GABAA

By Targets:	5-HT Receptor (2) AAK1 (2) Apoptosis (4) Bacterial (2) Calcium Channel (1) Chloride Channel (1) Cholinesterase (ChE) (1) COX (2) Cytochrome P450 (2) DNA/RNA Synthesis (1) Drug Metabolite (2) Dynamin (2) Endogenous Metabolite (25) Fungal (1) GABA Receptor (166) iGluR (2) Interleukin Related (1) Isotope-Labeled Compounds (8) Keap1-Nrf2 (1) Lipoxygenase (1) nAChR (1) NKCC (4) Opioid Receptor (1) Parasite (1) Phosphodiesterase (PDE) (1) Potassium Channel (4) Reactive Oxygen Species (1) RSV (1) Sirtuin (1) Sodium Channel (1) TNF Receptor (1) Virus Protease (1)
By Research Areas:	Cancer (16) Cardiovascular Disease (2) Infection (2) Inflammation/Immunology (10) Metabolic Disease (9) Neurological Disease (158)
Click Chemistry:	Azide (1) Alkynes (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-135482

GABAA receptor agent 2 TFA	GABA Receptor	Neurological Disease
GABAA receptor agent 2 TFA is a potent and high-affinity GABA_A receptor antagonist with an IC₅₀ of 24 nM (human α1β2γ2 GABA_A-expressing tsA201 cells) and a K_i of 28 nM (*rat GABA_A* receptors*). GABAA* receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3) .

HY-145258

GABAA receptor agent 6	GABA Receptor	Neurological Disease
GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an K_i of 0.56 µM. GABAA receptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability .

HY-147736

GABAA receptor agonist 2	GABA Receptor	Neurological Disease
GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression .

HY-147735

GABAA receptor agonist 1	GABA Receptor	Neurological Disease
GABAA receptor agonist 1 (compound 3e) is a potent GABAA receptor agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression .

HY-146100

GABAA receptor agent 8	GABA Receptor	Neurological Disease
GABAA receptor agent 8 (compoud 5e) is a potent GABAA receptor positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy .

HY-146099

GABAA receptor agent 7	GABA Receptor	Neurological Disease
GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy .

HY-133486

GABAA receptor agent 1

GABA Receptor Neurological Disease

GABAA receptor agent 1 is a high affinity ligand for GABAA receptor, with potent anticonvulsant activity .

GABAA receptor agent 1	GABA Receptor	Neurological Disease
GABAA receptor agent 1 is a high affinity ligand for GABAA receptor, with potent anticonvulsant activity .

HY-145256

GABAA receptor agent 4	GABA Receptor	Neurological Disease
GABAA receptor agent 4 (compound 1e) is a potent γ-GABAAR antagonist with an K_i of 0.18 µM. GABAA receptor agent 4 efficiently rescues inhibition of T cell proliferation. GABAA receptor agent 4 has the immunomodulatory potential .

HY-147657

GABAA receptor modulator-2	GABA Receptor	Neurological Disease
GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABA_AR negative allosteric modulator (NAM) with a K_i of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .

HY-145257

GABAA receptor agent 5	GABA Receptor	Neurological Disease
GABAA receptor agent 5 (compound 018) is a potent γ-GABAAR antagonist with an K_i of 0.020 µM. GABAA receptor agent 5 shows γ-GABAAR antagonist activity with low cellular membrane permeability .

HY-103501

SB-205384	GABA Receptor	Neurological Disease
SB-205384 is a *GABAA* receptor modulator. The primary effect of SB-205384 on GABAA-activated currents is a prolonged response decay half-life upon removal of the agonist .

HY-116813

ZK 93423

GABA Receptor Neurological Disease

ZK 93423 is a potent benzodiazepine GABAA receptor agonist with a certain cooling effect on rodents .
HY-147421

Xilmenolone

GABA Receptor Neurological Disease

Xilmenolone is a GABAA receptor positive allosteric modulator .

ZK 93423	GABA Receptor	Neurological Disease
ZK 93423 is a potent benzodiazepine *GABAA* receptor agonist with a certain cooling effect on rodents .

Xilmenolone	GABA Receptor	Neurological Disease
Xilmenolone is a GABAA receptor positive allosteric modulator .

HY-B1494

Picrotoxinin 3 Publications Verification	Chloride Channel GABA Receptor	Neurological Disease
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABA_A receptor antagonist, which negatively modulates the action of GABA on GABA_A receptors. Picrotoxinin inhibits α₁β₂γ_2L GABA_A receptor with an IC₅₀ of 1.15 μM .

HY-116622

α5IA

L-822179
GABA Receptor Neurological Disease

α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential .
HY-N10884

Withasomniferolide A

Others Others

Withasomniferolide A is a withanolide, isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .

α5IA L-822179	GABA Receptor	Neurological Disease
α5IA (L-822179) is a selective α5 *GABAA* receptor inverse agonist with neuroprotective potential .

Withasomniferolide A	Others	Others
Withasomniferolide A is a withanolide, isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .

HY-103524

Valerenic acid 1 Publications Verification (-)-Valerenic Acid	GABA Receptor 5-HT Receptor	Neurological Disease
Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of *GABA_A* receptors. Valerenic acid is also a partial agonist of the 5-HT_5a receptor. Valerenic acid mediates anxiolytic activity via GABA_A receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .

HY-113346

Tetrahydrodeoxycorticosterone Tetrahydro-11-deoxycorticosterone	GABA Receptor Endogenous Metabolite	Neurological Disease
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABA_A receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .

HY-103535

GBLD345

GABA Receptor Neurological Disease

GBLD345, a nonbenzodiazepine anxiolytic agent, is a non- selective, potent GABAA receptor positive allosteric modulator (PAM) .

GBLD345	GABA Receptor	Neurological Disease
GBLD345, a nonbenzodiazepine anxiolytic agent, is a non- selective, potent GABAA receptor positive allosteric modulator (PAM) .

HY-116457

Propanidid Sombrevin; Fabantol	GABA Receptor	Neurological Disease
Propanidid (Sombrevin; Fabantol) is a *γ-aminobutyric acid type A (GABA_A)* receptor** agonist and a short-acting non-barbiturate general anesthetic agent. Propanidid can decrease the arterial pressure .

HY-124030

3-Hydroxyphenazepam	Drug Metabolite	Neurological Disease
3-Hydroxyphenazepam is an active metabolite of Cinazepam. Cinazepam is a GABAA receptor agonist. 3-Hydroxyphenazepam can inhibit synaptosomal transporter-mediated [ ³H]GABA uptake .

HY-124463

Epiallopregnanolone 5α,3β-THDOC	GABA Receptor iGluR	Neurological Disease
Epiallopregnanolone (5α,3β-THDOC), a 3β-hydroxy neurosteroid, an antagonist at GABAA receptors and a NMDA receptor enhancer .

HY-16716

Basmisanil 1 Publications Verification RG1662; RO5186582	GABA Receptor	Neurological Disease
Basmisanil (RG1662) is a highly selective orally active *α subunit-containing GABAA* receptors (GABAAα5)** negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a K_i value of 5 nM and IC₅₀ value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .

HY-N10887

Withasomniferolide B	GABA Receptor	Neurological Disease
Withasomniferolide B is a withanolide. Withasomniferolide B can be isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .

HY-120837

PZ-II-029	GABA Receptor	Neurological Disease
PZ-II-029 is a *GABAA* positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects .

HY-B1606

Chlorothymol Chlorthymol; 6-Chlorothymol	GABA Receptor	Neurological Disease
Chlorothymol (Chlorthymol) is a potent GABA_A receptor subunit, LGC-37, inhibitor. Chlorothymol is an effective anticonvulsant. Chlorothymol is protective in several mouse seizure assays, including the 6-Hz 44-mA model of pharmacoresistant seizures .

HY-100991

FG 7142 ZK 39106; LSU-65	GABA Receptor	Neurological Disease
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (K_i=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC₅₀= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex .

HY-133596

12,14-Dichlorodehydroabietic acid	Potassium Channel GABA Receptor	Neurological Disease
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca ²⁺-activated K ⁺ (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks *GABA*-dependent chloride entry in mammalian brain and operates as a non-competitive *GABA_A* antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca ²⁺ and stimulates transmitter release .

HY-N2080

Songorine	GABA Receptor	Cancer
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC) .

HY-100369A

DMCM hydrochloride	GABA Receptor	Neurological Disease
DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with K_is of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively .

HY-N0301

Thiocolchicoside	GABA Receptor	Neurological Disease Inflammation/Immunology
Thiocolchicoside is a competitive *γ-aminobutyric acid type A (GAB_AA)* receptor antagonist and glycine receptor** agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties .

HY-10233

Gaboxadol hydrochloride 1 Publications Verification Lu 02-030 hydrochloride; THIP hydrochloride	GABA Receptor	Neurological Disease
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABA_A receptor and an antagonist of GABA_C receptors (IC₅₀=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED₅₀ value of 143 µM, a full agonist efficacy at α5 subunit (ED₅₀=28-129 µM) and a superagonist efficacy at α4β3δ (ED₅₀=6 µM). Gaboxadol hydrochloride is a non-opioid agent .

HY-107782

Picrotin	GABA Receptor	Neurological Disease
Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs/b> with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

HY-131997

2'MeO6MF	GABA Receptor	Neurological Disease Inflammation/Immunology
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABA_A receptors. 2'MeO6MF also can directly activate α2β2/3 and *α2β2/3γ2L GABA_A* receptors**. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response .

HY-N0301R

Thiocolchicoside (Standard)	GABA Receptor	Neurological Disease Inflammation/Immunology
Thiocolchicoside (Standard) is the analytical standard of Thiocolchicoside. This product is intended for research and analytical applications. Thiocolchicoside is a competitive *γ-aminobutyric acid type A (GAB_AA)* receptor antagonist and glycine receptor** agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties .

HY-106851

Panadiplon FG 10571; PNU 78875	GABA Receptor	Neurological Disease
Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a *5GABAA* partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors .

HY-100370

MRK-016	GABA Receptor	Cancer
MRK-016 is a selective, orally bioavailable inverse agonist of GABA_A α5 receptor, with an EC₅₀ of 3 nM for GABA_A α5, and K_is of 0.83, 0.85, 0.77 and 1.4 nM for human GABA_A α1β3γ2, GABA_A α2β3γ2, GABA_A α3β3γ2, and GABA_A α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.

HY-19308

RWJ-51204

GABA Receptor Neurological Disease

RWJ-51204 is a partial agonist of GABA(A) receptor, with K_i of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

RWJ-51204	GABA Receptor	Neurological Disease
RWJ-51204 is a partial agonist of GABA(A) receptor, with K_i of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

HY-P5860

MmTx1 toxin Micrurotoxin 1	GABA Receptor	Neurological Disease
MmTx1 toxin (Micrurotoxin 1) is an allosteric *GABA_A* receptor modulator that increases GABA_A receptor susceptibility to agonist .

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-100936

Etazolate hydrochloride SQ 20009; EHT 0202 hydrochloride	Phosphodiesterase (PDE) GABA Receptor	Neurological Disease Inflammation/Immunology
Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC₅₀ of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABA_A) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects .

HY-B1803A

Tracazolate hydrochloride ICI 136753 hydrochloride	GABA Receptor	Neurological Disease
Tracazolate (ICI 136753) hydrochloride is a potent *GABA_A* receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC₅₀=13.2 μM), α1β3γ2 (EC₅₀=1.5 μM). Tracazolate hydrochloride has the potency (EC₅₀) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity .

HY-Y1176

Isonipecotic acid

GABA Receptor Neurological Disease

Isonipecotic acid is a GABAA receptor partial agonist .
HY-117257

PF-0713

GABA Receptor Cancer

PF 0713 is a GABAA receptor agonist. .

Isonipecotic acid	GABA Receptor	Neurological Disease
Isonipecotic acid is a GABAA receptor partial agonist .

PF-0713	GABA Receptor	Cancer
PF 0713 is a *GABAA* receptor agonist. .

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-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-100686

U93631	GABA Receptor	Neurological Disease
U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.

HY-114871

SL651498	GABA Receptor	Neurological Disease
SL651498 is a full agonist of α2 and *α3 GABAA* receptors, and a partial agonist of α1 and α5 GABAA receptors**. SL651498 shows anxiolytic and anticonvulsant activities .

HY-N2079

(-)-Securinine

GABA Receptor Neurological Disease Cancer

(-)-Securinine is plant-derived alkaloid and also a GABA_A receptor antagonist.
HY-N6628

6,2'-Dihydroxyflavone

GABA Receptor Neurological Disease

6,2'-Dihydroxyflavone is a novel antagonist of GABA_A receptor.

Cat. No.	Product Name

HY-L120

GABA Receptor Compound Library

139 compounds

GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). GABA receptors are significant drug targets in the treatment of neuropsychiatric disorders such as epilepsy, insomnia, and anxiety, as well as in anesthesia in surgical operations.

MCE offers a unique collection of 139 GABA receptors inhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.

Cat. No.	Product Name	Type

HY-D1704

Bodipy TMR-X muscimol	Fluorescent Dyes/Probes
Bodipy TMR-X muscimol is a Bodipy labeled Muscimol (HY-N2313) (Ex=543 nm, Em=572 nm). Muscimol is a GABAA agonist. Bodipy TMR-X muscimol can be used for imaging the spread of reversible brain inactivations .

Cat. No.	Product Name	Type

HY-N2338

Cholesterol myristate Cholesteryl myristate; Cholesteryl tetradecanoate	Drug Delivery
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.

Cat. No.	Product Name	Target	Research Area

HY-P5964A

K1 peptide TFA

Peptides Neurological Disease

K1 peptide TFA is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP) .

HY-P1083

Dynamin inhibitory peptide	Dynamin	Neurological Disease
Dynamin inhibitory peptide competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide blocks the dopamine D3 effect on GABAA receptors .

HY-P5860

MmTx1 toxin Micrurotoxin 1	GABA Receptor	Neurological Disease
MmTx1 toxin (Micrurotoxin 1) is an allosteric *GABA_A* receptor modulator that increases GABA_A receptor susceptibility to agonist .

HY-P5857

MmTx2 toxin Micrurotoxin 2	GABA Receptor	Neurological Disease
MmTx2 toxin is a *GABA_A* receptor modulator that enhances *GABA_A* receptor sensitivity to agonists. MmTx2 toxin can be obtained from venom of coral snake. MmTx2 toxin can be used in the study of neurological diseases such as epilepsy, schizophrenia and chronic pain .

HY-P5964

K1 peptide

Peptides Neurological Disease

K1 peptide is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP) .

HY-P1083A

Dynamin inhibitory peptide TFA	Dynamin	Neurological Disease
Dynamin inhibitory peptide TFA competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide TFA blocks the dopamine D₃ effect on GABA_A receptors .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B1494

Picrotoxinin 3 Publications Verification	Structural Classification Natural Products other families Source classification Plants	Chloride Channel GABA Receptor
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABA_A receptor antagonist, which negatively modulates the action of GABA on GABA_A receptors. Picrotoxinin inhibits α₁β₂γ_2L GABA_A receptor with an IC₅₀ of 1.15 μM .

HY-113346

Tetrahydrodeoxycorticosterone Tetrahydro-11-deoxycorticosterone	Structural Classification Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Steroids	GABA Receptor Endogenous Metabolite
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABA_A receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .

HY-N2080

Songorine	Alkaloids Aconitum soongaricum Stapf Classification of Application Fields Source classification Ranunculaceae Plants Disease Research Fields Cancer	GABA Receptor
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC) .

HY-N10884

Withasomniferolide A	Structural Classification Source classification Withania somnifera Plants Solanaceae Steroids	Others
Withasomniferolide A is a withanolide, isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .

HY-N10887

Withasomniferolide B	Structural Classification Source classification Withania somnifera Plants Solanaceae Steroids	GABA Receptor
Withasomniferolide B is a withanolide. Withasomniferolide B can be isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .

HY-107782

Picrotin	Structural Classification other families Iridoids Terpenoids Source classification Plants	GABA Receptor
Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs/b> with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

HY-N2079

(-)-Securinine	Flueggea suffruticosa (Pall.) Baill. Alkaloids Classification of Application Fields Neurological Disease Source classification Pyridine Alkaloids Euphorbiaceae Plants Disease Research Fields Cancer	GABA Receptor
(-)-Securinine is plant-derived alkaloid and also a GABA_A receptor antagonist.

HY-N2160

6'''-Feruloylspinosin	Structural Classification Flavonoids other families Flavones Source classification Phenols Polyphenols Plants	GABA Receptor
6'''-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6'''-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons .

HY-N6648

Cirsimaritin	Flavonoids Flavones Leguminosae Source classification Phenols Polyphenols Abrus precatorius Linn. Plants	GABA Receptor
Cirsimaritin binds weakly to the benzodiazepine site on *GABA_A* receptors, with antidepressant, anxiolytic and antinociceptive activities.

HY-Y1683

DL-Menthol Racementhol	Structural Classification Natural Products Classification of Application Fields Leguminosae Labiatae Source classification Other Diseases Erythrina poeppigiana Plants Glycyrrhiza uralensis Fisch. Disease Research Fields	GABA Receptor
DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol relates to the activation of GABAA receptor .

HY-13694

Methionine 1 Publications Verification MRX-1024; D-Methionine	Structural Classification Human Gut Microbiota Metabolites Neurological Disease Classification of Application Fields Source classification Amino acids Endogenous metabolite Disease Research Fields Cancer	GABA Receptor Endogenous Metabolite
Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through *GABA_A* receptor activation.

HY-B0649

Propofol 5+ Cited Publications 2,6-Diisopropylphenol	Structural Classification Monophenols Neurological Disease Classification of Application Fields Source classification Phenols Endogenous metabolite Disease Research Fields Cancer	GABA Receptor Endogenous Metabolite
Propofol potently and directly activates *GABA_A* receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .

HY-Y0313

p-Hydroxybenzaldehyde	Brachyclados megalanthus Speg. Ketones, Aldehydes, Acids Labiatae Source classification Phenols Plants Endogenous metabolite	Endogenous Metabolite GABA Receptor
p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABA_A receptor of the α₁β₂γ₂S subtype at high concentrations.

HY-N0549

(-)-α-Pinene	Other Monoterpenes other families Terpenoids Source classification Plants Endogenous metabolite	GABA Receptor Bacterial Virus Protease Endogenous Metabolite
(-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site .

HY-N2338

Cholesterol myristate Cholesteryl myristate; Cholesteryl tetradecanoate	Structural Classification Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Steroids Cancer	nAChR GABA Receptor Potassium Channel Endogenous Metabolite
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.

HY-N2096

Kavain	Natural Products Source classification Piperaceae Piper methysticum G.Forst. Plants	GABA Receptor
Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor .

HY-N0718

Valepotriate Valtrate	other families Iridoids Terpenoids Source classification Plants	Apoptosis
Valepotriate can be isolated from Valeriana jatamansi Jones, has anti-epileptic and anti-cancer activities .

HY-113320

Etiocholanolone 5β-Androsterone	Structural Classification Microorganisms Source classification Endogenous metabolite Steroids	GABA Receptor Endogenous Metabolite
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the *GABA_A* receptor than its enantiomer form .

HY-N0042

Ginsenoside Rc Panaxoside Rc	Panax ginseng C. A. Meyer Triterpenes Structural Classification Neurological Disease Classification of Application Fields Terpenoids Source classification Plants Inflammation/Immunology Disease Research Fields Araliaceae	GABA Receptor TNF Receptor Interleukin Related
Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptor_A (GABA_A)-mediated ion channel currents (I_GABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.

HY-107198

(2S)-6-Prenylnaringenin 1 Publications Verification	Structural Classification Flavonoids Humulus lupulus L. Flavonones Source classification Phenols Polyphenols Plants Moraceae	GABA Receptor
(2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a *GABA_A* positive allosteric modulator at α+β- binding interface .

HY-B0649R

Propofol (Standard) 2,6-Diisopropylphenol (Standard)	Structural Classification Monophenols Source classification Phenols Endogenous metabolite	GABA Receptor Endogenous Metabolite
Propofol (Standard) is the analytical standard of Propofol. This product is intended for research and analytical applications. Propofol potently and directly activates *GABA_A* receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .

HY-N0067

γ-Aminobutyric acid 3 Publications Verification 4-Aminobutyric acid	Structural Classification Animals Ketones, Aldehydes, Acids Source classification Endogenous metabolite	GABA Receptor Endogenous Metabolite
γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABA_A receptors) and metabotropic receptors (GABA_B receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .

HY-N6084

Humulone α-Lupulic acid	Cardiovascular Disease Classification of Application Fields Ketones, Aldehydes, Acids Humulus lupulus L. Source classification Plants Moraceae Disease Research Fields	COX GABA Receptor Apoptosis
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABA_A receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties .

HY-N0662

Amentoflavone 5+ Cited Publications Didemethyl-ginkgetin	Structural Classification Flavonoids Classification of Application Fields Source classification Phenols Polyphenols Selaginellaceae Plants Biflavones Disease Research Fields Selaginella tamariscina (P. Beauv.) Spring Cancer	Reactive Oxygen Species Apoptosis Bacterial Fungal RSV GABA Receptor
Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active *GABA(A)* negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase .

HY-N0219

Bicuculline Maximum Cited Publications 20 Publications Verification (+)-Bicuculline; d-Bicuculline	Alkaloids Structural Classification Source classification Plants Isoquinoline Alkaloids Lamprocapnos spectabilis Papaveraceae	GABA Receptor
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter *GABA_A* receptor antagonist (IC₅₀=2 μM). Bicuculline also blocks Ca ²⁺ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .

HY-W012123

3,4,5-Trimethoxycinnamic acid	Simple Phenylpropanols Source classification Polygalaceae Phenylpropanoids Plants Endogenous metabolite Polygala tenuifolia Willd.	GABA Receptor Endogenous Metabolite
3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals . 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and *γ-subunit of GABAA* receptor**, but shows no effect on the amounts of α-, β-subunits .

HY-W028263

6-Hydroxyflavanone	Structural Classification Flavonoids Flavonones Source classification Muntingia calabura L. Plants Muntingiaceae	COX Opioid Receptor GABA Receptor Lipoxygenase
6-Hydroxyflavanone is a compound that can be isolated from the Muntingia calabura leaves. 6-Hydroxyflavanone targets cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), and opioid and GABA-A receptors that has anti-inflammatory and anti-neuropathic pain potential. 6-Hydroxyflavanone can be used for the research of diabetes .

HY-N0067R

γ-Aminobutyric acid (Standard) 4-Aminobutyric acid (Standard)	Structural Classification Animals Ketones, Aldehydes, Acids Source classification Endogenous metabolite	Endogenous Metabolite GABA Receptor
γ-Aminobutyric acid (Standard) is the analytical standard of γ-Aminobutyric acid. This product is intended for research and analytical applications. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABA_A receptors) and metabotropic receptors (GABA_B receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .

HY-B1671

(+)-Kavain	Structural Classification Source classification Other Phenylpropanoids Piper methysticum G.Forst. Piperaceae Phenylpropanoids Plants	GABA Receptor Sodium Channel Calcium Channel
(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na ⁺ and Ca ²⁺ channels . (+)-Kavain is shown to bind at the α4β2δ GABA_A receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .

Species:	Human (5)
Tag:	His (4) GST (1) MBP (1) Fc (1)
Source:	E. coli (5)

Cat. No.	Compare	Product Name	Species	Source

HY-P72639

	GABARAP Protein, Human (His, Fc) GABA(A) Receptor-Associated Protein; GABARAP Protein; HCG1987397 Isoform CRA_b; GABARAP	Human	E. coli
	GABARAP (gamma-aminobutyric acid receptor-associated protein) is a protein that performs multiple functions within cells. As a ubiquitin-like modifier, it participates in the intracellular transport of GABA(A) receptors and interacts with the cytoskeleton. GABARAP Protein, Human (His, Fc) is the recombinant human-derived GABARAP protein, expressed by E. coli , with N-His, C-hFc labeled tag. The total length of GABARAP Protein, Human (His, Fc) is 117 a.a., with molecular weight of ~50 kDa.

HY-P71447

	GABRB2 Protein, Human (His) GABA(A) receptor subunit beta-2	Human	E. coli
	GABRB2 protein is an important component of heteropentameric GABA receptors that form ligand-gated chloride channels. It plays a crucial role in establishing functional inhibitory GABAergic synapses, contributing to synaptic depression. GABRB2 Protein, Human (His) is the recombinant human-derived GABRB2 protein, expressed by E. coli , with N-His labeled tag. The total length of GABRB2 Protein, Human (His) is 219 a.a., with molecular weight of ~29.3 kDa.

HY-P76942

	GABARAP Protein, Human (His-MBP) GABA(A) Receptor-Associated Protein; HCG1987397 Isoform CRA_b	Human	E. coli
	GABARAP Protein is essential for regulating ubiquitination and degradation of TIAM1, a guanyl-nucleotide exchange factor (GEF) involved in RAC1 activation and downstream signaling. The D6/7 E3 ubiquitin ligase complex, where GABARAP is a key component, contributes to diverse biological processes, including cytoskeletal organization, cell migration, proliferation, and apoptosis. GABARAP Protein, Human (His-MBP) is the recombinant human-derived GABARAP protein, expressed by E. coli , with N-His, N-MBP labeled tag. The total length of GABARAP Protein, Human (His-MBP) is 117 a.a., with molecular weight of 49-58 kDa.

HY-P70861

	GABARAP Protein, Human (GST) GABA(A) Receptor-Associated Protein; GABARAP Protein; HCG1987397 Isoform CRA_b; GABARAP	Human	E. coli
	GABARAP (gamma-aminobutyric acid receptor-associated protein) is a protein that performs multiple functions within cells. As a ubiquitin-like modifier, it participates in the intracellular transport of GABA(A) receptors and interacts with the cytoskeleton. GABARAP Protein, Human (GST) is the recombinant human-derived GABARAP protein, expressed by E. coli , with N-GST labeled tag. The total length of GABARAP Protein, Human (GST) is 117 a.a., with molecular weight of ~37.0 kDa.

HY-P70913

	GABARAPL1/GEC-1 Protein, Human (His) Gamma-Aminobutyric Acid Receptor-Associated Protein-Like 1; Early Estrogen-Regulated Protein; GABA(A) Receptor-Associated Protein-Like 1; Glandular Epithelial Cell Protein 1; GEC-1; GABARAPL1; GEC1	Human	E. coli
	GABARAPL1/GEC-1 is a multifunctional ubiquitin-like modifier that contributes to cell surface expression of kappa-type opioid receptors and contributes to autophagy, shaping autophagosome vacuoles. Unlike LC3, which is involved in phagophore elongation, the GABARAP/GATE-16 subfamily plays a crucial role in late autophagosome maturation. GABARAPL1/GEC-1 Protein, Human (His) is the recombinant human-derived GABARAPL1/GEC-1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of GABARAPL1/GEC-1 Protein, Human (His) is 117 a.a., with molecular weight of ~20.0 kDa.

Cat. No.	Product Name	Chemical Structure

HY-B0649S1

Propofol-d18
Propofol-d₁₈ is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission[1].

HY-113346S

Tetrahydrodeoxycorticosterone-d3 1 Publications Verification
Tetrahydrodeoxycorticosterone-d₃ is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].

HY-13694S

Methionine-d3
Methionine-d₃ is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.

HY-Y1176S

Isonipecotic acid-d9

Isonipecotic acid-d₉ is the deuterium labeled Isonipecotic acid[1]. Isonipecotic acid is a GABAA receptor partial agonist[2].

HY-121877S

Valnoctamide-d5
Valnoctamide-d₅ is the deuterium labeled Valnoctamide. Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors[1][2].

HY-13694S1

Methionine-d4
Methionine-d₄ is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.

HY-B0649S

Propofol-d17
Propofol-d₁₇ is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties[1].

HY-139145S

Etbicyphat-13C3
Etbicyphat- ¹³C₃ is the ¹³C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].

HY-Y0313S

p-Hydroxybenzaldehyde-d4
p-Hydroxybenzaldehyde-d₄ is the deuterium labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.

HY-Y0313S1

p-Hydroxybenzaldehyde-13C
p-Hydroxybenzaldehyde- ¹³C is the ¹³C-labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.

HY-113320S

Etiocholanolone-d5
Etiocholanolone-d₅ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].

HY-Y0313S2

p-Hydroxybenzaldehyde-d5
p-Hydroxybenzaldehyde-d₅ is the deuterium labeled p-Hydroxybenzaldehyde[1]. p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations[2].

HY-113320S1

Etiocholanolone-d2
Etiocholanolone-d₂ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].

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].

HY-123489S

3α,21-Dihydroxy-5α-pregnan-20-one-d3
3α,21-Dihydroxy-5α-pregnan-20-one-d₃ is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.

HY-N0067S1

γ-Aminobutyric acid-d2
γ-Aminobutyric acid-d₂ is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].

HY-N0067S

γ-Aminobutyric acid-d6
γ-Aminobutyric acid-d₆ is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].

HY-N0067S3

γ-Aminobutyric acid-13C4
γ-Aminobutyric acid- ¹³C₄ is the ¹³C-labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].

HY-N0067S2

γ-Aminobutyric acid-4,4-d2
γ-Aminobutyric acid-4,4-d₂ is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].

HY-16579AS2

Etifoxine-d5
Etifoxine-d₅ is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].

HY-B0135S

Furosemide-d5

Furosemide-d₅ is the deuterium labeled Furosemide. Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2[1]. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema[2].

Cat. No.	Compare	Product Name	Application	Reactivity

HY-P82013

GABA A Receptor beta 2 Antibody (YA1758)

GABA; GABA(A) receptor beta 2; GABA(A) receptor subunit beta-2; GABRB2
WB Human, Mouse, Rat
HY-P82516

GABA A Receptor beta 1 Antibody (YA2261)

GABA-A receptor; beta-1 polypeptide; Gabrb-1; GABRB1; GARB1
WB Human, Mouse, Rat

Cat. No.	Product Name		Classification

HY-103476

Ro15-4513		Azide
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

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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