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Results for "

allosteric+agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Amino Acid Derivatives (1) Amyloid-β (2) Apoptosis (1) Bacterial (1) Bombesin Receptor (2) CaSR (7) Cholinesterase (ChE) (1) CXCR (5) Dopamine Receptor (1) Drug Derivative (1) Drug Intermediate (1) Drug Metabolite (1) Endogenous Metabolite (8) ERK (1) Estrogen Receptor/ERR (2) Free Fatty Acid Receptor (2) G protein-coupled Bile Acid Receptor 1 (1) GPR65 (1) GPR84 (1) HIV (3) HSV (1) Isotope-Labeled Compounds (4) mAChR (13) MARCKS (2) mGluR (2) nAChR (1) PANK (1) PPAR (1) Proteasome (1) Reference Standards (5) RXFP Receptor (1) Sigma Receptor (1) STING (1) Tau Protein (1) TRP Channel (1) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (14) Cardiovascular Disease (8) Endocrinology (7) Infection (4) Inflammation/Immunology (9) Metabolic Disease (7) Neurological Disease (17)

By Targets:

5-HT Receptor (1)

Amino Acid Derivatives (1)

Amyloid-β (2)

Apoptosis (1)

Bacterial (1)

Bombesin Receptor (2)

CaSR (7)

Cholinesterase (ChE) (1)

CXCR (5)

Dopamine Receptor (1)

Drug Derivative (1)

Drug Intermediate (1)

Drug Metabolite (1)

Endogenous Metabolite (8)

ERK (1)

Estrogen Receptor/ERR (2)

Free Fatty Acid Receptor (2)

G protein-coupled Bile Acid Receptor 1 (1)

GPR65 (1)

GPR84 (1)

HIV (3)

HSV (1)

Isotope-Labeled Compounds (4)

mAChR (13)

MARCKS (2)

mGluR (2)

nAChR (1)

PANK (1)

PPAR (1)

Proteasome (1)

Reference Standards (5)

RXFP Receptor (1)

Sigma Receptor (1)

STING (1)

Tau Protein (1)

TRP Channel (1)

Wnt (1)

β-catenin (1)

By Research Areas:

Cancer (14)

Cardiovascular Disease (8)

Endocrinology (7)

Infection (4)

Inflammation/Immunology (9)

Metabolic Disease (7)

Neurological Disease (17)

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-70037

Cinacalcet 15+ Cited Publications AMG 073	CaSR Endogenous Metabolite	Cardiovascular Disease Cancer
Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease research.

HY-70037A

Cinacalcet hydrochloride 15+ Cited Publications AMG-073 hydrochloride	CaSR Endogenous Metabolite	Cardiovascular Disease Cancer
Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.

HY-P0172

ATI-2341 4 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

HY-128770

LY3154207 2 Publications Verification	Dopamine Receptor	Neurological Disease
LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC₅₀=3 nM) .

HY-112606

ML-290	RXFP Receptor	Others
ML-290 is a first-in-class and potent relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes, with an EC₅₀ of 94 nM . ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.

HY-14342

MK-5046 2 Publications Verification	Bombesin Receptor	Metabolic Disease
MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC₅₀ and an EC₅₀ value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity .

HY-19752A

VU0357017 hydrochloride CID-25010775	mAChR	Neurological Disease
VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M₁ muscarinic acetylcholine receptor, with an EC₅₀ of 477 nM. VU0357017 hydrochloride is highly selective for M₁ and has no activity at M₂-M₅ up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia .

HY-P0172A

ATI-2341 TFA 4 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

HY-107111

GSK1034702	mAChR	Neurological Disease
GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC₅₀=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .

HY-114011

AMG7703	Free Fatty Acid Receptor	Metabolic Disease Inflammation/Immunology
AMG7703 is a selective and allosteric agonists of FFA2 (GPR43), the receptor for short-chain fatty acids (SCFAs), acetate, and propionate. AMG7703 can be used to research for in inflammatory and metabolic .

HY-117163

FzM1.8 1 Publications Verification	Wnt β-catenin	Cancer
FzM1.8, derives from FzM1, is an allosteric agonist of FZD4 with pEC₅₀ of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K .

HY-160857

TOP5668	Estrogen Receptor/ERR	Endocrinology
TOP5668 is an orally active follicle-stimulating hormone receptor allosteric agonist. TOP5668 can induce the production of testosterone in stromal cells and promote follicular genesis and superovulation in rats .

HY-153615

CVN636	mGluR	Neurological Disease
CVN636 is a potent, orally active and selective mGluR7 allosteric agonist with an EC₅₀ value of 7 nM for hu mGluR7. CVN636 has central nervous system (CNS) permeability .

HY-14562

TBPB	mAChR Amyloid-β	Neurological Disease Inflammation/Immunology
TBPB (tert-butyl peroxybenzoate) is a highly selective, blood-brain-permeable M1 mAChR allosteric agonist (EC₅₀=289 nM) with anti-schizophrenia and anti-inflammatory activities. TBPB can enhance the sensitivity of M1 receptors to acetylcholine, activate downstream signaling pathways, and inhibit the release of pro-inflammatory cytokines (TNF-α, IL-6). TBPB can regulate the processing of amyloid and can be used in the study of neurodegenerative diseases (such as Alzheimer's disease) and inflammation-related diseases (such as sepsis) .

HY-100336

AC260584 1 Publications Verification	mAChR	Neurological Disease
AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC₅₀ of 7.6.

HY-W101299

*N-Acetyl-D-allo-isoleucine*	Amino Acid Derivatives	Metabolic Disease
N-Acetyl-D-allo-isoleucine is an amino acid derivative. N-Acetyl-D-allo-isoleucine is promising for research of amino acid metabolism, such as abnormal isoleucine metabolism .

HY-113616A

VU0364572 TFA	MARCKS mAChR	Neurological Disease
VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC₅₀ of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant .

HY-116586

AF710B	Sigma Receptor mAChR ERK Amyloid-β Tau Protein	Neurological Disease
AF710B is an orally effective allosteric agonist for the M1 muscarinic receptor and σ1 receptor. AF710B activates the downstream phosphorylated ERK1/2 and phosphorylated CREB signaling pathways. AF710B simultaneously improves cognitive function and alleviates the core pathological features of Alzheimer's disease, including Aβ deposition, excessive Tau phosphorylation and neuroinflammation. AF710B is applicable to the research of Alzheimer's disease .

HY-W193844

MLS001006105 ZINC13684400	GPR65	Inflammation/Immunology
MLS001006105 (ZINC13684400) is a GPR65 allosteric agonist. MLS001006105 displays GPR65 allosteric agonist activity at pH 8.40 but not at lower pH .

HY-110087

4BP-TQS	nAChR	Neurological Disease
4BP-TQS is a potent allosteric agonist of α7 nAChR. 4BP-TQS activates nAChRs via an allosteric transmembrane site .

HY-164909

PZ-3022	PANK	Metabolic Disease
PZ-3022 is an orally active allosteric agonist of pantothenate kinase (PanK) with an EC₅₀ of 5.3 nM against PanK3. PZ-3022 antagonizes the inhibitory effect of C3-CoA. PZ-3022 increases CoA levels in cells and the liver, upregulates CoASH and C2-CoA, downregulates C3-CoA, and restores impaired TCA cycle and mitochondrial function. PZ-3022 can be used for the research of propionic acidemia and metabolic CoA deficiency .

HY-135601

Cinacalcet metabolite M4	Drug Metabolite	Cardiovascular Disease
Cinacalcet metabolite M4 is a metabolite of Cinacalcet. Cinacalcet is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease .

HY-70037AR

Cinacalcet hydrochloride (Standard) AMG-073 hydrochloride (Standard)	Reference Standards CaSR Endogenous Metabolite	Cardiovascular Disease Cancer
Cinacalcet (hydrochloride) (Standard) is the analytical standard of Cinacalcet (hydrochloride). This product is intended for research and analytical applications. Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.

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-118806A

AC-42 hydrochloride	mAChR	Neurological Disease
AC-42 hydrochloride is the hydrochloride salt form of AC-42 (HY-118806). AC-42 hydrochloride is an allosteric agonist for muscarinic M1 receptor with EC₅₀s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 hydrochloride stimulates the inositol phosphate (IP)-accumulation and calcium mobilization in CHO cells .

HY-14342A

(R)-MK-5046	Bombesin Receptor	Metabolic Disease
(R)-MK-5046 is the isomer of MK-5046 (HY-14342), and can be used as an experimental control. MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC₅₀ and an EC₅₀ value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity .

HY-70037AS

Cinacalcet-d3 hydrochloride AMG 073-d₃ hydrochloride	Isotope-Labeled Compounds CaSR Endogenous Metabolite	Cardiovascular Disease
Cinacalcet-d₃ (hydrochloride) is the deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.

HY-160856

TOP5300 TOP05300	Estrogen Receptor/ERR	Endocrinology
TOP5300 is an orally active follicle-stimulating hormone receptor allosteric agonist. TOP5300 can induce the production of testosterone in stromal cells and promote follicular genesis and superovulation in rats .

HY-113616

VU0364572	mAChR MARCKS	Neurological Disease
VU0364572 is a selective allosteric agonist of the M1 muscarinic receptor with an EC₅₀ of 0.11 μM. VU0364572 has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 is orally active and is CNS penetrant .

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-P4910

Baceridin	Proteasome Apoptosis	Cancer
Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research .

HY-121140

AZ1729	Free Fatty Acid Receptor	Metabolic Disease
AZ1729 is a potent free fatty acid 2 receptor (FFA2) activator, acting as a direct allosteric agonist and as a positive allosteric modulator. AZ1729 increases the activity of the endogenously produced short chain fatty acid propionate in G_i-mediated pathways, but not at those transduced by G_q/G₁₁. AZ1729 induces inhibition of isoproterenol-induced lipolysis in mouse adipocytes. AZ1729 also can Induce migration of human neutrophils. AZ1729 can be used for researching the signaling pathways of the physiological roles of FFA2 .

HY-P2120

Pseudobactin A	Bacterial	Others
Pseudobactin A is a non-fluorescent extracellular iron carrier produced by the plant growth-promoting bacterium Pseudomonas B10 .

HY-114589

VU0240382	mGluR	Others
VU0240382 is a metabotropic glutamate receptor subtype 5 modulator whose activity differs depending on whether it has allosteric agonist activity. VU0240382 with allosteric agonist activity can activate mGlu(5) receptors in cell lines, but has no agonist activity in natural systems and has similar efficacy to mGlu(5) modulators without allosteric agonist activity in animal models.

HY-70037S

Cinacalcet-d3 AMG 073-d₃	Isotope-Labeled Compounds CaSR Endogenous Metabolite	Cardiovascular Disease
Cinacalcet-d₃ is the deuterium labeled Cinacalcet. Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.

HY-70037R

Cinacalcet (Standard) AMG 073 (Standard)	CaSR Endogenous Metabolite Reference Standards	Cardiovascular Disease Cancer
Cinacalcet (Standard) is the analytical standard of Cinacalcet. This product is intended for research and analytical applications. Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease research.

HY-119806

TMPPAA	5-HT Receptor	Neurological Disease
TMPPAA is an allosteric agonist and positive allosteric modulator of the 5-HT3 receptor. TMPPAA enhances 5-HT-mediated 5-HT3AR signaling .

HY-W653978

Cinacalcet-d4 hydrochloride AMG-073-d4 hydrochloride	Isotope-Labeled Compounds CaSR Endogenous Metabolite	Cardiovascular Disease Cancer
Cinacalcet-d₄ (AMG-073-d₄) hydrochlorideis deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment .

HY-118806

AC-42	mAChR	Neurological Disease
AC-42 is a poent M1 muscarinic selective allosteric agonist with EC₅₀s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 stimulates the IP-accumulation and calcium mobilization in CHO cells .

HY-19752

VU0357017 CID-25010775 free base	mAChR	Neurological Disease
VU0357017 (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M₁ muscarinic acetylcholine receptor, with an EC₅₀ of 477 nM. VU0357017 is highly selective for M₁ and has no activity at M₂-M₅ up to the highest concentrations tested (30 μM). VU0357017 can be used for the research of Alzheimer’s disease and schizophrenia .

HY-107111A

GSK1034702 hydrochloride	Cholinesterase (ChE) mAChR	Neurological Disease
GSK1034702 hydrochloride is an orally active and allosteric agonist of M1 mAChR (pEC₅₀=8.1) that can cross the blood-brain barrier. GSK1034702 hydrochloride activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 hydrochloride can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 hydrochloride can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .

HY-100336R

AC260584 (Standard)	mAChR Reference Standards	Neurological Disease
AC260584 (Standard) is the analytical standard of AC260584 (HY-100336). This product is intended for research and analytical applications. AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.

HY-180674

LA24	STING	Inflammation/Immunology
LA24 is a potent STING allosteric agonist, with an EC₅₀ of 0.82 μM. LA24 induces the phosphorylation of STING and IRF3. LA24 can be used for the study of STING-targeted immunotherapies .

HY-P4613

*Fmoc-D-allo-Thr-OH*	Drug Derivative Drug Intermediate	Others
Fmoc-D-allo-Thr-OH is a derivative of D-allothreonine (HY-W001959), which is commonly used as a building block in solid-phase peptide synthesis (SPPS) .

HY-P11022

TL-119 A-3302-B	Endogenous Metabolite HSV TRP Channel	Infection Cancer
TL-119 (A-3302-B) is a polypeptide. TL-119 can be isolated from the bacteria Micromonospora sp. MAG 9-7 and Saccharomonospora sp. CNQ-490. TL-119 inhibits TRPV-1. TL-119 exhibits antiviral activity against HSV-2. TL-119 possesses anticancer activity against gastric cancer and colorectal cancer .

HY-182723

PSB-16671	GPR84	Cancer
PSB-16671 is an allosteric agonist of GPR84. PSB-16671 recruits β-arrestins and couples to Gi, enhances the Gi activation potency of orthosteric agonists, and exerts a synergistic effect with orthosteric agonists. PSB-16671 promotes G protein activation and partial chemotaxis independent of GPR84 in mouse neutrophils, maintains the phagocytic function of macrophages against cancer cells without inducing receptor desensitization. PSB-16671 can be used in cancer-related research .

HY-122222

MRL20	PPAR	Others
MRL20 is a PPARγ constitutive and allosteric agonist. MRL20 enhances the interaction between PPARγ and the co-activating peptide of TRAP220, with its EC₅₀ being 10 nM. Even after being covalently blocked in the constitutive pocket by GW9662 (HY-16578) or T0070907 (HY-13202), MRL20 can still strengthen the interaction between PPARγ and TRAP220, with EC₅₀ values of 176 and 440 nM respectively. MRL20 fails to completely inhibit its cell activation effect. MRL20 can be used to study the allosteric regulatory mechanism of PPARγ .

HY-180845

*TGR5 agonist* 9**	G protein-coupled Bile Acid Receptor 1	Metabolic Disease
TGR5 agonist 9 is a highly selective and orally active TGR5 allosteric agonist with EC₅₀ values for hTGR5 and mTGR5 of 0.48 and 0.49 μM, respectively. TGR5 agonist 9 can recruit β-arrestin 1 (EC₅₀ = 78.8 μM) and β-arrestin 2 (EC₅₀ = 12.3 μM), and has a higher efficacy in cAMP accumulation (EC₅₀ = 0.48 μM). TGR5 agonist 9 exhibits a significant hypoglycemic effect in the ICR mouse model. TGR5 agonist 9 can be used for research on diabetes .

HY-107111R

GSK1034702 (Standard)	Reference Standards mAChR	Neurological Disease
GSK1034702 (Standard) is the analytical standard of GSK1034702 (HY-107111). This product is intended for research and analytical applications. GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC₅₀=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .

Cat. No.	Product Name	Target	Research Area