subtype-selective

By Targets:	5-HT Receptor (1) Adrenergic Receptor (1) Dopamine Receptor (1) Epigenetic Reader Domain (1) GABA Receptor (6) Histone Methyltransferase (1) iGluR (3) Isotope-Labeled Compounds (1) JAK (1) LPL Receptor (1) mAChR (2) mGluR (1) nAChR (1) P2Y Receptor (2) Potassium Channel (3) PPAR (1) PROTACs (1) Sirtuin (3) Sodium Channel (1) Somatostatin Receptor (1) TRP Channel (1)
By Research Areas:	Cancer (6) Endocrinology (1) Inflammation/Immunology (3) Metabolic Disease (5) Neurological Disease (23)
Click Chemistry:	Alkynes (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-108498

L-817818	Somatostatin Receptor	Endocrinology
L-817818 is a potent and subtype-selective agonist of the somatostatin receptor. L-817818 provides a direct approach to defining somatostatin receptor physiological functions

HY-101869

MK-0343

MRK-409
GABA Receptor Neurological Disease

MK0343 (MRK-409) is an orally bioavailable GABA_A receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic .
HY-101640

TPA 023

GABA Receptor Neurological Disease

TPA 023 is a GABAA α2/α3 subtype-selective agonist, with K_i of 0.19-0.41 nM.

MK-0343 MRK-409	GABA Receptor	Neurological Disease
MK0343 (MRK-409) is an orally bioavailable GABA_A receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic .

TPA 023	GABA Receptor	Neurological Disease
TPA 023 is a GABAA α2/α3 subtype-selective agonist, with K_i of 0.19-0.41 nM.

HY-117196

GW 9578	PPAR	Metabolic Disease Inflammation/Immunology
GW9578 is a subtype-selective PPARα agonist (EC₅₀s of 5 and 50 nM for murine and human PPAR-α) with potent lipid-lowering activity .

HY-162117

LBG30300

mGluR Neurological Disease

LBG30300 is a subtype-selective mGlu₂ receptor agonist EC₅₀ 0.6 nM. LBG30300 is blood-brain barrier permeable .
HY-107713

PPDA

iGluR Neurological Disease

PPDA is a subtype-selective NMDA receptor antagonist that preferentially binds to NR2C/NR2D containing receptors .

LBG30300	mGluR	Neurological Disease
LBG30300 is a subtype-selective mGlu₂ receptor agonist EC₅₀ 0.6 nM. LBG30300 is blood-brain barrier permeable .

PPDA	iGluR	Neurological Disease
PPDA is a subtype-selective NMDA receptor antagonist that preferentially binds to NR2C/NR2D containing receptors .

HY-136459

NMDA receptor antagonist 2	iGluR	Neurological Disease
NMDA receptor antagonist 2 is a potent and orally active *NR2B subtype-selective* NMDA antagonist with an IC₅₀ and a K_i** of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease .

HY-15831

L-838417-d9	Isotope-Labeled Compounds GABA Receptor	Neurological Disease
L-838417-d₉ is the deuterium labeled L-838417. L-838417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].

HY-103229

Cl-HIBO	iGluR	Neurological Disease
Cl-HIBO is a highly subtype-selective GluR1/2 agonist (EC₅₀=4.7 and 1.7 μM, respectively). Cl-HIBO is a potent AMPA receptor agonist (IC₅₀=0.22 μM). Cl-HIBO has desensitizing properties .

HY-108592

UCL 2077	Potassium Channel	Neurological Disease
UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC₅₀ = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization . UCL 2077 is also a subtype-selective blocker of the epilepsy associated KCNQ channels .

HY-152227

PROTAC TYK2 degradation agent1	PROTACs JAK	Inflammation/Immunology
PROTAC TYK2 degradation agent1 is a potent and subtype-selective TYK2 degrader. PROTAC TYK2 degradation agent1 has TYK2 degradation activity with DC₅₀ value of 14 nM. PROTAC TYK2 degradation agent1 can be used for the research of autoimmune disease .

HY-151487

CypD-IN-3	Sirtuin	Neurological Disease Metabolic Disease Cancer
CypD-IN-3 is a potent and subtype-selective cyclophilin D (CypD) inhibitor. CypD-IN-3 has CypD affinity with an IC₅₀ value of 0.01 μM. CypD-IN-3 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes .

HY-151488

CypD-IN-4	Sirtuin	Neurological Disease Metabolic Disease Cancer
CypD-IN-4 is a potent and subtype-selective cyclophilin D (CypD) inhibitor. CypD-IN-4 has CypD affinity with an IC₅₀ value of 0.057 μM. CypD-IN-4 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes .

HY-110092

PSB-1114 tetrasodium	P2Y Receptor	Metabolic Disease
PSB-1114 tetrasodium is a potent, enzymatically stable, and subtype-selective P2Y₂ receptor agonist with an EC₅₀ of 134 nM. PSB-1114 tetrasodium displays >50-fold selectivity versus the P2Y₄ (EC₅₀ of 9.3 μM) and P2Y₆ (EC₅₀ of 7.0 μM) receptors .

HY-142723

KCa2 channel modulator 1	Potassium Channel	Neurological Disease
KCa2 channel modulator 1 (compound 2o) is a potent subtype-selective positive modulator of K_Ca2 channel. KCa2 channel modulator 1 potentiates human K_Ca2.3 channels with an EC₅₀ value of 0.19 μM and 0.99 μM on the rat K_Ca2.2 channel subtype .

HY-151489

CypE-IN-1	Sirtuin	Neurological Disease Metabolic Disease Cancer
CypD-IN-1 is a potent and subtype-selective cyclophilin E (CypE) inhibitor. CypD-IN-1 has CypE affinity with IC₅₀ and K_i values of 0.013 μM and 0.072 μM, respectively. CypD-IN-1 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes .

HY-110092A

PSB-1114 triethylamine	P2Y Receptor	Cancer
PSB-1114 triethylamine is a potent, enzymatically stable, and subtype-selective P2Y₂ receptor agonist with an EC₅₀ of 134 nM. PSB-1114 triethylamine displays >50-fold selectivity versus the P2Y₄ (EC₅₀ of 9.3 μM) and P2Y₆ (EC₅₀ of 7.0 μM) receptors .

HY-11048

NS11394 3 Publications Verification	GABA Receptor	Neurological Disease
NS11394 is an orally active and unique subtype-selective GABA_A positive allosteric receptor (PAM), with a K_i of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABA_A-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties .

HY-12439

ML380 1 Publications Verification	mAChR	Neurological Disease
ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC₅₀s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR .

HY-142735

KCa2 channel modulator 2	Potassium Channel	Neurological Disease
KCa2 channel modulator 2 (compound 2q) is a potent subtype-selective positive modulator of K_Ca2 channel. KCa2 channel modulator 2 exhibits similar potency on the rat K_Ca2.2a and human K_Ca2.3 channel subtypes, with EC₅₀s of 0.64 μM and 0.60 μM, respectively

HY-123249

HZ166	GABA Receptor	Neurological Disease
HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 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-18596

SB-215505	5-HT Receptor	Neurological Disease
SB-215505 is a potent and subtype-selective 5-HT_2B receptor antagonist with pK_i values of 8.3, 6.77, 7.66 for 5-HT_2B, 5-HT_2A, 5-HT_2C, respectively . SB-215505 increases wakefulness and motor activity in rats .

HY-13285

Ki16425 Maximum Cited Publications 7 Publications Verification Debio 0719	LPL Receptor	Neurological Disease Cancer
Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with K_is of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK . Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells .

HY-P5158

Conopeptide rho-TIA	Adrenergic Receptor	Others
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α_1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α_1A-Adrenergic Receptor and *α_1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype* and may provide useful information for the development of novel α₁-Adrenergic Receptor subtype-selective drugs** .

HY-103066

Br-PBTC	nAChR	Neurological Disease
Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2，α2β4，α4β2，α4β4，(α4β2)₂α4 and (α4β2)₂β2 EC₅₀ ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit .

HY-120874

PF-06372865	GABA Receptor	Neurological Disease
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABA_A positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABA_A receptors containing α1/α2/α3/α5 subunits (K_is of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy .

HY-N0584A

Anisodamine hydrobromide 6-Hydroxyhyoscyamine hydrobromide	mAChR	Inflammation/Immunology
Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties .

HY-128770

LY3154207 1 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-N0584

Anisodamine 6-Hydroxyhyoscyamine
Anisodamine (6-Hydroxyhyoscyamine), a belladonna alkaloid, is a non-subtype-selective muscarinic, and also a nicotinic cholinoceptor antagonist. Anisodamine employs in traditional Chinese medicine for many ailments, mainly to improve the microcirculation in states of shock, and also in organophosphate poisoning .

HY-133012

GFB-8438	TRP Channel	Neurological Disease
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC₅₀s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model .

HY-126291

GNE-616	Sodium Channel	Neurological Disease
GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (K_i of 0.79 nM and K_d of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM K_d and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively .

HY-12583

A-366 2 Publications Verification	Histone Methyltransferase Epigenetic Reader Domain	Cancer
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC₅₀s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC₅₀=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (K_i=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .

Cat. No.	Product Name

HY-L170

Allosteric Modulators (AMs) Compound Library	174 compounds
An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands. MCE designs a unique collection of 174 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Allosteric Modulators (AMs) Compound Library

174 compounds

An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.

MCE designs a unique collection of 174 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Cat. No.	Product Name	Target	Research Area

HY-P5158

Conopeptide rho-TIA	Adrenergic Receptor	Others
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α_1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α_1A-Adrenergic Receptor and *α_1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype* and may provide useful information for the development of novel α₁-Adrenergic Receptor subtype-selective drugs** .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0584A

Anisodamine hydrobromide 6-Hydroxyhyoscyamine hydrobromide	Alkaloids Pyrrole Alkaloids Classification of Application Fields Anisodus tanguticus (Maxinowicz) Pascher Source classification Plants Solanaceae Disease Research Fields Inflammation/Immunology	mAChR
Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties .

Cat. No.	Product Name	Chemical Structure

HY-15831

L-838417-d9
L-838417-d₉ is the deuterium labeled L-838417. L-838417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].

Cat. No.	Product Name		Classification

HY-123249

HZ166		Alkynes
HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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