Search Result

Results for "

Allosteric antagonists

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (2) Autophagy (1) Bcl-2 Family (1) Calcium Channel (1) Cannabinoid Receptor (1) Caspase (1) CaSR (1) CCR (8) Cholinesterase (ChE) (1) CX3CR1 (1) CXCR (9) Cytochrome P450 (2) Dopamine Receptor (8) Drug Derivative (1) ERK (1) Estrogen Receptor/ERR (1) GABA Receptor (4) Galectin (1) GCGR (2) GPR35 (1) HCN Channel (1) Histamine Receptor (5) HIV (3) iGluR (2) Influenza Virus (1) Integrin (1) Interleukin Related (1) Isotope-Labeled Compounds (2) Ligands for Target Protein for PROTAC (1) mAChR (10) mGluR (19) MicroRNA (1) mTOR (1) Neurokinin Receptor (2) Neuropeptide Y Receptor (1) Neurotensin Receptor (1) Opioid Receptor (2) Orphan GPCR (1) P2X Receptor (7) P2Y Receptor (2) PERK (1) PI3K (1) PPAR (2) Prostaglandin Receptor (1) Protease Activated Receptor (PAR) (1) Protein Arginine Deiminase (1) Reference Standards (7) SARS-CoV (1) Src (1) Taste Receptor (1) TGF-beta/Smad (1) Topoisomerase (1) TSH Receptor (1)
By Research Areas:	Cancer (24) Cardiovascular Disease (5) Endocrinology (9) Infection (8) Inflammation/Immunology (28) Metabolic Disease (8) Neurological Disease (44)

By Targets:

Akt (1)

Apoptosis (2)

Autophagy (1)

Bcl-2 Family (1)

Calcium Channel (1)

Cannabinoid Receptor (1)

Caspase (1)

CaSR (1)

CCR (8)

Cholinesterase (ChE) (1)

CX3CR1 (1)

CXCR (9)

Cytochrome P450 (2)

Dopamine Receptor (8)

Drug Derivative (1)

ERK (1)

Estrogen Receptor/ERR (1)

GABA Receptor (4)

Galectin (1)

GCGR (2)

GPR35 (1)

HCN Channel (1)

Histamine Receptor (5)

HIV (3)

iGluR (2)

Influenza Virus (1)

Integrin (1)

Interleukin Related (1)

Isotope-Labeled Compounds (2)

Ligands for Target Protein for PROTAC (1)

mAChR (10)

mGluR (19)

MicroRNA (1)

mTOR (1)

Neurokinin Receptor (2)

Neuropeptide Y Receptor (1)

Neurotensin Receptor (1)

Opioid Receptor (2)

Orphan GPCR (1)

P2X Receptor (7)

P2Y Receptor (2)

PERK (1)

PI3K (1)

PPAR (2)

Prostaglandin Receptor (1)

Protease Activated Receptor (PAR) (1)

Protein Arginine Deiminase (1)

Reference Standards (7)

SARS-CoV (1)

Src (1)

Taste Receptor (1)

TGF-beta/Smad (1)

Topoisomerase (1)

TSH Receptor (1)

By Research Areas:

Cancer (24)

Cardiovascular Disease (5)

Endocrinology (9)

Infection (8)

Inflammation/Immunology (28)

Metabolic Disease (8)

Neurological Disease (44)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10046

Plerixafor Maximum Cited Publications 102 Publications Verification AMD 3100; JM3100; SID791	CXCR HIV	Infection Inflammation/Immunology Endocrinology Cancer
Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC₅₀ of 1-10 nM .

HY-13848

Rugocrixan 20+ Cited Publications AZD8797; KAND567	CX3CR1 CXCR	Inflammation/Immunology Endocrinology Cancer
AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with K_is of 3.9 and 2800 nM, respectively .

HY-10198

Navarixin 30+ Cited Publications SCH 527123; MK-7123	CXCR	Inflammation/Immunology Endocrinology Cancer
Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with K_d values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly .

HY-19904

Adomeglivant 4 Publications Verification LY2409021	GCGR	Metabolic Disease
Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus .

HY-111052

AZD7325	GABA Receptor Cytochrome P450	Neurological Disease Inflammation/Immunology
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (K_i=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.

HY-B0520A

Benztropine mesylate 5 Publications Verification Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate	Dopamine Receptor mAChR Histamine Receptor	Infection Neurological Disease Metabolic Disease Cancer
Benztropine mesylate (Benzatropine mesylate) is an orally active and BBB-permeable centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D₂ dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

HY-156815

YL-365	Orphan GPCR	Neurological Disease Inflammation/Immunology
YL-365 is a potent and selective GPR34 antagonist with an IC₅₀ of 17 nM. YL-365 binds to a portion of the orthosteric binding pocket of GPR34 and induces allosteric changes that stabilize the receptor in an inactive conformation. YL-365 down-regulates expression of the proinflammatory gene iNOS in M1 microglia and suppresses proinflammatory responses. YL-365 reduces mechanical allodynia in a dose-dependent manner in a mouse model of neuropathic pain. YL-365 can be used for the research of neuropathic pain .

HY-123617

AZ8838	Protease Activated Receptor (PAR)	Inflammation/Immunology
AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pK_i of 6.4 for hPAR2 .

HY-13831

BPTU 1 Publications Verification BMS-646786	P2Y Receptor	Neurological Disease Cancer
BPTU (BMS-646786) is a non-nucleotide P2Y₁ receptor allosteric antagonist with antithrombotic activity. BPTU is able to block the P2Y1 receptor located at the neuromuscular junction of the gastrointestinal tract .

HY-50688

SB-265610 5+ Cited Publications	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-15445

CTEP 2 Publications Verification RO 4956371; mGluR5 inhibitor	mGluR	Neurological Disease
CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC₅₀ of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors. CTEP 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-122575

Aurintricarboxylic acid 3 Publications Verification	P2X Receptor Influenza Virus Topoisomerase MicroRNA Apoptosis	Infection Neurological Disease Inflammation/Immunology
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC₅₀s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively . Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase . Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis . Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway . Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC₅₀ of 0.6 μM . Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC₅₀ of 0.47 µM .

HY-133073

CCR7 Ligand 1 3 Publications Verification CCR7-Cmp2105	CCR Ligands for Target Protein for PROTAC	Cancer
CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a K_d of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC₅₀ of 7.3 μM .

HY-19519A

Ladarixin sodium 1 Publications Verification DF 2156A	CXCR	Infection Inflammation/Immunology Cancer
Ladarixin sodium (DF 2156A) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin sodium can be used for the research of COPD and asthma .

HY-19519

Ladarixin 1 Publications Verification DF 2156A free base	CXCR	Inflammation/Immunology Cancer
Ladarixin (DF 2156A free base) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin can be used for the research of COPD and asthma .

HY-119217

AZ084 2 Publications Verification	CCR	Inflammation/Immunology Endocrinology Cancer
AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a K_i of 0.9 nM. Has potential to treat asthma . AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer .

HY-103111

MMPIP hydrochloride	mGluR	Neurological Disease
MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (K_B values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice .

HY-176710

PAD-PF2	Protein Arginine Deiminase Opioid Receptor mAChR	Neurological Disease Inflammation/Immunology Cancer
PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC₅₀ = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC₅₀ = 12.3 μM). The IC₅₀ values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca ²⁺-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer .

HY-139202

XVA143	Integrin	Inflammation/Immunology
XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo .

HY-110237

BX430	P2X Receptor Calcium Channel	Cardiovascular Disease
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC₅₀ of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.

HY-153213

Org 274179-0	TSH Receptor	Metabolic Disease
Org 274179-0 is a potent and allosteric antagonist of thyroid-stimulating hormone (TSH) receptor, with an IC₅₀ of nanomolar concentration. Org 274179-0 completely inhibits TSH (and TSI)-mediated TSH receptor activation with little effect on the potency of TSH. Org 274179-0 can be used for the research of Graves' disease (GD) .

HY-112247

SR 16832	PPAR TGF-beta/Smad	Metabolic Disease Inflammation/Immunology
SR 16832 is a dual-site covalent, orthosteric and allosteric PPARγ antagonist. SR 16832 activates the TGF-β signaling pathway and upregulates the expression of Vimentin and Fibronectin (Fibronectin). SR 16832 is toxic to bronchial epithelium. SR 16832 can be used in research related to type 2 diabetes and pulmonary fibrosis .

HY-B0520

Benztropine 5 Publications Verification Benzatropine; Benzotropine	Dopamine Receptor mAChR Histamine Receptor	Cancer
Benztropine (Benzatropine; Benzotropine) is an orally active and BBB-permeable centrally acting anticholinergic agent that can be used for Parkinson's disease research . Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine is also a human D₂ dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

HY-16639

ML314	GPR35 Neurotensin Receptor	Neurological Disease Endocrinology
ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC₅₀ = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions .

HY-11095

NPS 2390	mGluR CaSR PI3K Akt mTOR Autophagy Apoptosis Bcl-2 Family Caspase	Cardiovascular Disease Neurological Disease
NPS 2390 is an allosteric antagonist of calcium-sensing receptor (CaSR) and mGluR1/5. NPS 2390 inhibits the PI3K/Akt/mTOR signaling pathway, reduces hypoxia-induced intracellular calcium elevation, decreases the expression of autophagy (autophagy) proteins, regulates the expression of phenotypic marker proteins, and inhibits the proliferation of pulmonary artery smooth muscle cells. NPS 2390 attenuates the endogenous apoptosis (apoptosis) pathway, increases the expression level of Bcl-2, downregulates the expression levels of Bax, cytochrome c and caspase-3, alleviates cerebral edema and improves neurological function in rat models. NPS 2390 can be used in studies related to hypoxic pulmonary hypertension, traumatic brain injury, stroke and pain .

HY-145684

EP2 receptor antagonist-1	Prostaglandin Receptor	Inflammation/Immunology
EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects .

HY-129946

Dopamine D2 receptor antagonist-1	Dopamine Receptor	Neurological Disease
Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity .

HY-50081

CCR2-RA-[R] 4 Publications Verification	CCR	Inflammation/Immunology Endocrinology
CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC₅₀ of 103 nM.

HY-100405

FTIDC	mGluR	Neurological Disease
FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC₅₀ of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1 .

HY-100588

VU0364770	mGluR	Neurological Disease
VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC₅₀s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with K_i values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .

HY-178121

JNJ-78911118	iGluR	Neurological Disease Inflammation/Immunology
JNJ-78911118 is a potent, brain-penetrant, selective GluN2A antagonist (IC₅₀ = 44 nM). JNJ-78911118 shows >200-fold selectivity against GluN1/2B, 2C and 2D receptors. JNJ-78911118 functions as a negative allosteric modulator (NAM) by insurmountably suppressing glutamate efficacy and reducing glycine potency at GluN1/2A receptors. JNJ-78911118 produces profound pharmacodynamic effects in vivo. JNJ-78911118 can be used for depression research .

HY-118967

VUANT1 VU0183254	HCN Channel	Others
VUANT1 (VU0183254) is an allosteric antagonist of insect odorant receptor ion channels, which has the activity of inhibiting insect odorant receptor signaling. VUANT1 can inhibit the activation of insect odorant receptors through allosteric regulation, which is important for the study of the molecular mechanism of insect olfactory signaling. Although it may be of limited use in insect control programs, it can be used as a pharmacological tool to study related mechanisms.

HY-107503

MMPIP	mGluR	Neurological Disease
MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (K_B values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice .

HY-N8852

6-Methoxyflavanone 6-MeOF	GABA Receptor Taste Receptor	Neurological Disease Metabolic Disease
6-Methoxyflavanone (6-MeOF) is a flavonoid compound that can cross the blood-brain barrier. 6-Methoxyflavanone is a positive allosteric modulator of GABA_A receptors. 6-Methoxyflavanone exhibits positive allosteric regulatory effects on human recombinant α1β2γ2L and α2β2γ2L GABA_A receptors, and is relatively inactive on the α1β2 GABA_A receptor. 6-Methoxyflavanone showes inhibitory behavior towards the activation of bitter receptor hTAS2R39 and hTAS2R14, demonstrating a reversible and non-overcome antagonistic effect. 6-Methoxyflavanone has the effects of anti-anxiety, analgesia and relief of neuropathic pain .

HY-112874

BMS-681 BMS-687681	CCR	Neurological Disease Inflammation/Immunology Cancer
BMS-681 is an orthosteric antagonist of CC chemokine receptor 2 (CCR2). BMS-681 restricts the movement of the extracellular end of TM6 by stabilizing TM7. TM7 and TM6 are the main components of the orthosteric binding site. BMS-681 can be used to study inflammatory neurodegenerative diseases and cancer .

HY-110152

LSN2463359	mGluR	Neurological Disease
LSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu₅). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model . LSN2463359 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-165125

(S)-VU0637120	Neuropeptide Y Receptor	Metabolic Disease
(S)-VU0637120 is a Y4R antagonist that effectively reduces the binding response of its endogenous ligand, pancreatic polypeptide (PP), on Y4R, with an IC₅₀ value of 2.7 μM. (S)-VU0637120 binds to the allosteric site of Y4R, which is located in the core region of the Y4R transmembrane structure, near the binding pocket of pancreatic polypeptide (PP), with a K_B value of 300-400 nM. (S)-VU0637120 holds potential for research in the field of metabolic diseases .

HY-121094

*Androgen receptor allosteric* antagonist 1**	Estrogen Receptor/ERR	Cancer
Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the K_i of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer .

HY-133555

mGluR2 antagonist 1	mGluR	Neurological Disease
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC₅₀ of 9 nM) with excellent brain permeability .

HY-10046S

Plerixafor-d4	Isotope-Labeled Compounds CXCR HIV	Infection Inflammation/Immunology Endocrinology Cancer
Plerixafor-d₄ is the deuterium labeled Plerixafor. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC₅₀ of 1-10 nM .

HY-15469

GW791343 dihydrochloride 1 Publications Verification	P2X Receptor	Neurological Disease
GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC₅₀ of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease .

HY-175504

MLS6357	Dopamine Receptor PERK	Neurological Disease
MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC₅₀s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC₅₀ > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC₅₀ of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder .

HY-176980

CCR6 antagonist 4	CCR	Inflammation/Immunology
CCR6 antagonist 4 (compound OXM1) is a potent and selective CC chemokine receptor 6 (CCR6) allosteric antagonist (IC₅₀ = 158 nM). CCR6 antagonist 4 binds to an extracellular pocket and disrupts the receptor activation network. CCR6 antagonist 4 can be used for chronic inflammatory diseases research .

HY-176979

CCR6 antagonist 3	CCR	Inflammation/Immunology
CCR6 antagonist 3 (compound OXM2) is a potent and selective CC chemokine receptor 6 (CCR6) allosteric antagonist (IC₅₀ = 166 nM). CCR6 antagonist 3 binds to an extracellular pocket and disrupts the receptor activation network. CCR6 antagonist 3 can be used for chronic inflammatory diseases research .

HY-100979

W-84 dibromide HDMPPA	mAChR	Others
W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [ ³H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine .

HY-110179

PSNCBAM-1	Cannabinoid Receptor	Metabolic Disease
PSNCBAM-1 is a selective CB1 receptor allosteric antagonist with an EC₅₀ of 0.1 μM. PSNCBAM-1 can be used in the researches of obesity .

HY-118238

Remeglurant MRZ-8456	mGluR	Neurological Disease
Remeglurant (MRZ-8456) acts as a selective, orally active and allosteric antagonist of the mGlu5 receptor, with an IC₅₀ of 13 nM. Remeglurant (MRZ-8456) can be used in the research for dyskinesia in Parkinson’s disease (PD) .

HY-118356

WIN 62,577	Neurokinin Receptor mAChR	Neurological Disease
WIN 62,577 is a rat-specific, but non-human, NK1 receptor antagonist. WIN 62,577 interacts with M1-M4 mAChRs and is an allosteric enhancer of acetylcholine affinity targeting the M3 receptor.

HY-10046R

Plerixafor (Standard) AMD 3100 (Standard); JM3100 (Standard); SID791 (Standard)	Reference Standards CXCR HIV	Infection Inflammation/Immunology Endocrinology Cancer
Plerixafor (Standard) is the analytical standard of Plerixafor. This product is intended for research and analytical applications. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC₅₀ of 1-10 nM .

HY-15470

GW791343 trihydrochloride	P2X Receptor	Neurological Disease
GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC₅₀ of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease .

Cat. No.	Product Name	Target	Research Area

HY-P10010

DB21, Galectin-1 Antagonist	Galectin	Cancer
DB21, Galectin-1 Antagonist is a dibenzofuran conjugated peptidomimetic that acts as an allosteric inhibitor of galectin-1 (GAL1)binding to cell surface glycans. DB21, Galectin-1 Antagonis increases inhibition of angiogenesis and tumour growth in melanoma, lung adenocarcinoma and ovarian cancer models .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N18260

Desmodilactone	Structural Classification Grona styracifolia (Osbeck) H. Ohashi & K. Ohashi Ketones, Aldehydes, Acids Plants Fabaceae Source Classification	P2Y Receptor
Desmodilactone is a P2Y1R allosteric antagonist. Desmodilactone can be used for the research of thrombosis .

Cat. No.	Product Name	Chemical Structure

HY-10046S

Plerixafor-d4
Plerixafor-d₄ is the deuterium labeled Plerixafor. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC₅₀ of 1-10 nM .

HY-B0520AS1

Benztropine-d3 mesylate

Benztropine-d₃ (mesylate) is the deuterium labeled Benztropine mesylate . Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

HY-B0520AS

Benztropine-13C,d3 mesylate

Benztropine- ¹³C,d₃ (mesylate) is the ¹³C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks