aggregation induced by PAR4 agonists (IC50 = 6.39 nM) but also inhibits mouse platelet aggregation. PAR4 antagonist 8 can be used in antithrombotic research .
|
-
-
- HY-N0925
-
|
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-N6969
-
|
|
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-107616
-
|
|
LPL Receptor
Apoptosis
|
Others
|
|
H2L5186303 is an effective and selective LPA2 receptor antagonist, with an IC50 of 9 nM, and it has anti-inflammatory effects. H2L5186303 can inhibit intestinal cell proliferation and promote apoptosis .
|
-
-
- HY-101234
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
ICI 162846 is an orally active antagonist of H2 receptor. ICI 162846 inhibits acid production accompanied by an increase in the secretion of histamine in chronic duodenal ulcer (CDU) models. ICI 162846 is effective in preventing CDU .
|
-
-
- HY-10053
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
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-A0118
-
|
NKTR-118; AZ-13337019
|
Opioid Receptor
|
Neurological Disease
Cancer
|
|
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-P4745
-
|
|
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 KB 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-101946
-
|
|
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-19668A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SGS518 oxalate is a selective 5-HT6R antagonist. SGS518 oxalate 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 [1]
|
-
-
- HY-B0954A
-
|
|
mAChR
|
Endocrinology
|
|
Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm .
|
-
-
- HY-129482
-
|
|
Others
|
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.
|
-
-
- HY-W370556
-
|
|
Others
|
Neurological Disease
|
|
(Rac)-LM11A-31 is a racemate of LM11A-31. LM11A-31 is a non-peptide modulator of p75NTR (neurotrophin receptor p75) and is an orally effective proNGF antagonist .
|
-
-
- HY-159802
-
|
|
Others
|
Endocrinology
|
|
Tolamolol is a selective beta-adrenergic antagonist with significant activity in reducing exercise-induced ST-segment depression. Tolamolol is clinically equivalent to propranolol in suppressing angina and exhibits greater cardiac selectivity. Tolamolol is effective in reducing the frequency of angina attacks and the amount of glyceryl trinitrate used. Tolamolol is effective in lowering blood pressure and has a positive effect on increasing the amount of exercise that can be performed before angina attacks. The use of Tolamolol also helps improve the suppression of arrhythmias .
|
-
-
- HY-14789
-
-
-
- HY-14369
-
-
-
- HY-U00449S
-
|
|
Isotope-Labeled Compounds
RAR/RXR
|
Cancer
|
|
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-A0118A
-
|
NKTR-118 oxalate; AZ-13337019 oxalate
|
Opioid Receptor
|
Neurological Disease
Cancer
|
|
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-A0069R
-
|
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
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-125615
-
|
|
Glycoprotein VI
|
Cardiovascular Disease
Others
|
|
DMP 728 methanesulfonate is a platelet glycoprotein (GP) IIb/IIIa receptor antagonist. DMP 728 methanesulfonate shows dose-dependent antiplatelet and antithrombotic effects. DMP 728 methanesulfonate can be used in the study of effective antithrombotic agents in thromboembolic diseases of coronary and peripheral arteries .
|
-
-
- HY-12407
-
|
|
VD/VDR
|
Metabolic Disease
|
|
ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor .
|
-
-
- HY-120084
-
|
|
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-155041
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Antihypertensive agent 2 (Compound 4g) is an antihypertensive agent. Antihypertensive agent 2 has effective antagonistic activities against angiotensin II receptor 1. Antihypertensive agent 2 reduces the blood pressure with equal or more potency compared to Losartan (HY-17512) .
|
-
-
- HY-N0925R
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
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-133017
-
|
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-107601
-
|
ACET
|
iGluR
|
Neurological Disease
|
|
UBP316 (ACET) is a highly potent and selective kainate receptor GluK1 (GluR5) antagonist, with a Kb 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-119097
-
|
|
mGluR
|
Neurological Disease
|
|
LY456066 is a selective non-competitive metabotropic glutamate receptors (mGluR1) antagonist with an IC50 value of 52.0 nM. LY456066 is effective in rodent models of anxiolysis and nociception. LY456066 reduces hyperalgesia and the amount of licking and flinching following formalin injection, which is promising for research of analgesics for chronic pain .
|
-
-
- HY-107566A
-
|
|
Histamine Receptor
Parasite
|
Infection
|
|
Conessine dihydrobromide is a steroidal alkaloid and an effective, selective histamine H3 receptor antagonist with Ki values of 5.4, 6.0, 5.7, and 25 nM for human, dog, guinea pig, and rat H3 receptors, respectively. Conessine dihydrobromide exhibits antimalarial activity and can be used in infection-related research .
|
-
- HY-127113
-
|
|
Leukotriene Receptor
|
Cardiovascular Disease
|
|
Q8, an effective antiangiogenic drug, is a CysLt1 antagonist (IC50 of 4.9 μM). Q8 is sufficient to reduce cellular levels of NF-κB and calpain-2 and secreted levels of the proangiogenic proteins intercellular adhesion molecule-1, vascular cell adhesion protein-1, and VEGF .
|
-
- HY-12598A
-
DHPG
3 Publications Verification
(RS)-3,5-DHPG
|
mGluR
|
Neurological Disease
|
|
DHPG ((RS)-3,5-DHPG) is an amino acid, which acts as a selective and potent agonist of group I mGluR (mGluR 1 and mGluR 5), shows no effect on Group II or Group III mGluRs . DHPG ((RS)-3,5-DHPG) is also an effective antagonist of mGluRs linked to phospholipase D .
|
-
- HY-106301
-
|
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-B1161A
-
|
(+)-Methoprene; (7S)-Methoprene
|
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-10053S1
-
|
|
Isotope-Labeled Compounds
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
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[1][2].
|
-
- HY-A0118AS
-
|
|
Isotope-Labeled Compounds
Opioid Receptor
|
Neurological Disease
|
|
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[1][2].
|
-
- HY-B0971
-
|
Prophenpyridamine maleate; Tripoton maleate; Pheniramine 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-B0971A
-
|
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-B0661C
-
|
YM12617 hydrochloride; LY253351 hydrochloride
|
Others
|
Endocrinology
|
|
Tamsolusin (YM12617) hydrochloride is a highly selective alpha-1A adrenergic receptor antagonist used in the treatment of benign prostatic hypertrophy, demonstrating effective biological activity in alleviating associated symptoms. Tamsolusin hydrochloride can also be quantified using a validated spectrofluorimetric method, showcasing its potential for routine quality control analysis in pharmaceutical formulations.
|
-
- HY-107322A
-
|
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 (Ki = 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-18641
-
|
|
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?Ki?values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo .
|
-
- HY-19917
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
JNJ-39220675 is a selective and brain-penetrating histamine H3 receptor antagonist with activity in regulating alcohol stimulation and reward. JNJ-39220675 is effective in reducing alcohol intake and preference in alcohol-preferring rats. JNJ-39220675 does not affect the ataxic effects of alcohol, the rate of alcohol elimination, or alcohol-induced nucleocapsid dopamine release .
|
-
- HY-B0905
-
|
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-B0905A
-
|
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-107725A
-
|
|
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-111066
-
|
|
Others
|
Others
|
|
JNJ-37822681 is a fast dissociating D2 antagonist with activity in inhibiting schizophrenia. JNJ-37822681 has high specificity for D2 receptors and is effective in animal models, inducing increased levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibiting antidepressant activity in the mouse tail suspension test, while having a good brain distribution and lower prolactin release.
|
-
- HY-B0905S
-
|
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-B0780
-
-
- HY-B0905R
-
|
|
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-U00449
-
|
|
RAR/RXR
|
Cancer
|
|
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. 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-106301R
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Devazepide (Standard) is the analytical standard of Devazepide. This product is intended for research and analytical applications. 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-100840A
-
|
4-Carboxy-3-hydroxyphenylglycine
|
mGluR
|
Neurological Disease
|
|
(RS)-4C3HPG (4-Carboxy-3-hydroxyphenylglycine) is an effective competitive antagonist at the metabotropic glutamate receptor 1 (mGluR1) in the central nervous system, and it is also an agonist at mGluR2/3. (RS)-4C3HPG exhibits neuroprotective effects in an acute global ischemia rat model .
|
-
- HY-B0349
-
|
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-B0349A
-
|
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-B0349B
-
|
Meclozine dihydrochloride monohydrate
|
Histamine Receptor
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
Meclizine (Meclozine) dihydrochloride monohydrate, 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 monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease .
|
-
- HY-107129
-
|
|
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-118758
-
|
γ-Kainic acid-glutamic acid
|
Sodium Channel
|
Neurological Disease
|
|
γ-Kainylglutamic acid (γ-Kainic acid-glutamic acid), a dipeptide derived from kainic and L-Glutamic acids, is a selective antagonist of amino acid induced neuroexcitation with anticonvulsant properties. γ-Kainylglutamic acid inhibits the stimulation of Na + fluxes induced in brain slices by the neuroexcitant N-methyl-D-aspartic acid. γ-Kainylglutamic acid is also effective in protecting mice from picrotoxin-induced convulsions with an EC50 value of 0.17 μmol .
|
-
- HY-101676
-
|
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 Ki value of 0.5 µM.
|
-
- HY-108521
-
|
|
RAR/RXR
Apoptosis
|
Metabolic Disease
Cancer
|
|
HX531 is an effective RXR antagonist with oral activity, with an IC50 of 18 nM, with activity against black melanoma. HC531 can eliminate the anti-apoptotic effects of all-trans-retinoic acid (t-RA) and exerts anti-obesity and anti-diabetic effects through leptin-dependent pathways and the p53-p21Cip1 pathway, resulting in G0/G1 cell cycle arrest .
|
-
- HY-19279A
-
|
|
Others
|
Endocrinology
|
|
JTH-601 Free base is a novel alpha1-adrenoceptor antagonist that exhibits potent activity in inhibiting phenylephrine-induced contractions in lower urinary tract tissues. JTH-601 Free base competitively antagonizes alpha1-adrenoceptor-mediated contractile responses, demonstrating greater potency than prazosin or tamsulosin. JTH-601 Free base is anticipated to be effective in treating urinary outlet obstruction associated with benign prostatic hyperplasia.
|
-
- HY-B0349R
-
|
|
Histamine Receptor
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
Meclizine (dihydrochloride) (Standard) is the analytical standard of Meclizine (dihydrochloride). This product is intended for research and analytical applications. 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-B0020
-
|
SDZ-ICS-930
|
5-HT Receptor
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Tropisetron Hydrochloride (SDZ-ICS-930) is an effective neuroprotective agent that acts as a 5-HT3 receptor antagonist, a calmodulin inhibitor, and an α7-nAChRreceptor agonist, with an IC50 of 70.1 nM for the 5-HT3 receptor. Tropisetron Hydrochloride has anti-inflammatory properties and immune-regulating functions, effectively alleviating symptoms associated with chemotherapy and post-surgery. Tropisetron Hydrochloride reduces Ab (HY-P4867)-induced hippocampal neuroinflammation .
|
-
- HY-13208
-
|
AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
|
IAP
Apoptosis
|
Cancer
|
|
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .
|
-
- HY-U00449G
-
|
|
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.
|
-
- HY-117792
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
LY314228 is an aminoguanidine 5-HT2 antagonist with relative selectivity for 5-HT2A receptors (IC50: 147.9 nM). The Ki values ??of LY314228 targeting different 5-HT subtypes are 65 nM (5-HT 2A), 1214 nM (5-HT 2B), and 168 nM (5-HT 2C), respectively. LY314228 is an effective inhibitor of 5-HT-induced paw edema in rats with an ED50 of 6.4 mg/kg in ovariectomized female rats. .
|
-
- HY-101094
-
|
R79598
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
|
-
- HY-B0020R
-
|
SDZ-ICS-9323 (Standard)
|
5-HT Receptor
nAChR
|
Neurological Disease
Cancer
|
|
Tropisetron (Hydrochloride) (Standard) is the analytical standard of Tropisetron (Hydrochloride). Tropisetron Hydrochloride (SDZ-ICS-930) is an effective neuroprotective agent that acts as a 5-HT3 receptor antagonist, a calmodulin inhibitor, and an α7-nAChRreceptor agonist, with an IC50 of 70.1 nM for the 5-HT3 receptor. Tropisetron Hydrochloride has anti-inflammatory properties and immune-regulating functions, effectively alleviating symptoms associated with chemotherapy and post-surgery. Tropisetron Hydrochloride reduces Ab (HY-P4867)-induced hippocampal neuroinflammation .
|
-
- HY-U00237B
-
|
|
Others
|
Others
|
|
L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
|
-
- HY-162677
-
|
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
|
MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-U00449G
-
|
|
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
-
|
|
Biochemical Assay Reagents
|
|
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 |
Target |
Research Area |
-
- HY-P1023
-
|
|
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-P2118
-
-
- HY-P4745
-
|
|
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 KB 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-P2446
-
|
APTAA-LHRH
|
Peptides
|
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.
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-U00449S
-
|
|
|
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 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[1][2].
|
-
-
- HY-A0118AS
-
|
|
|
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[1][2].
|
-
-
- HY-B0905S
-
|
|
|
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 .
|
-
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent:
