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pain treatment

" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (1) 5-HT Receptor (2) Calcium Channel (2) Cannabinoid Receptor (1) COX (1) Dopamine Receptor (1) FAAH (1) GlyT (2) iGluR (4) Isotope-Labeled Compounds (1) P2X Receptor (2) Phosphodiesterase (PDE) (1) Phospholipase (1) Potassium Channel (3) Prostaglandin Receptor (2) Reference Standards (1) Sigma Receptor (2) Sodium Channel (9) Trk Receptor (1) TRP Channel (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (2) Endocrinology (2) Inflammation/Immunology (10) Metabolic Disease (2) Neurological Disease (19)

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0718

Methoxyflurane DA-759	Potassium Channel	Neurological Disease
Methoxyflurane disrupts neuronal transmission by interfering with the release and re-uptake of neurotransmitters at post-synaptic terminals, or altering ionic conductance following receptor activation[1]. Methoxyflurane is an analgesic agent that provides rapid short-term analgesia. Methoxyflurane may shows a effective non-opioid treatment option for trauma pain .

HY-P1681A

GpTx-1 TFA	Sodium Channel	Neurological Disease
GpTx-1 TFA is a peptide-based Na_V1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 TFA demonstrates potent inhibitory activity against the Na_V1.7 channel with an IC₅₀ value of 10 nM, while exhibiting excellent selectivity for Na_V1.4 (IC₅₀ = 0.301 μM) and Na_V1.5 (IC₅₀ = 4.20 μM), showing >20-fold and >950-fold selectivity respectively .

HY-14777

Radiprodil RGH-896	iGluR	Neurological Disease
Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions .

HY-N2428

N-(3-Methoxybenzyl)Palmitamide	FAAH	Neurological Disease
N-(3-Methoxybenzyl)Palmitamide is a promising inhibitor of FAAH for the treatment of pain, inflammation and CNS degenerative disorders .

HY-N4030

Humantenmine Gelsenicine	Others	Inflammation/Immunology
Humantenmine, a newalkaloid isolated from Gelsemium elegan Banth in China, has the potential for pain and rheumatic arthritis treatment .

HY-15736

Sodium Channel inhibitor 1	Sodium Channel	Neurological Disease
Sodium Channel inhibitor1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment.

HY-119373

Cav 2.2 blocker 1 1 Publications Verification	Calcium Channel	Neurological Disease
Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain, with an IC₅₀ of 1 nM .

HY-B1798A

Tocainide hydrochloride	Sodium Channel	Inflammation/Immunology
Tocainide hydrochloride is a sodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus .

HY-B1798

Tocainide	Sodium Channel	Cardiovascular Disease
Tocainide hydrochloride is an orally activesodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus .

HY-14777R

Radiprodil (Standard)	iGluR	Neurological Disease
Radiprodil (Standard) is the analytical standard of Radiprodil. This product is intended for research and analytical applications. Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions .

HY-157802A

(S)-LTGO-33	Sodium Channel	Neurological Disease
(S)-LTGO-33 is a small molecule inhibitor of voltage-gated sodium channel NaV1.8. (S)-LTGO-33 can be used in the treatment of pain disorders .

HY-B1901S

Eperisone-d10 hydrochloride	Isotope-Labeled Compounds	Neurological Disease
Eperisone-d₁₀ (hydrochloride) is the deuterium labeled Eperisone hydrochloride. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an antispastic agent used for treatment of diseases characterized by muscle stiffness and pain. It works by relaxing both skeletal muscles and vascularsmooth muscles, thus demonstrating avariety of effects such as reduction ofmyotonia, improvement of circulationand suppression of the pain reflex. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect [2 .

HY-U00325

11β-HSD1-IN-1	11β-HSD	Neurological Disease
11β-HSD1-IN-1 is an inhibitor of 11β-hydroxydehydrogenase 1 (11β-HSD1), with an IC₅₀ of 52 nM, and used for the treatment of pain.

HY-W835175

Neramexane hydrochloride	iGluR
Neramexane hydrochloride is an oral N-methyl-D-aspartate (NMDA) receptor antagonist, as a potential neuroprotectant for various central nervous system disorders, including Alzheimer's disease, and for the potential treatment of drug and alcohol dependence, and pain.

HY-138973

Neramexane	iGluR
Neramexane is an oral N-methyl-D-aspartate (NMDA) receptor antagonist, as a potential neuroprotectant for various central nervous system disorders, including Alzheimer's disease, and for the potential treatment of drug and alcohol dependence, and pain.

HY-D2868

DAPI 4',6-Diamidino-2-phenylindole	Sodium Channel	Neurological Disease
DAPI (Compound 3) is an acid-sensing ion channel 3 (ASIC3) inhibitor. DAPI binds to ASIC3 and blocks the channel function. DAPI can be used in the study of chronic pain treatment .

HY-124382

AS1928370	TRP Channel	Neurological Disease
AS1928370 is a novel and central nervous system (CNS) penetrant TRPV1 antagonist and can prevent ligand-induced activation in vivo. AS1928370 is a promising agent for neuropathic pain treatment research .

HY-114237

GDC-0276	Sodium Channel	Neurological Disease
GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC₅₀ value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects .

HY-111996

Kv3 modulator 1	Potassium Channel	Inflammation/Immunology
Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 has the potential for inflammatory pain treatment .

HY-167734

Pemedolac AY-30715	COX	Inflammation/Immunology
Pemedolac (AY-30715) is a potent analgesic with significant pain-relief efficacy against chemically induced and inflammatory pain in animal models. Pemedolac displays a notable separation between analgesic effects and anti-inflammatory activity, achieving effective pain relief at much lower doses than those required for anti-inflammatory or gastric irritant effects. Pemedolac also shows low ulcerogenic potential, indicating a safer profile compared to standard NSAIDs while being utilized for the treatment of neurological, skin, and musculoskeletal disorders.

HY-123637

Autotaxin-IN-1	Phosphodiesterase (PDE)	Inflammation/Immunology
Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC₅₀=2.2 nM), PK properties, and a robust PK/PD relationship. Autotaxin-IN-1 is used in treatment of osteoarthritis pain .

HY-17569R

Difluprednate (Standard)	Reference Standards Phospholipase	Inflammation/Immunology
Difluprednate (Standard) is the analytical standard of Difluprednate. This product is intended for research and analytical applications. Difluprednate is a topical corticosteroid, which is thought to act by the induction of phospholipase A2 inhibitory proteins (lipocortins). Difluprednate is used for the symptomatic treatment of inflammation and pain associated with ocular surgery.

HY-125821

Sigma-1 receptor antagonist 1	Sigma Receptor	Neurological Disease
Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (K_i = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain .

HY-B1798R

Tocainide (Standard)	Sodium Channel	Cardiovascular Disease
Tocainide (Standard) is the analytical standard of Tocainide. This product is intended for research and analytical applications. Tocainide hydrochloride is an orally activesodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus .

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-128830

Kv3 modulator 3	Potassium Channel	Inflammation/Immunology
Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain .

HY-16781

Grapiprant 4 Publications Verification CJ-023423; RQ-00000007; AAT-007	Prostaglandin Receptor	Metabolic Disease Endocrinology Cancer
Grapiprant (CJ-023423) is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E₂ (PGE₂). Grapiprant displaces [ ³H]-PGE₂ (1 nM) binding to dog recombinant EP4 receptor with IC₅₀ value of 35 nM and K_i value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment ^[3].

HY-124637

ALE-0540	Trk Receptor	Neurological Disease
ALE-0540, a nonpeptidic small molecule, is a nerve growth factor receptor antagonist. ALE-0540 inhibits the binding of NGF to tyrosine kinase (Trk) A or both p75 and TrkA with IC₅₀ values of 5.88 μM and 3.72 μM, respectively. ALE-0540 can be used to examine mechanisms leading to the development of agents for the treatment of pain .

HY-131914B

EST64454 maleate	Sigma Receptor	Inflammation/Immunology
EST64454 maleate is a highly soluble σ1 receptor antagonist, demonstrating potent antinociceptive properties for pain treatment. EST64454 maleate exhibits excellent metabolic stability across various species and possesses an adequate pharmacokinetic profile in rodents. EST64454 maleate has been identified as a promising clinical candidate due to its favorable aqueous solubility and high permeability in Caco-2 cells.

HY-P5813

Cd1a β-TRTX-cd1a; β-Theraphotoxin-cd1a	Calcium Channel	Neurological Disease
Cd1a is a β-toxin derived from the African spider Ceratogyrus darlingi. Cd1a can regulate calcium ion channels. Cd1a inhibits human calcium ion channels (Ca_v2.2)(IC₅₀2.6 μM) and mouse sodium ion channels (Na_v1.7). Cd1a can be used in the development of peripheral pain treatment drugs .

HY-109067A

Opiranserin hydrochloride VVZ-149 hydrochloride	GlyT 5-HT Receptor P2X Receptor	Neurological Disease
Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC₅₀s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC₅₀=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain .

HY-16781R

Grapiprant (Standard)	Prostaglandin Receptor	Metabolic Disease Endocrinology Cancer
Grapiprant (Standard) is the analytical standard of Grapiprant. This product is intended for research and analytical applications. Grapiprant (CJ-023423) is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). Grapiprant displaces [3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor with IC50 value of 35 nM and Ki value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment .

HY-109067

Opiranserin VVZ-149	GlyT 5-HT Receptor P2X Receptor	Neurological Disease
Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC₅₀s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC₅₀=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain .

HY-155707

MOR agonist-3	Dopamine Receptor	Inflammation/Immunology
MOR agonist-3 (Compound 84) is a D3R/MOR antagonist/partial agonist a(K_i 382 nM and 55.2 nM respectively). MOR agonist-3 has the potential to produce analgesic effects through MOR (μ-opioid receptor) (HY-149337) partial agonists and to reduce opioid abuse through D3R antagonists. MOR agonist-3 can be used in the treatment of inflammation and neuropathic pain research .

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 .

Cat. No.	Product Name

HY-L139

Pain-Related Compound Library	2,658 compounds
Pain is a kind of distressing feeling caused by the stimulation of tissue damage. According to the International Association for the Study of Pain (IASP), pain is defined as ”An unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage”. Pain is usually classified according to its location, duration, underlying causes, and intensity. For example, acute and chronic pain, muscle pain, and nerve pain. Pain is the main symptom of most diseases, which seriously affects the quality of life and body function of patients. In the medical treatment of pain, anti-inflammatory drugs and opioid analgesic agents have traditionally been used, but the side effects are serious. In recent years, targeted drugs targeting the ERK/MAPK pathway or other targets have gradually become a research hotspot. MCE supplies a unique collection of 2,658 compounds targeting key proteins in the pain system. MCE Pain-Related Compound Library is a useful tool for pain related research and anti-pain drug development.

Pain-Related Compound Library

2,658 compounds

Pain is a kind of distressing feeling caused by the stimulation of tissue damage. According to the International Association for the Study of Pain (IASP), pain is defined as ”An unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage”.

Pain is usually classified according to its location, duration, underlying causes, and intensity. For example, acute and chronic pain, muscle pain, and nerve pain. Pain is the main symptom of most diseases, which seriously affects the quality of life and body function of patients. In the medical treatment of pain, anti-inflammatory drugs and opioid analgesic agents have traditionally been used, but the side effects are serious. In recent years, targeted drugs targeting the ERK/MAPK pathway or other targets have gradually become a research hotspot.

MCE supplies a unique collection of 2,658 compounds targeting key proteins in the pain system. MCE Pain-Related Compound Library is a useful tool for pain related research and anti-pain drug development.

HY-L118

Sodium Channel Blocker Library	164 compounds
Sodium channels conduct sodium ions (Na+) through a cell's plasma membrane that are the source of excitatory currents for the nervous system and muscle. Na channels are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). Dysfunction in voltage-gated sodium channels correlates with neurological and cardiac diseases, including epilepsy, myopathies, pain and cardiac arrhythmias. Sodium channel blockers are used in the treatment of cardiac arrhythmia, pain and convulsion. MCE offers a unique collection of 164 sodium channel blocker and antagonists, all of which have the identified inhibitory effect on sodium channels. MCE Sodium Channel Blocker Library can be used for neurological and cardiac diseases drug discovery and sodium channel research.

Sodium Channel Blocker Library

164 compounds

Sodium channels conduct sodium ions (Na+) through a cell's plasma membrane that are the source of excitatory currents for the nervous system and muscle. Na channels are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). Dysfunction in voltage-gated sodium channels correlates with neurological and cardiac diseases, including epilepsy, myopathies, pain and cardiac arrhythmias. Sodium channel blockers are used in the treatment of cardiac arrhythmia, pain and convulsion.

MCE offers a unique collection of 164 sodium channel blocker and antagonists, all of which have the identified inhibitory effect on sodium channels. MCE Sodium Channel Blocker Library can be used for neurological and cardiac diseases drug discovery and sodium channel research.

HY-L143

Marine-Sourced Natural Product Library	62 compounds
Oceans cover more than 70% of the Earth’s surface and host a huge species diversity. Marine organisms are considered the most recent source of bioactive natural products after terrestrial plants and nonmarine microorganisms. Marine biological sources are taxonomically diverse and include sponges, tunicates, corals, mollusks, fungi, and sediment-derived bacteria. Marine organisms can produce a plethora of small molecules with novel chemical structures and potent biological properties, being a rich source for the discovery of pharmacologically active compounds, already with several marine-derived agents approved as drugs. Ziconotide, a peptide originally discovered in a tropical cone snail, was the first marine-derived compound to be approved in the United States in December 2004 for the treatment of pain. Then, in October 2007, Trabectedin became the first marine anticancer drug to be approved in the European Union. MCE offers a unique collection of 62 marine-sourced natural products which can be used for drug discovery for high throughput screening (HTS) and high content screening (HCS). MCE marine-sourced natural product library is an important source for drug discovery and development.

Marine-Sourced Natural Product Library

62 compounds

Oceans cover more than 70% of the Earth’s surface and host a huge species diversity. Marine organisms are considered the most recent source of bioactive natural products after terrestrial plants and nonmarine microorganisms. Marine biological sources are taxonomically diverse and include sponges, tunicates, corals, mollusks, fungi, and sediment-derived bacteria.

Marine organisms can produce a plethora of small molecules with novel chemical structures and potent biological properties, being a rich source for the discovery of pharmacologically active compounds, already with several marine-derived agents approved as drugs. Ziconotide, a peptide originally discovered in a tropical cone snail, was the first marine-derived compound to be approved in the United States in December 2004 for the treatment of pain. Then, in October 2007, Trabectedin became the first marine anticancer drug to be approved in the European Union.

MCE offers a unique collection of 62 marine-sourced natural products which can be used for drug discovery for high throughput screening (HTS) and high content screening (HCS). MCE marine-sourced natural product library is an important source for drug discovery and development.

Cat. No.	Product Name	Type

HY-D2868

DAPI 4',6-Diamidino-2-phenylindole	Fluorescent Dyes/Probes
DAPI (Compound 3) is an acid-sensing ion channel 3 (ASIC3) inhibitor. DAPI binds to ASIC3 and blocks the channel function. DAPI can be used in the study of chronic pain treatment .

Cat. No.	Product Name	Target	Research Area

HY-P1681A

GpTx-1 TFA	Sodium Channel	Neurological Disease
GpTx-1 TFA is a peptide-based Na_V1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 TFA demonstrates potent inhibitory activity against the Na_V1.7 channel with an IC₅₀ value of 10 nM, while exhibiting excellent selectivity for Na_V1.4 (IC₅₀ = 0.301 μM) and Na_V1.5 (IC₅₀ = 4.20 μM), showing >20-fold and >950-fold selectivity respectively .

HY-P5813

Cd1a β-TRTX-cd1a; β-Theraphotoxin-cd1a	Calcium Channel	Neurological Disease
Cd1a is a β-toxin derived from the African spider Ceratogyrus darlingi. Cd1a can regulate calcium ion channels. Cd1a inhibits human calcium ion channels (Ca_v2.2)(IC₅₀2.6 μM) and mouse sodium ion channels (Na_v1.7). Cd1a can be used in the development of peripheral pain treatment drugs .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2428

N-(3-Methoxybenzyl)Palmitamide	Natural Products other families Source classification Plants	FAAH
N-(3-Methoxybenzyl)Palmitamide is a promising inhibitor of FAAH for the treatment of pain, inflammation and CNS degenerative disorders .

HY-N4030

Humantenmine Gelsenicine	Alkaloids Structural Classification other families Classification of Application Fields Source classification Plants Inflammation/Immunology Disease Research Fields Indole Alkaloids	Others
Humantenmine, a newalkaloid isolated from Gelsemium elegan Banth in China, has the potential for pain and rheumatic arthritis treatment .

Cat. No.	Product Name	Chemical Structure

HY-B1901S

Eperisone-d10 hydrochloride

Eperisone-d₁₀ (hydrochloride) is the deuterium labeled Eperisone hydrochloride. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an antispastic agent used for treatment of diseases characterized by muscle stiffness and pain. It works by relaxing both skeletal muscles and vascularsmooth muscles, thus demonstrating avariety of effects such as reduction ofmyotonia, improvement of circulationand suppression of the pain reflex. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect [2 .

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pain treatment

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Peptides

NaturalProducts

Isotope-Labeled Compounds

Natural
Products