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Results for "

functional selectivity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (4) ADAMTS (1) ADC Linker (2) Angiotensin Receptor (1) Arrestin (2) Biochemical Assay Reagents (1) Cannabinoid Receptor (2) Caspase (1) CCR (2) CDK (1) Cholinesterase (ChE) (2) CRAC Channel (2) CXCR (2) Dopamine Receptor (4) EGFR (1) Epigenetic Reader Domain (1) Fluorescent Dye (2) GABA Receptor (2) GHSR (3) Glucocorticoid Receptor (1) GPR84 (1) GPR88 (2) Histamine Receptor (3) HIV (1) Interleukin Related (3) mAChR (2) mGluR (1) nAChR (1) NOD-like Receptor (NLR) (1) P2X Receptor (2) Prostaglandin Receptor (1) Sigma Receptor (1)
By Research Areas:	Cancer (8) Cardiovascular Disease (2) Endocrinology (3) Infection (1) Inflammation/Immunology (14) Metabolic Disease (8) Neurological Disease (15)
Click Chemistry:	TCO (2) Labeling and Fluorescence Imaging (2) Alkynes (1)

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-148258

GDC-2394	NOD-like Receptor (NLR) Interleukin Related Caspase	Inflammation/Immunology
GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC₅₀s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation .

HY-103475

GS39783	GABA Receptor	Neurological Disease
GS39783 is a positive allosteric modulator (PAM) of GABA_BR. Positive modulation of the GABA_BR can be used for the research of Nicotine addiction .

HY-110132

JNJ-27141491

CCR Inflammation/Immunology

JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2 .
HY-161105

FPIP

5-HT Receptor Others

FPIP is a selectivity agonist of 5-HT1A with a functional potency (pEC₅₀=8.92) .
HY-112426

LAU159

GABA Receptor Neurological Disease

LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC₅₀ of 2.2 μM .

JNJ-27141491	CCR	Inflammation/Immunology
JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2 .

FPIP	5-HT Receptor	Others
FPIP is a *selectivity* agonist of 5-HT1A with a functional potency (pEC₅₀=8.92) .

LAU159	GABA Receptor	Neurological Disease
LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC₅₀ of 2.2 μM .

HY-14900

Tedalinab GRC-10693	Cannabinoid Receptor	Inflammation/Immunology
Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment .

HY-16996A

BD-1047 dihydrobromide 5 Publications Verification	Sigma Receptor	Neurological Disease
BD-1047 (dihydrobromide) is a selective functional antagonist of sigma-1 receptor, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia .

HY-101336

RS 17053 hydrochloride RS-17053
RS 17053 hydrochloride is a potent and selective α1_A adrenoceptor antagonist, with a pK_i value of 9.1 in native cell membrane and a pA₂ value of 9.8 in functional assays.

HY-126346

DL-175	GPR84	Inflammation/Immunology
DL-175 (compound 13) is a selective GPR84 agonist with biased agonistic activity. DL-175 can selectively activate functional responses in immune cells and induce enhanced chemotaxis and phagocytosis of human bone marrow cells. DL-175 is a potential chemical probe .

HY-106432A

Sabcomeline hydrochloride SB-202026 hydrochloride; Memric hydrochloride	mAChR	Neurological Disease
Sabcomeline (SB-202026) hydrochloride is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline hydrochloride can be used for Alzheimer's disease research .

HY-106432

Sabcomeline SB-202026; Memric	mAChR	Neurological Disease
Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research .

HY-18760

LY2812223	mGluR	Neurological Disease
LY2812223 is a highly potent, functionally selective mGlu₂ receptor agonist with mGlu₂ binding affinity for mGlu₂ and mGlu₃ (K_i=144 nM and 156 nM, respectively) .

HY-10013

Taranabant 1 Publications Verification MK-0364	Cannabinoid Receptor	Metabolic Disease
Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding K_i of 0.13 nM for the human CB1R in vitro.

HY-151682

H-L-Lys(Norbornene-methoxycarbonyl)-OH	ADC Linker	Others
H-L-Lys(Norbornene-methoxycarbonyl)-OH, a norbornene-derivatized lysine, can be click-functionalized. H-L-Lys(Norbornene-methoxycarbonyl)-OH can be used for the mild and selective modification of proteins in a copper-free click reaction .

HY-151682A

H-L-Lys(Norbornene-methoxycarbonyl)-OH hydrochloride	ADC Linker	Others
H-L-Lys(Norbornene-methoxycarbonyl)-OH hydrochloride, a norbornene-derivatized lysine, can be click-functionalized. H-L-Lys(Norbornene-methoxycarbonyl)-OH hydrochloride can be used for the mild and selective modification of proteins in a copper-free click reaction .

HY-112612

RTI-13951-33	GPR88	Neurological Disease
RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC₅₀ of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 reduces alcohol reinforcement and intake behaviors in rats .

HY-112612A

RTI-13951-33 hydrochloride 1 Publications Verification	GPR88	Neurological Disease
RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, with an EC₅₀ of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 hydrochloride reduces alcohol reinforcement and intake behaviors in rats .

HY-114231

Exaluren ELX-02; NB-124	Others	Others
Exaluren (ELX-02) is an synthetic eukaryotic ribosome-selective glycoside that induces read through of nonsense mutations, resulting in normally localized full-length functional proteins. Exaluren is used for the research of cystic fibrosis caused by nonsense mutations .

HY-125096

C108297	Glucocorticoid Receptor	Metabolic Disease Inflammation/Immunology
C108297 is a selective glucocorticoid receptor (GR) modulator (GR binding K_i 0.7 nM; GR reporter gene functional K_i 0.6 nM). C108297 attenuates obesity by reducing caloric intake and increasing lipolysis and fat oxidation, and in addition attenuates inflammation .

HY-114996

ADAMTS-5 Inhibitor 3 Publications Verification	ADAMTS	Inflammation/Immunology
ADAMTS-5 Inhibitor is a potent ADAMTS-5 (aggrecanase-2) inhibitor, with an IC₅₀ of 1.1 µM. ADAMTS-5 Inhibitor shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1) .

HY-103416

A-77636 hydrochloride 1 Publications Verification	Dopamine Receptor	Neurological Disease
A-77636 hydrochloride is a potent, orally active, selective and long acting dopamine D1 receptor agonist (pK_i=7.40; K_i=39.8 nM) with antiparkinsonian activity. A-77636 hydrochloride is functionally inactive at dopamine D2 receptor .

HY-111385

UNC9994 hydrochloride 1 Publications Verification	Dopamine Receptor 5-HT Receptor Arrestin	Neurological Disease
UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D₂ receptor (D₂R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a K_i of 79 nM for D₂R. UNC9994 hydrochloride is also an antagonist of G_i-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity .

HY-121467A

Acotiamide hydrochloride Z-338; YM443	Cholinesterase (ChE)	Others Metabolic Disease Inflammation/Immunology
Acotiamide hydrochloride is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC₅₀ of 1.79 μM. Acotiamide hydrochloride can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide hydrochloride has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .

HY-121467

Acotiamide Z-338 free base; YM443 free base	Cholinesterase (ChE)	Metabolic Disease Inflammation/Immunology
Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC₅₀ of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .

HY-19618

BRD3308
BRD3308 is a highly selective HDAC3 inhibitor with an IC₅₀ of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC₅₀ of 1.26 μM) or HDAC2 (IC₅₀ of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency .

HY-D0976

NF279	P2X Receptor HIV	Infection
NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC₅₀ of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC₅₀=1.62 μM), P2X4 (IC₅₀>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env .

HY-115487

MF-766	Prostaglandin Receptor	Inflammation/Immunology Cancer
MF-766 is a highly potent, selective and orally active EP4 antagonist with a K_i of 0.23 nM. MF-766 behaves as a full antagonist with an IC₅₀ of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay. MF-766 can be used for cancer and inflammation diseases research .

HY-18664

PFI-4 1 Publications Verification	Epigenetic Reader Domain	Cancer
PFI-4 (compound 11) is a potent and highly selective BRPF1 Bromodomain (BRPF1B) inhibitor, with an IC₅₀ of 172 nM. PFI-4 can be used to explore the functional mechanisms of the HBO1/BRPF1 complex and to study bone loss and osteolytic malignant bone lesions .

HY-B2155

Acotiamide monohydrochloride trihydrate
Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC₅₀ of 1.79 μM. Acotiamide monohydrochloride trihydrate can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide monohydrochloride trihydrate has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .

HY-126220

KMG-301AM	Fluorescent Dye	Others
KMG-301AM is the acetoxy methyl esterified form of KMG-301. KMG-301AM successfully accumulates in mitochondria and then it is hydrolyzed to KMG-301. KMG-301 is an Mg ²⁺-selective fluorescent probe functional in mitochondria in intact cells. Since the mitochondrial membrane is impermeable to KMG-301, it is not released upon depolarization of the mitochondrial membrane potential. KMG-301 can indicate changes in mitochondrial Mg2+ concentration and shows Mg ²⁺ transport across the mitochondrial membrane in the early phases of a cellular model .

HY-14495

BMS-604992 EX-1314	GHSR	Metabolic Disease
BMS-604992 (EX-1314) is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 demonstrates high-affinity binding (K_i=2.3 nM) and potent functional activity (EC₅₀=0.4 nM). BMS-604992 can stimulate food intake in rodents .

HY-14495B

BMS-604992 dihydrochloride EX-1314 dihydrochloride	GHSR	Metabolic Disease
BMS-604992 (EX-1314) dihydrochloride is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 dihydrochloride demonstrates high-affinity binding (k_i=2.3 nM) and potent functional activity (EC₅₀=0.4 nM). BMS-604992 dihydrochloride can stimulate food intake in rodents .

HY-13499

JNJ-41443532 CCR2 antagonist 5	CCR	Inflammation/Immunology
JNJ-41443532 (CCR2 antagonist 5) is a selective, orally active hCCR2 inhibitor with good binding affinity (IC₅₀=37 nM) and potent functional antagonism (chemotaxis IC₅₀=30 nM). JNJ-41443532 displays a K_i of 9.6 µM for mCCR2 binding. JNJ-41443532 can be used in the research of inflammatory disease .

HY-126220A

KMG-301AM TFA	Fluorescent Dye	Others
KMG-301AM TFA is the acetoxy methyl esterified form of KMG-301. KMG-301AM TFA successfully accumulates in mitochondria and then it is hydrolyzed to KMG-301. KMG-301 is an Mg ²⁺-selective fluorescent probe functional in mitochondria in intact cells. Since the mitochondrial membrane is impermeable to KMG-301, it is not released upon depolarization of the mitochondrial membrane potential. KMG-301 can indicate changes in mitochondrial Mg2+ concentration and shows Mg ²⁺ transport across the mitochondrial membrane in the early phases of a cellular model .

HY-14348

GSK163090	5-HT Receptor Dopamine Receptor	Neurological Disease
GSK163090 is a potent, selective and orally active 5-HT_1A/1B/1D receptor antagonist with pK_i values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pK_i value of 6.1. GSK163090 has antidepressant and anxiolytic activities .

HY-117829

UNC9994	Dopamine Receptor 5-HT Receptor Histamine Receptor Arrestin	Neurological Disease
UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC₅₀ <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of G_i-regulated cAMP production. Antipsychotic Activity .

HY-14495A

BMS-604992 free base EX-1314 free base	GHSR	Metabolic Disease
BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 free base demonstrates high-affinity binding (k_i=2.3 nM) and potent functional activity (EC₅₀=0.4 nM). BMS-604992 free base can stimulate food intake in rodents .

HY-112626

CDK12-IN-2	CDK	Cancer
CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC₅₀=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12 .

HY-101189

JNJ-39758979	Histamine Receptor	Neurological Disease Endocrinology
JNJ-39758979 is a selective, orally active, and high-affinity histamine H₄ receptor antagonist with K_is of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H₄ receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .

HY-113618A

RO2959 hydrochloride	CRAC Channel Interleukin Related	Cardiovascular Disease
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC₅₀ of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC₅₀ of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways .

HY-101189B

JNJ-39758979 dihydrochloride	Histamine Receptor	Inflammation/Immunology
JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H₄ receptor antagonist, with K_is of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H₄ receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity .

HY-Y0415

Tetraethylammonium (fluoride) N,N,N-triethylethanaminium (fluoride)
Tetraethylammonium fluoride is an organic compound containing both ammonium and fluorine functional groups. It is commonly used as a reagent in various chemical synthesis applications, especially as a source of fluoride ions for nucleophilic reactions. Tetraethylammonium fluoride has several properties that make it suitable for these applications, including its high solubility in polar solvents and its ability to selectively activate certain chemical bonds. In addition, it is used as a catalyst for organic reactions and as a surfactant in the production of semiconductors and microelectronics.

HY-Y0971

Tetrabutylammonium (fluoride) TBAF	Biochemical Assay Reagents	Others
Tetrabutylammonium fluoride is an organic compound containing both ammonium and fluorine functional groups. It is commonly used as a reagent in various chemical synthesis applications, especially as a source of fluoride ions for nucleophilic reactions. Tetrabutylammonium fluoride has several properties that make it suitable for these applications, including its high solubility in polar solvents and its ability to selectively activate certain chemical bonds. In addition, it can be used as a catalyst for organic reactions and as an electrolyte for batteries.

HY-107678

SEN12333 WAY-317538	nAChR	Neurological Disease
SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K_>i=260 nM) and acts as full agonist in functional Ca ²⁺ flux studies (EC₅₀=1.6 μM). SEN 12333 is used for AD and schizophrenia research .

HY-103441

JNJ28871063 hydrochloride	EGFR	Cancer
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC₅₀ values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .

HY-113618B

RO2959 monohydrochloride	CRAC Channel Interleukin Related	Cardiovascular Disease
RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC₅₀ of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC₅₀ of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways .

HY-123857

JNJ-55308942	P2X Receptor	Neurological Disease Inflammation/Immunology
JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC₅₀=10 nM, K_i=7.1 nM; rP2X7: IC₅₀=15 nM, K_i=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain .

HY-115531

UNC-2170	Others	Cancer
UNC-2170 is a functionally active, fragment-like ligand for 53BP1 (IC₅₀=29 µM; K_d=22 µM). UNC-2170 shows at least 17-fold selectivity for 53BP1 as compared to nine other methyl-lysine (Kme) reader proteins. 53BP1 is a Kme binding protein that plays a central role in DNA Damage Repair (DDR) pathways and is recruited to sites of double-strand breaks (DSB) .

HY-P0172A

ATI-2341 TFA 2 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-P0172

ATI-2341	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) .

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