Search Result
Results for "
non-peptide antagonist
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-103363
-
-
-
- HY-B0780
-
-
-
- HY-101986
-
-
-
- HY-14789
-
NBI-56418
|
GnRH Receptor
|
Endocrinology
Cancer
|
Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).
|
-
-
- HY-101844
-
|
Bombesin Receptor
|
Cancer
|
ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
|
-
-
- HY-135500
-
|
Endothelin Receptor
|
Endocrinology
|
ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .
|
-
-
- HY-123617
-
-
-
- HY-19214
-
-
-
- HY-16711
-
-
-
- HY-120261
-
-
-
- HY-18347A
-
-
-
- HY-103357
-
-
-
- HY-107533
-
|
GnRH Receptor
|
Endocrinology
|
T-98475 (Compound 26d) is a potent, orally active, non-peptide luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.2 nM .
|
-
-
- HY-101986C
-
AR-H 053591 dihydrochloride
|
Neuropeptide Y Receptor
|
Neurological Disease
|
BIIE-0246 dihydrochloride (AR-H 053591 dihydrochloride) is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 value of 15 nM .
|
-
-
- HY-10049A
-
|
Neurokinin Receptor
|
Neurological Disease
|
CP 122721 hydrochloride is a potent, non-peptide and selective nonpeptide neurokinin NK1 antagonist, with a pIC50 of 9.8 for human NK1 receptor expressed in IM-9 cells. CP 122721 hydrochloride exhibits anxiolytic and antidepressant-like effects .
|
-
-
- HY-109093
-
KLH-2109; OBE-2109
|
GnRH Receptor
|
Inflammation/Immunology
Cancer
|
Linzagolix (KLH-2109; OBE-2109) is a potent, non-peptide, and orally active GnRH antagonist. Linzagolix can be used for uterine fibroids, endometriosis, adenomyosis research .
|
-
-
- HY-108479
-
SR140333
|
Neurokinin Receptor
|
Neurological Disease
|
Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
|
-
-
- HY-108555
-
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
FR171113 is a specific and non-peptide thrombin receptor antagonist. FR171113 exhibits the antithrombotic effects of a PAR1 antagonist. FR171113 inhibits thrombin-induced platelet aggregation with an IC50 of 0.29 μM. .
|
-
-
- HY-14184
-
-
-
- HY-19947
-
Glucagon receptor antagonists-4
|
GCGR
|
Metabolic Disease
|
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM) .
|
-
-
- HY-10095
-
BIBN-4096; BIBN 4096BS
|
CGRP Receptor
|
Neurological Disease
|
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP .
|
-
-
- HY-10095A
-
BIBN-4096 hydrochloride; BIBN4096BS hydrochloride
|
CGRP Receptor
|
Neurological Disease
|
Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP .
|
-
-
- HY-19529
-
-
-
- HY-103304
-
|
Others
|
Neurological Disease
|
CGRP antagonist 4 is an antagonist of calcitonin gene-related peptide (CGRP) receptor. CGRP antagonist 4 shows the highest affinity for CGRP receptors in the human brain. CGRP antagonist 4 can be used to study the binding properties of non-peptide calcitonin gene-related peptide (CGRP) receptor antagonist (gepants) in rat, pig and human menes .
|
-
-
- HY-70068
-
-
-
- HY-12080
-
ZK-811752
|
CCR
|
Inflammation/Immunology
Endocrinology
|
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
|
-
-
- HY-14184A
-
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
|
-
-
- HY-12080A
-
ZK-811752 hydrochloride
|
CCR
|
Inflammation/Immunology
Endocrinology
|
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
|
-
-
- HY-14184S
-
-
-
- HY-N2600
-
|
Bombesin Receptor
|
Cancer
|
Kuwanon H is a flavonoid isolated from Morus alba, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells .
|
-
-
- HY-19431
-
|
Endothelin Receptor
|
Cardiovascular Disease
|
Ro 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM) .
|
-
-
- HY-U00235
-
|
Integrin
|
Inflammation/Immunology
|
SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.
|
-
-
- HY-76612
-
-
-
- HY-108483
-
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation .
|
-
-
- HY-108677
-
|
Oxytocin Receptor
|
Endocrinology
|
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 hydrochloride used as a tocolytic agent .
|
-
-
- HY-10898
-
-
-
- HY-110155A
-
|
Others
|
Neurological Disease
|
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist .
|
-
-
- HY-108625
-
SHA 68
1 Publications Verification
|
Neuropeptide Y Receptor
|
Neurological Disease
|
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .
|
-
-
- HY-106840A
-
|
Cholecystokinin Receptor
|
Neurological Disease
Metabolic Disease
|
L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors .
|
-
-
- HY-108626
-
NCGC84
|
Neuropeptide Y Receptor
|
Neurological Disease
|
ML154 (NCGC84) is a selective, brain-penetrant and non-peptide neuropeptide S receptor (NPSR) antagonist with a pA2 of 9.98. ML154 potently inhibits NPS-stimulated cellular calcium, cAMP, and ERK phosphorylation responses with IC50 values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively .
|
-
-
- HY-106203
-
SSR-125543
|
CFTR
|
Metabolic Disease
|
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . 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
-
SSR-125543 hydrochloride
|
CFTR
|
Metabolic Disease
|
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . 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-15011
-
|
Oxytocin Receptor
|
Others
|
L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR .
|
-
-
- HY-15522
-
|
Oxytocin Receptor
|
Neurological Disease
|
WAY-267464 is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder .
|
-
-
- HY-15023
-
PF-3274167
|
Oxytocin Receptor
|
Endocrinology
|
Cligosiban (PF-3274167), a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (Ki=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V1b and V1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents .
|
-
-
- HY-108679
-
|
Oxytocin Receptor
|
Neurological Disease
|
WAY-267464 hydrochloride is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 hydrochloride can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 hydrochloride can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder .
|
-
-
- HY-107692
-
|
Neurokinin Receptor
|
Neurological Disease
|
SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit .
|
-
-
- HY-103377
-
|
CRFR
|
Inflammation/Immunology
Endocrinology
|
Antalarmin (hydrochloride) is a non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a Ki of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome .
|
-
-
- HY-106840
-
|
Cholecystokinin Receptor
|
Neurological Disease
Metabolic Disease
|
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance .
|
-
-
- HY-15039
-
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
|
-
- HY-101764
-
SR 27897
|
Cholecystokinin Receptor
|
Metabolic Disease
|
Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin .
|
-
- HY-106994A
-
YM598
|
Endothelin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .
|
-
- HY-106994
-
YM598 free base
|
Endothelin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .
|
-
- HY-15015A
-
-
- HY-16992A
-
W-54011
4 Publications Verification
|
Complement System
Reactive Oxygen Species
|
Inflammation/Immunology
|
W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca 2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively .
|
-
- HY-100292
-
-
- HY-15015
-
Oxytocin receptor antagonist 1
|
Oxytocin Receptor
|
Endocrinology
|
OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist.
|
-
- HY-19732
-
-
- HY-107691
-
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .
|
-
- HY-110155
-
|
Neurotensin Receptor
|
Neurological Disease
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
|
-
- HY-123744
-
-
- HY-19670
-
-
- HY-19210
-
|
Endothelin Receptor
|
Cardiovascular Disease
|
SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
|
-
- HY-19191
-
-
- HY-15009
-
-
- HY-107664
-
|
Neurotensin Receptor
|
Neurological Disease
|
SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders .
|
-
- HY-107664A
-
|
Neurotensin Receptor
|
Neurological Disease
|
SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders .
|
-
- HY-108480
-
|
Neurokinin Receptor
|
Neurological Disease
|
SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against human NK1 receptor. SDZ NKT 343 has good analgesic activity .
|
-
- HY-101720
-
BIBU-52
|
Integrin
|
Cardiovascular Disease
|
Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.
|
-
- HY-10315
-
RWJ-53308
|
Integrin
|
Cardiovascular Disease
|
Elarofiban (RWJ-53308) is a nonpeptide, orally active fibrinogen receptor antagonist. Elarofiban has the potential for platelet mediated thrombotic disorders research .
|
-
- HY-101720A
-
BIBU-52 hydrochloride
|
Integrin
|
Cardiovascular Disease
|
Fradafiban (BIBU-52) hydrochloride is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.
|
-
- HY-124475
-
|
CRFR
|
Neurological Disease
|
Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier .
|
-
- HY-10309
-
RO 48-3657
|
Integrin
|
Cardiovascular Disease
|
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-proagent of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation .
|
-
- HY-19307
-
|
|
|
SB-273005 is a potent nonpeptide and orally active integrin antagonist with Kis of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively .
|
-
- HY-106277A
-
MEN16132
|
Bradykinin Receptor
|
Metabolic Disease
|
Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis .
|
-
- HY-106277
-
|
Bradykinin Receptor
|
Metabolic Disease
|
Fasitibant (free base) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant (free base) has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis .
|
-
- HY-100301
-
|
Bradykinin Receptor
|
Inflammation/Immunology
Endocrinology
|
FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist. FR167344 free base shows a high affinity binding to the B2 receptor with an IC50 value of 65 nM and no binding affinity for the B1 receptor.
|
-
- HY-14886
-
MEN16132 free base
|
Bradykinin Receptor
|
Cardiovascular Disease
Neurological Disease
|
Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model .
|
-
- HY-12436
-
|
Neurotensin Receptor
|
Neurological Disease
|
NTRC-824 (Compound 5) is a potent, selective and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist with an IC50 of 38 nM and a Ki of 202 nM. NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (Ki >30 μM) .
|
-
- HY-13406
-
TAK-779
2 Publications Verification
Takeda 779
|
CCR
HIV
CXCR
|
Infection
Inflammation/Immunology
Endocrinology
|
TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
|
-
- HY-110166
-
|
Others
|
Neurological Disease
|
PD 90780 is a non peptide antagonist of nerve growth factor (NGF). PD 90780 interacts with NGF, prevents NGF binds with p75 NTR. PD 90780 inhibits NGF-p75 NTR interaction with IC50s of 23.1 and 1.8 µM in PC12 cells and PC12 nnr5 cells, respectively .
|
-
- HY-B1330
-
|
Cholecystokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities .
|
-
- HY-50688
-
|
CXCR
|
Inflammation/Immunology
|
SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively .
|
-
- HY-103354
-
|
Cholecystokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities .
|
-
- 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-103354A
-
|
Cholecystokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
Proglumide hemicalcium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide hemicalcium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities .
|
-
- HY-16981
-
|
CXCR
|
Inflammation/Immunology
|
SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells .
|
-
- HY-101368A
-
|
|
|
WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [ 3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [ 3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM) .
|
-
- HY-120295
-
|
Endothelin Receptor
Apoptosis
|
Cardiovascular Disease
Endocrinology
|
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level .
|
-
- HY-15102
-
MK-0429
3 Publications Verification
L-000845704
|
Integrin
|
Inflammation/Immunology
Cancer
|
MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively .
|
-
- HY-14994
-
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
|
-
- HY-14993
-
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
|
-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-14184S
-
|
Macitentan-d4 is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1].
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-106203A
-
SSR-125543 hydrochloride
|
|
Alkynes
|
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . 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-106203
-
SSR-125543
|
|
Alkynes
|
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . 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.
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: