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Results for "

analgesics for chronic pain

" in MedChemExpress (MCE) Product Catalog:

By Targets:	iGluR (1) Keap1-Nrf2 (1) mGluR (1) Necroptosis (1) Opioid Receptor (2) Potassium Channel (2) Prostaglandin Receptor (1) Sodium Channel (3) TRP Channel (1)
By Research Areas:	Cancer (5) Inflammation/Immunology (7) Metabolic Disease (1) Neurological Disease (9)

Inhibitors & Agonists

Screening Libraries

Peptides

Targets Recommended: Ligands for Target Protein for PROTAC Ligands for E3 Ligase PROTAC-Linker Conjugates for PAC Drug-Linker Conjugates for ADC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-119097

LY456066	mGluR	Neurological Disease
LY456066 is a selective non-competitive metabotropic glutamate receptors (mGluR1) antagonist with an IC₅₀ value of 52.0 nM. LY456066 is effective in rodent models of anxiolysis and nociception. LY456066 reduces hyperalgesia and the amount of licking and flinching following formalin injection, which is promising for research of analgesics for chronic pain .

HY-108449

Acoltremon 1 Publications Verification WS-12; AR-15512; AVX-012	TRP Channel	Cancer
Acoltremon (WS-12; AR-15512) is a potent and selective TRPM8 agonist, the menthol derivative, as a cooling agent. Acoltremon shows analgesic effect, and can be used in chronic neuropathic pain research .

HY-110358

QAQ dichloride	Sodium Channel	Inflammation/Immunology
QAQ dichloride, a photoswitchable voltage-gated Na_v and K_v channels blocker, blocks channels in its trans form (of the azobenzene photoswitch), but not in its cis form. QAQ dichloride is membrane-impermeant and only infiltrates pain-sensing neurons that express endogenous import channels. QAQ dichloride acts as a light-sensitive analgesic and can be used for studying of signaling mechanisms in acute and chronic pain .

HY-107527A

Org 25543	Others	Inflammation/Immunology
Org 25543 is a selective inhibitor of the glycine transporter 2, exhibiting analgesic properties in a rat model of chronic pain.

HY-111258

GSK345931A	Prostaglandin Receptor	Neurological Disease Inflammation/Immunology
GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain .

HY-168166

CHET3	Others	Neurological Disease
CHET3 is a sex-selective activator with potent analgesic activity. CHET3 was discovered to be a highly selective omnidirectional modulator of TASK-3-containing K2P channels, including TASK-3 homologues and TASK-3/TASK-1 heterologues. CHET3 exhibited significant analgesic effects in multiple acute and chronic pain models in mice, which could be abolished by pharmacological means or genetic knockout of TASK-3. CHET3 is able to functionally modulate the membrane excitability of specific small sensory neurons, which supports its analgesic effects on thermal hypersensitivity and mechanical hyperalgesia in chronic pain .

HY-P5907

Helianorphin-19	Opioid Receptor	Neurological Disease
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a K_i of 21 nM and an EC₅₀ of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .

HY-W709349

Flupirtine hydrochloride D 9998 hydrochloride	Potassium Channel iGluR	Inflammation/Immunology
Flupirtine hydrochloride (D 9998 hydrochloride) is a selective neuropotassium channel opener with analgesic activity. Flupirtine hydrochloride is used to inhibit a variety of pain conditions, including chronic musculoskeletal pain, migraines, and neuralgia. Flupirtine hydrochloride has antidepressant and antioxidant properties and may increase the analgesic effect in combination therapy with morphine. Flupirtine hydrochloride relieves abnormally increased muscle tension and has a muscle relaxant effect. Flupirtine hydrochloride is clinically superior to other drugs, such as tramadol and pantoxan, plus its side effects are better tolerated. Flupirtine hydrochloride has a significant effect on inhibiting neural hyperexcitability and therefore exhibits inhibitory potential in various pain states .

HY-159094

Nav1.8-IN-15	Sodium Channel	Neurological Disease
Nav1.8-IN-15 (compound 6) is a potent Nav1.8 inhibitor. Nav1.8-IN-15 shows analgesic effect. Nav1.8-IN-15 has the potential for the research of chronic pain .

HY-110358A

QAQ	Sodium Channel	Inflammation/Immunology
QAQ dichloride dichloride, a photoswitchable voltage-gated Na_v and K_v channels blocker, blocks channels in its trans form (of the azobenzene photoswitch), but not in its cis form. QAQ dichloride dichloride is membrane-impermeant and only infiltrates pain-sensing neurons that express endogenous import channels. QAQ dichloride dichloride acts as a light-sensitive analgesic and can be used for studying of signaling mechanisms in acute and chronic pain .

HY-P3223

Biphalin TFA	Opioid Receptor	Neurological Disease
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .

HY-116275

KRM-II-81	Others	Cancer
KRM-II-81 is a gamma-aminobutyric acid type A (GABAA) receptor ligand with analgesic, anxiolytic and anti-epileptic activities. KRM-II-81 exhibits positive allosteric modulation of GABAA receptors selective for the α2/3 subunit. KRM-II-81 reduces formalin-induced pain response after oral administration. KRM-II-81 significantly reduces pain behavior induced by chronic spinal nerve ligation. Analysis of KRM-II-81 showed that its plasma and brain concentrations were positively correlated with analgesic effects. The enhancement effect of KRM-II-81 on GABA current shows its key role in the analgesic mechanism. KRM-II-81 was less effective in respiratory depression, demonstrating its safety and tolerability .

HY-107794

Clodronate disodium tetrahydrate 2 Publications Verification Disodium clodronate tetrahydrate	Others	Neurological Disease Inflammation/Immunology Cancer
Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl ^- competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC₅₀ of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain .

HY-107794R

Clodronate disodium tetrahydrate (Standard)	Others	Neurological Disease Inflammation/Immunology Cancer
Clodronate (disodium tetrahydrate) (Standard) is the analytical standard of Clodronate (disodium tetrahydrate). This product is intended for research and analytical applications. Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl-competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC₅₀ of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain .

HY-168214

Kv7.2/Kv7.3 agonist 1	Potassium Channel	Neurological Disease
Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally active agonist for KV7.2/7.3 channel (KCNQ2/3) with an EC₅₀ of 1.03 μM. Kv7.2/Kv7.3 agonist 1 exhibits analgesic efficacy in mice chronic constriction injury (CCI) model and mice Streptozotocin (HY-13753)-induced diabetic peripheral neuropathic pain (DPNP) model, with ED₅₀ of 12.02 and 9.63 mg/kg .

HY-14909

Bardoxolone Maximum Cited Publications 15 Publications Verification CDDO; RTA 401	Keap1-Nrf2 Necroptosis	Metabolic Disease Cancer
Bardoxolone (RTA 401; CDDO) is a novel nuclear regulatory factor (NRf-2) activator. Bardoxolone is a potent necroptosis inhibitor that inhibits Z-VAD-FMK-induced necroptosis. Bardoxolone methyl enhances the antioxidant system, modulates inflammatory cytokines and inhibits apoptosis in rat kidney, demonstrating inhibition on APAP-induced acute kidney injury (AKI) and analgesic effect. Additionally, Bardoxolone methyl decreases Paclitaxel (PAC) (HY-B0015)-induced mitochondrial damage in neuronal cells. Bardoxolone methyl is promising for the research of chemotherapy-induced neuropathic pain and chronic kidney disease .

Cat. No.	Product Name

HY-L139

Pain-Related Compound Library	2,012 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 2,012 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

2,012 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 2,012 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.

Cat. No.	Product Name	Target	Research Area

HY-P5907

Helianorphin-19	Opioid Receptor	Neurological Disease
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a K_i of 21 nM and an EC₅₀ of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .

HY-P3223

Biphalin TFA	Opioid Receptor	Neurological Disease
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .

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