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Results for "

pain

" in MCE Product Catalog:

218

Inhibitors & Agonists

1

Screening Libraries

20

Peptides

39

Natural
Products

9

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-119864
    Drinidene

    Others Neurological Disease
    Drinidene can be used for the research of pain disorders extracted from patent AU2018254530A1.
  • HY-131914A
    EST64454 hydrochloride

    Sigma Receptor Neurological Disease
    EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain.
  • HY-131004
    CB2R PAM

    Cannabinoid Receptor Neurological Disease
    CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain.
  • HY-101907
    ASP7663

    TRP Channel Neurological Disease
    ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions.
  • HY-19958
    XEN907

    Sodium Channel Neurological Disease
    XEN907 is a potent and spirooxindole blocker of NaV1.7, with an IC50 of 3 nM. XEN907 also inhibits CYP3A4 in a recombinant human enzyme assay. XEN907 can be used for the research of pain.
  • HY-N0478
    Neoline

    Bullatine B

    Others Neurological Disease
    Neoline, the active ingredient of processed aconite root (PA), alleviated oxaliplatin-induced peripheral neuropathy in mice. Neoline can be used as a marker compound to determine the quality of the PA products for the treatment of neuropathic pain.
  • HY-110358
    QAQ dichloride

    Sodium Channel Inflammation/Immunology
    QAQ dichloride, a photoswitchable voltage-gated Nav and Kv 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-16723A
    (R)-Funapide

    (R)-TV 45070; (R)-XEN402

    Sodium Channel Neurological Disease
    (R)-Funapide ((R)-TV 45070) is the less active R-enantiomer of Funapide. Funapide is a potent Nav1.7 sodium channel blocker that can be used for pain research.
  • HY-107682
    TQS

    nAChR Inflammation/Immunology Neurological Disease
    TQS is a α7 nicotinic acetylcholine receptor (nAChR) positive allosteric modulator. TQS can be used for the research of neuroinflammatory pain.
  • HY-117714
    AZD-3161

    Sodium Channel Neurological Disease
    AZD-3161 is a potent and selective blocker of NaV1.7 channel, with a pIC50 of 7.1. AZD-3161 can be used for the research of neuropathic and inflammatory pain.
  • HY-N1198
    Strictosamide

    Parasite Fungal Infection Inflammation/Immunology
    Strictosamide has important effects on inflammation and inflammatory pain. Strictosamide possesses antiplasmodial and antifungal activities.
  • HY-100129
    JNJ-17203212

    TRP Channel Neurological Disease
    JNJ-17203212 is a selective, potent and competitive TRPV1 antagonist. JNJ-17203212 is developed for researching pain management, such as migraine.
  • 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-135653
    EC5026

    BPN-19186

    Epoxide Hydrolase Neurological Disease
    EC5026 (BPN-19186) is a first-in-class, non-opioid and orally active soluble Epoxide Hydrolase (sEH) inhibitor. EC5026 shows efficacy for inflammatory and neuropathic pain.
  • HY-14485
    Ro-51

    P2X Receptor Neurological Disease
    Ro-51 is a potent and selective dual P2X3/P2X2/3 antagonist, with IC50 of 2 nM and 5 nM for P2X3 and P2X2/3, respectively. Ro-51 can be used for the research for pain.
  • HY-115506
    PF-05105679

    TRP Channel Neurological Disease
    PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. PF-05105679 has the potential for cold-related pain.
  • HY-B1430
    Butamben

    Butyl 4-aminobenzoate

    Calcium Channel Sodium Channel Potassium Channel Neurological Disease
    Butamben (Butyl 4-aminobenzoate) has local narcotic effect. Butamben results in long-lasting relief from pain, without impairing motor function or other sensory functions.
  • HY-133130
    JNJ-42226314

    MAGL Neurological Disease
    JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain.
  • HY-P0244
    Dermorphin

    Opioid Receptor Neurological Disease
    Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.
  • HY-109067
    Opiranserin

    VVZ-149

    GlyT 5-HT Receptor P2X Receptor Neurological Disease
    Opiranserin, 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-N2258
    Poncirin

    Apoptosis Inflammation/Immunology
    Poncirin is isolated from Poncirus trifoliata with anti-inflammory activites. Poncirin significantly reduces mechanical hyperalgesia and allodynia in Complete Freund’s Adjuvant (CFA)-induced inflammatory pain models.
  • HY-P0244A
    Dermorphin TFA

    Opioid Receptor Neurological Disease
    Dermorphin TFA is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.
  • HY-137459
    Vocacapsaicin

    CA-008

    TRP Channel Neurological Disease
    Vocacapsaicin (CA-008), a prodrug of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin can provide meaningful and long-lasting pain relief.
  • HY-122001
    PF-05186462

    Sodium Channel Neurological Disease
    PF-05186462 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channel, with an IC50 of 21 nM. PF-05186462 shows significant selectivity for Nav1.7 versus other sodium channels (Nav 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, and 1.8). PF-05186462 can be used for the research of acute or chronic pain.
  • HY-15451
    MDA 19

    Cannabinoid Receptor Neurological Disease
    MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity.
  • HY-B0161E
    (±)-Duloxetine hydrochloride

    (Rac)-Duloxetine hydrochloride

    Serotonin Transporter Neurological Disease
    (±)-Duloxetine ((Rac)-Duloxetine) hydrochloride is the racemate of Duloxetine hydrochloride. Duloxetine hydrochloride, a serotonin-norepinephrine reuptake inhibitor, can be used for diabetic neuropathic pain and fibromyalgia as well as major depressive disorder research.
  • HY-138761
    EP4 receptor antagonist 3

    Prostaglandin Receptor Cancer Inflammation/Immunology
    EP4 receptor antagonist 3 is a potent EP4 receptor antagonist, example 3,extracted from patent WO2010019796 A1. EP4 receptor antagonist 3 can be used for the reseacrh of EP4 receptor-mediated diseases, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer.
  • HY-B1469
    Isosorbide

    D-Isosorbide; Dianhydro-D-glucitol

    Others Metabolic Disease Cardiovascular Disease
    Isosorbide (D-Isosorbide), an orally active vasodilating agent that can be used for the research of heart failure and angina (chest pain). Isosorbide is also an oral hyperosmotic diuretic.
  • HY-126941
    Hecogenin acetate

    Opioid Receptor Neurological Disease
    Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors.
  • HY-N2433
    Paederosidic acid methyl ester

    Potassium Channel Neurological Disease
    Paederosidic acid methyl ester is a ATP‐sensitive K + channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K + channel in the brain and spinal cord level.
  • HY-10413
    MK-2894

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    MK-2894 is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). MK-2894 possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis.
  • HY-10414
    MK-2894 sodium salt

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    MK-2894 sodium salt is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). MK-2894 sodium salt possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis.
  • 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-141547
    Nav1.7-IN-8

    Sodium Channel Cytochrome P450 Inflammation/Immunology
    Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain.
  • HY-100822
    (R)-(+)-HA-966

    (+)-HA-966

    iGluR Neurological Disease
    (R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine. (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain.
  • HY-N7699A
    D-Trimannuronic acid

    TNF Receptor Inflammation/Immunology Neurological Disease
    D-Trimannuronic acid, an alginate oligomer is extracted from seaweed. D-Trimannuronic acid can induce TNF‐α secretion by mouse macrophage cell lines. D-Trimannuronic acid can be used for the research of pain and vascular dementia.
  • HY-107794
    Clodronate disodium tetrahydrate

    Disodium clodronate tetrahydrate

    Others Inflammation/Immunology Neurological Disease
    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-12883B
    PF 05089771 tosylate

    Sodium Channel Neurological Disease
    PF 05089771 tosylate is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.
  • HY-12883
    PF 05089771

    Sodium Channel Neurological Disease
    PF 05089771 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.
  • HY-120824
    Mofezolac

    COX Inflammation/Immunology
    Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitory activity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities.
  • HY-N7699E
    D-Heptamannuronic acid

    Others Neurological Disease
    D-Heptamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Heptamannuronic acid can be used for the research of pain and vascular dementia.
  • HY-N7699C
    D-Pentamannuronic acid

    Others Neurological Disease
    D-Pentamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Pentamannuronic acid can be used for the research of pain and vascular dementia.
  • HY-N7699F
    D-Octamannuronic acid

    Others Neurological Disease
    D-Octamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Octamannuronic acid can be used for the research of pain and vascular dementia.
  • HY-N7699G
    D-Nonamannuronic acid

    Others Neurological Disease
    D-Nonamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Nonamannuronic acid can be used for the research of pain and vascular dementia.
  • HY-N7699B
    D-Tetramannuronic acid

    Others Neurological Disease
    D-Tetramannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Tetramannuronic acid can be used for the research of pain and vascular dementia.
  • HY-N7699D
    D-Hexamannuronic acid

    Others Neurological Disease
    D-Hexamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Hexamannuronic acid can be used for the research of pain and vascular dementia.
  • HY-19589
    JTS-653

    TRP Channel Inflammation/Immunology Neurological Disease
    JTS-653 is a highly potent and selective transient receptor potential vanilloid 1 (TRPV1) antagonist in vitro and in vivo. JTS-653 attenuates chronic pain refractory to non-steroidal anti-inflammatory agents.
  • HY-110237
    BX430

    P2X Receptor Calcium Channel Cardiovascular Disease
    BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
  • HY-17481
    Bumadizone

    Others Inflammation/Immunology
    Bumadizone is a non-steroidal anti-inflammatory drug (NSAID) and can relieve pain.
  • HY-131019
    JF-NP-26

    mGluR Neurological Disease
    JF-NP-26, an inactive photocaged derivative of raseglurant, is the first caged mGlu5 receptor negative allosteric modulator. Uncaging of JF-NP-26 is elicited with light pulses in the visible spectrum (405 nm). JF-NP-26 induces light-dependent analgesia in models of inflammatory and neuropathic pain in freely behaving animals.
  • HY-103111
    MMPIP hydrochloride

    mGluR Neurological Disease
    MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
  • HY-107503
    MMPIP

    mGluR Neurological Disease
    MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
  • 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 Ki 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-B1888A
    Bromfenac sodium

    COX Inflammation/Immunology
    Bromfenac sodium is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium is a brominated non-steroidal anti-inflammatory/analgesic drug (NSAID), and it is commonly used for the research of postoperative inflammation and pain following cataract surgery, and pseudophakic cystoid macular edema (CME).
  • HY-14380
    PF-3845

    FAAH Autophagy Inflammation/Immunology Cancer
    PF-3845 is a potent, selective, irreversible and orally active inhibitor of fatty acid amide hydrolase (FAAH), with a Ki of 0.23 µM. PF-3845 is a covalent inhibitor that carbamylates FAAH's serine nucleophile. PF-3845 can reduce pain sensation, inflammation, and anxiety/depression without substantial effects on motility or cognition.
  • HY-14886
    Fasitibant chloride

    MEN16132 free base

    Bradykinin Receptor Neurological Disease Cardiovascular Disease
    Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model.
  • HY-B1888B
    Bromfenac sodium hydrate

    Bromfenac monosodium salt sesquihydrate

    COX Inflammation/Immunology
    Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium hydrate is a brominated non-steroidal anti-inflammatory/analgesic drug (NSAID), and it is commonly used for the research of postoperative inflammation and pain following cataract surgery, and pseudophakic cystoid macular edema (CME).
  • HY-18618
    SB-612111

    Opioid Receptor Inflammation/Immunology Neurological Disease
    SB-612111 is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.
  • HY-18617
    SB-612111 hydrochloride

    Opioid Receptor Inflammation/Immunology Neurological Disease
    SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.
  • HY-101437
    Ralfinamide

    FCE-26742A

    Sodium Channel Neurological Disease
    Ralfinamide (FCE-26742A) is an orally available Na + blocker derived from α-aminoamide, with function of suppressing pain.
  • HY-A0259
    Floctafenine

    COX Inflammation/Immunology
    Floctafenine, a nonsteroidal anti-inflammatory agent (NSAID), acts as an effective analgesic agent. Floctafenine is an inhibitor of COX-1 and COX-2 activities in vitro,showing a slightly higher potency towards COX-I. Floctafenine is used for the research of short term pain treatment.
  • HY-101437A
    Ralfinamide mesylate

    FCE-26742A mesylate

    Sodium Channel Neurological Disease
    Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na + channel blocker derived from α-aminoamide, with function of suppressing pain.
  • HY-N3710
    Dehydrocrenatidine

    Kumujian G; O-Methylpicrasidine I

    JAK Apoptosis Cancer Neurological Disease
    Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain.
  • HY-B1695
    Methyl nicotinate

    Others Inflammation/Immunology
    Methyl nicotinate, the methyl ester of Niacin found in alcoholic beverages, that is used as an active ingredient as a rubefacient in over-the-counter topical preparations indicated for muscle and joint pain.
  • HY-106199
    Adenosine A1 receptor activator T62

    Adenosine Receptor Inflammation/Immunology Neurological Disease
    Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain.
  • HY-17474A
    Parecoxib Sodium

    SC 69124A

    COX Inflammation/Immunology Cancer
    Parecoxib Sodium (SC 69124A) is a highly selective and orally active COX-2 inhibitor, the prodrug of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib Sodium can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
  • HY-17474
    Parecoxib

    SC 69124

    COX Cancer Inflammation/Immunology
    Parecoxib (SC 69124) is a highly selective and orally active COX-2 inhibitor, the prodrug of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
  • HY-B0563A
    Ropivacaine hydrochloride monohydrate

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is a local anesthetic agent widely used for regional anesthesia and neuropathic pain management in vivo.
  • HY-B0563C
    Ropivacaine mesylate

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine mesylate is a long-acting amide local anaesthetic agent for a spinal block and effectively blocks neuropathic pain. Ropivacaine blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibressup>[1]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane.
  • HY-101670
    MTPPA

    M 5011

    Others Inflammation/Immunology
    MTPPA is a drug for treating symptoms of inflammation and pain.
  • 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-B0563
    Ropivacaine

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacain is a potent sodium channel blocker and acts as a local anesthetic agent. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is used for the research of regional anesthesia and neuropathic pain management.
  • HY-B0563B
    Ropivacaine hydrochloride

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is a local anesthetic agent widely used for regional anesthesia and neuropathic pain management in vivo.
  • HY-128891
    Eperisone

    Others Neurological Disease
    Eperisone 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 is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect[2 .
  • HY-101719
    Ketocaine

    Rec 7-0518

    Others Neurological Disease
    Ketocaine is a butyrophenone derivative used topically for pain relief.
  • HY-B1901
    Eperisone hydrochloride

    (±)-Eperisone hydrochloride

    Others Neurological Disease
    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-106907
    Furprofen

    PGE synthase Inflammation/Immunology Endocrinology
    Furprofen is an non-steroidal anti-inflammatory drug (NSAID) with analgesic properties. Furprofen acts via the inhibition of prostaglandin (PGE) synthesis. Furprofen can be treated orally for the relief of pain.
  • HY-133115AS
    N-Desmethylnefopam D5 hydrochloride

    β-catenin Neurological Disease
    N-Desmethylnefopam D5 hydrochloride is a deuterium labeled N-Desmethylnefopam hydrochloride. N-Desmethylnefopam hydrochloride is the main metabolite of Nefopam. N-Desmethylnefopam hydrochloride is a centrally-acting but non-opioid analgesic agent, for the relief of moderate to severe pain.
  • HY-13985
    Nav1.7 inhibitor

    Sodium Channel Neurological Disease
    Nav1.7 inhibitor (compound II), a sulfonamide, is a potent Nav1.7 inhibitor. Nav1.7 inhibitor has the potential for a wide range of disorders, particularly pain.
  • HY-N0405
    Orientin

    Others Cancer Neurological Disease
    Orientin is a naturally occurring bioactive flavonoid that possesses diverse biological properties, including anti-inflammation, anti-oxidative, anti-tumor, and cardio protection. Orientin is a promising neuroprotective agent suitable for therapy for neuropathic pain.
  • HY-15568A
    A-317491 sodium salt hydrate

    P2X Receptor Inflammation/Immunology Neurological Disease
    A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
  • HY-15568
    A-317491

    P2X Receptor Inflammation/Immunology Neurological Disease
    A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
  • 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-G0004
    Acetaminophen metabolite 3-hydroxy-acetaminophen

    3-Hydroxyacetaminophen

    Drug Metabolite Inflammation/Immunology
    3-hydroxy-acetaminophen is a metabolite of Acetaminophen, which is a pain medicine.
  • 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 (Ki = 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-B1583S
    (Z)-Capsaicin-d3

    TRP Channel HSV Neurological Disease
    (Z)-Capsaicin-d3 (Zucapsaicin-d3) is the deuterium labeled (Z)-Capsaicin. (Z)-Capsaicin is the cis isomer of capsaicin, acts as an orally active TRPV1 agonist, and is used in the research of neuropathic pain.
  • HY-131868
    TRPV3 antagonist 74a

    TRP Channel Neurological Disease
    TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain.
  • HY-17569
    Difluprednate

    Others Inflammation/Immunology
    Difluprednate(Durezol) is a corticosteroid, approved difluprednate for the treatment of post-operative ocular inflammation and pain.
  • HY-101582
    ZT 52656A hydrochloride

    Opioid Receptor Neurological Disease
    ZT 52656A is a selective kappa opioid agonist, used for the prevention or alleviation of pain in the eye.
  • HY-N6967
    Levomenol

    (-)-α-Bisabolol

    Others Inflammation/Immunology Neurological Disease
    Levomenol is a monocyclic sesquiterpene alcohol found in various plants and mainly in Matricaria chamomilla, which exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol has neuroprotective effects, can attenuate nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain.
  • HY-B1183
    Hydrocortisone acetate

    Hydrocortisone 21-acetate; Cortisol 21-acetate

    Glucocorticoid Receptor Endogenous Metabolite Inflammation/Immunology Endocrinology
    Hydrocortisone acetate is a corticosteroid, used to decrease swelling, itching, and pain that is caused by minor skin irritations or by hemorrhoids.
  • HY-B1462
    Chlorzoxazone

    Cytochrome P450 Inflammation/Immunology
    Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort.
  • HY-P1346
    APETx2

    Sodium Channel Inflammation/Immunology Neurological Disease
    APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.
  • HY-P1346A
    APETx2 TFA

    Sodium Channel Inflammation/Immunology Neurological Disease
    APETx2 TFA, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.
  • HY-B1079
    Suxibuzone

    Others Inflammation/Immunology
    Suxibuzone is a drug used for joint and muscular pain, is a prodrug of the non steroidal anti inflammatory drug Phenylbutazone.
  • HY-B2156
    Menaquinone-4

    Vitamin K2(MK-4); Menaquinone K4

    Endogenous Metabolite Cancer
    Menaquinone-4 is a vitamin K, used as a hemostatic agent, and also a adjunctive therapy for the pain of osteoporosis.
  • HY-105283
    PF 04531083

    Sodium Channel Neurological Disease
    PF 04531083 is a selective NaV1.8 blocker, and used for the research of neuropathic/inflammatory pain.
  • HY-16322
    Minodronic acid

    YM-529

    P2X Receptor Apoptosis Cancer
    Minodronic acid (YM-529) is a third-generation bisphosphonate that directly and indirectly prevents proliferation, induces apoptosis, and inhibits metastasis of various types of cancer cells. Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain.
  • 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-N0388
    Gelsemine

    Others Neurological Disease
    Gelsemine, an alkaloid from the Chinese herb Gelsemium elegans, is effective in mitigating chronic pain. Antinociceptive and hypnotic effects.
  • HY-N0313
    Euphol

    Endogenous Metabolite MAGL Inflammation/Immunology
    Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain.
  • HY-B1583
    (Z)-Capsaicin

    Zucapsaicin; Civamide; cis-Capsaicin

    TRP Channel HSV Neurological Disease
    (Z)-Capsaicin is the cis isomer of capsaicin, acts as an orally active TRPV1 agonist, and is used in the research of neuropathic pain.
  • HY-N5025
    Bullatine A

    P2X Receptor Apoptosis Cancer Inflammation/Immunology
    Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed.
  • HY-B0619
    Zaltoprofen

    CN100

    COX Inflammation/Immunology
    Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain.
  • HY-112430
    TRPM8 antagonist 2

    TRP Channel Neurological Disease
    TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
  • 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-117048
    PF-4191834

    PF-04191834

    Lipoxygenase Inflammation/Immunology
    PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain.
  • HY-19427A
    AZD9056 hydrochloride

    P2X Receptor Inflammation/Immunology
    AZD9056 hydrochloride is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.
  • 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-111029
    ALX-1393

    GlyT Neurological Disease
    ALX-1393, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model.
  • HY-N0021
    Verbascoside

    Acteoside; Kusaginin; TJC160

    PKC Apoptosis Bacterial HSV Cancer Inflammation/Immunology Neurological Disease
    Verbascoside is isolated from Lantana camara, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 µM, and has antitumor, anti-inflammatory and antineuropathic pain activity.
  • HY-139081
    GDC-0310

    Sodium Channel Neurological Disease
    GDC-0310 is a selective acyl-sulfonamide Nav1.7 inhibitor, with an IC50 of 0.6 nM for hNav1.7.
  • HY-114301A
    PF-06305591 dihydrate

    Sodium Channel Neurological Disease
    PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.
  • HY-76705
    Methyl N-methylanthranilate

    Others Others
    Methyl N-methylanthranilate, a terpene, is a pungent compound that can be found in Citrus reticulate Blanco leaves. Methyl N-methylanthranilate has the potential for pain research.
  • HY-125820
    Sigma-1 receptor antagonist 3

    Sigma Receptor Potassium Channel Neurological Disease
    Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC50 of 1.54 μM. Sigma-1 receptor antagonist 3 has the potential for the neuropathic pain.
  • HY-B0985
    Phenazopyridine hydrochloride

    Others Others
    Phenazopyridine hydrochloride is a chemical, which has a local analgesic effect, often used to alleviate the pain, irritation, discomfort, or urgency caused by urinary tract infections, surgery, or injury to the urinary tract.
  • HY-119373
    Cav 2.2 blocker 1

    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-14425
    NB001

    HTS 09836

    Adenylate Cyclase Neurological Disease
    NB001 (HTS 09836) is an adenylcyclase 1 (AC1) inhibitor which has effect on neural and non-neural pain by modulating AC1 activity.
  • HY-B1132
    Clidinium bromide

    Ro 2-3773

    mAChR Neurological Disease
    Clidinium bromide is a quaternary amine antimuscarinic agent. Clidinium bromide may help symptoms of cramping and abdominal/stomach pain by decreasing stomach acid, and slowing the intestines in vivo.
  • 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-N1469
    Kaurenoic acid

    Others Inflammation/Immunology Neurological Disease
    Kaurenoic acid is a diterpene from Sphagneticola trilobata, inhibits Inflammatory Pain by the inhibition of cytokine production and activation of the NO–cyclic GMP–PKG–ATP-sensitive potassium channel signaling pathway.
  • HY-P1220
    Huwentoxin-IV

    Sodium Channel Neurological Disease
    Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain.
  • HY-P1267
    α-Conotoxin PnIA

    nAChR Neurological Disease
    α-Conotoxin PnIA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
  • HY-10448
    Capsaicin

    (E)-Capsaicin

    TRP Channel Autophagy Apoptosis Cancer
    Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects.
  • HY-126382
    Hesperidin methylchalcone

    NF-κB Inflammation/Immunology
    Hesperidin methylchalcone (Hesperidin methyl chalcone) inhibits oxidative stress, cytokine production and NF-κB activation. Hesperidin methylchalcone inhibits inflammation and pain. Hesperidin methylchalcone exhibits vasoprotective activity.
  • HY-B0955
    Oxethazaine

    Oxetacaine

    HBV Neurological Disease
    Oxethazaine (Oxetacaine), a precursor of phentermine acidic, is an acid-resistent and orally active analgesic agent. Oxethazaine (Oxetacaine) has the potential for the relief of pain associated with peptic ulcer disease or esophagitis.
  • HY-U00325
    11β-HSD1-IN-1

    Others 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-P1267A
    α-Conotoxin PnIA TFA

    nAChR Neurological Disease
    α-Conotoxin PnIA TFA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
  • HY-P1220A
    Huwentoxin-IV TFA

    Sodium Channel Neurological Disease
    Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain.
  • HY-N0688
    Linderane

    Cytochrome P450 Inflammation/Immunology
    Linderane, isolated from the root of Lindera strychnifolia, is an irreversible inhibitor cytochrome P450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp.
  • HY-101789
    Nav1.7-IN-3

    Sodium Channel Neurological Disease
    Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
  • HY-131870
    GX-201

    Sodium Channel Inflammation/Immunology
    GX-201 is a selective NaV1.7 inhibitor, with an IC50 of <3.2 nM for hNaV1.7.
  • HY-101418
    JNJ-47965567

    P2X Receptor Neurological Disease
    JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology.
  • HY-15762
    Valdecoxib

    SC 65872

    COX Inflammation/Immunology
    Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain.
  • HY-100771
    PCC0208009

    Indoleamine 2,3-Dioxygenase (IDO) Cardiovascular Disease
    PCC0208009 is a potent IDO inhibitor with an IC50 value of 4.52 nM in HeLa cell. PCC0208009 alleviates neuropathic pain and comorbidities by regulating synaptic plasticity of anterior cingulate cortex (ACC) and amygdala .
  • HY-B1057
    Nefopam hydrochloride

    Fenazoxine hydrochloride

    β-catenin Neurological Disease
    Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo.
  • 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-N7601
    Benzoylalbiflorin

    Paeonivayin

    Others Inflammation/Immunology
    Benzoylalbiflorin, a monoterpenoid, is isolated from Radix Paeoniae Alba. Radix Paeoniae Alba is a traditional Chinese medicine that has been used for the research of rheumatoid arthritis, to alleviate inflammation, amenorrhea, epistaxis, abdominal pain, and other symptoms.
  • HY-B0683
    Limaprost

    17α,20-dimethyl-δ2-PGE1; ONO1206; OP1206

    PGE synthase Inflammation/Immunology Cardiovascular Disease
    Limaprost (OP1206) is a PGE1 analogue and a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost pain relief, has antianginal effects, and can be used for ischaemic symptoms research.
  • HY-111613
    Pinaverium bromide

    Calcium Channel Others
    Pinaverium bromide is an L-type calcium channel blocker with selectivity for the gastrointestinal tract, effectively relieves pain, diarrhea and intestinal discomfort, provides good therapeutic efficacies without significant adverse effects on Irritable bowel syndrome (IBS) patients.
  • HY-119447
    Mavacoxib

    COX Inflammation/Immunology
    Mavacoxib is a selective, oral long-acting cyclooxygenase-2 (COX-2) inhibitor and a long-acting non-steroidal anti-inflammatory drug (NSAID). Mavacoxib is used to treat pain and inflammation associated with degenerative joint disease in dogs.
  • HY-124283A
    LEI-101

    Cannabinoid Receptor Neurological Disease
    LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors.
  • HY-137563
    A2793

    Potassium Channel Neurological Disease
    A2793 is an efficient dual TWIK-related acid-sensitive K + channel (TASK)-1/TRESK inhibitor, with an IC50 of 6.8 μM for mTRESK. A2764 is more selective for TRESK, and it only moderately influences TREK-1 and TALK-1.
  • HY-B0578
    Loxoprofen

    COX Inflammation/Immunology
    Loxoprofen is a non-steroidal anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively.
  • HY-B0578A
    Loxoprofen sodium

    COX Inflammation/Immunology
    Loxoprofen sodium is a non-steroidal anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively.
  • HY-B1057S
    Nefopam D3 hydrochloride

    β-catenin Neurological Disease
    Nefopam D3 hydrochloride is the deuterium labeled Nefopam hydrochloride. Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo.
  • HY-133115
    N-Desmethylnefopam

    β-catenin Neurological Disease
    N-Desmethylnefopam is the main metabolite of Nefopam. N-Desmethylnefopam is a centrally-acting but non-opioid analgesic agent, for the relief of moderate to severe pain. Nefopam targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo.
  • HY-P0062
    Ziconotide

    Calcium Channel Neurological Disease
    Ziconotide is an analgesic agent and has been used to treat neuropathic and non-neuropathic pain. Ziconotide acts by binding to N-type calcium channels situated on the terminal part of primary afferent neurons of the nociceptive pathway therefore reducing synaptic transmission with potent antinociceptive effects.
  • HY-B0262
    Methocarbamol

    Sodium Channel Neurological Disease
    Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research.
  • HY-P1091
    Hemopressin (human, mouse)

    Cannabinoid Receptor Neurological Disease
    Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models.
  • HY-13988
    AT-56

    PGE synthase Inflammation/Immunology
    AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2.
  • HY-B2156S
    Menaquinone-4-d7

    Endogenous Metabolite Cancer
    Menaquinone-4-d7 (Vitamin K2(MK-4)-d7) is the deuterium labeled Menaquinone-4. Menaquinone-4 is a vitamin K, used as a hemostatic agent, and also a adjunctive therapy for the pain of osteoporosis.
  • HY-B0955S
    Oxethazaine-d6

    HBV Neurological Disease
    Oxethazaine-d6 (Oxetacaine-d6) is the deuterium labeled Oxethazaine. Oxethazaine (Oxetacaine), a precursor of phentermine acidic, is an acid-resistent and orally active analgesic agent. Oxethazaine (Oxetacaine) has the potential for the relief of pain associated with peptic ulcer disease or esophagitis.
  • HY-P0062A
    Ziconotide TFA

    Calcium Channel Neurological Disease
    Ziconotide TFA is an analgesic agent and has been used to treat neuropathic and non-neuropathic pain. Ziconotide TEA acts by binding to N-type calcium channels situated on the terminal part of primary afferent neurons of the nociceptive pathway therefore reducing synaptic transmission with potent antinociceptive effects.
  • HY-N1478
    Gardenoside

    Others Neurological Disease
    Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis.
  • HY-P1216A
    HS014 TFA

    Melanocortin Receptor Neurological Disease
    HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA modulates the behavioral effects of morphine in mice. HS014 TFA increases food intake in free-feeding rats.
  • HY-111274
    Indomethacin farnesil

    Indometacin farnesil

    COX Autophagy Inflammation/Immunology
    Indomethacin farnesil is an orally active prodrug of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.
  • HY-134189A
    EST73502 hydrochloride

    Sigma Receptor Opioid Receptor Neurological Disease
    EST73502 hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 hydrochloride has antinociceptive activity.
  • HY-136207
    TC-2559 difumarate

    nAChR Neurological Disease
    TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
  • HY-134189
    EST73502

    Opioid Receptor Sigma Receptor Neurological Disease
    EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.
  • HY-P1090
    Hemopressin(rat)

    Cannabinoid Receptor Neurological Disease
    Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models.
  • HY-P1091A
    Hemopressin(human, mouse) TFA

    Cannabinoid Receptor Neurological Disease
    Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models.
  • HY-110199
    TC-I 2014

    TRP Channel Neurological Disease
    TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models.
  • HY-135731
    4-Methylamino antipyrine

    COX Drug Metabolite Inflammation/Immunology
    4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties.
  • HY-B1320
    Meclofenamic acid sodium

    Meclofenamate sodium

    Gap Junction Protein Inflammation/Immunology
    Meclofenamic acid (Meclofenamate) sodium is a nonsteroidal anti-inflammatory drug (NSAID) approved for use in arthritis (osteo and rheumatoid), analgesia (mild to moderate pain), dysmenorrhea, and heavy menstrual blood loss (menorrhagia). Meclofenamic acid sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor.
  • HY-B0262S1
    Methocarbamol-d3

    Sodium Channel Neurological Disease
    Methocarbamol-d3 is the deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research.
  • HY-109127
    Berotralstat

    Others Others
    Berotralstat (BCX7353) is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.
  • HY-135731A
    4-Methylamino antipyrine hydrochloride

    COX Drug Metabolite Inflammation/Immunology
    4-Methylamino antipyrine hydrochloride is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine hydrochloride has analgesic, antipyretic, and relatively weak antiinflammatory properties.
  • HY-P1090A
    Hemopressin(rat) TFA

    Cannabinoid Receptor Neurological Disease
    Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models.
  • HY-12741
    LDN-212320

    LDN-0212320; OSU-0212320

    EAAT2 Neurological Disease
    LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC[1]
  • HY-P1216
    HS014

    Melanocortin Receptor Neurological Disease
    HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.
  • HY-12811
    PF-04856264

    Sodium Channel Neurological Disease
    PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect.
  • HY-N2333
    Resiniferatoxin

    (+)-Resiniferatoxin

    TRP Channel Cardiovascular Disease
    Resiniferatoxin ((+)-Resiniferatoxin), derived from the Euphorbia resinifera plant, is a selective transient receptor potential vanilloid 1 (TRPV1) receptor agonist. Resiniferatoxin eliminates TRPV1+ primary sensory afferents and blunt cardiac sympathetic afferent reflex for a relatively long period.
  • HY-121235
    Clonixin

    SCH-10304

    Others Inflammation/Immunology
    Clonixin (SCH-10304) is an orally active analgesic and a non-steroidal anti-inflammatory agent in rodents.
  • HY-135891
    AZD2423

    CCR Neurological Disease
    AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
  • HY-110285
    ML382

    Others Neurological Disease
    ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM.
  • HY-N2573
    Corydalmine

    L-Corydalmine

    Fungal CXCR Infection Neurological Disease
    Corydalmine (L-Corydalmine) inhibits spore germination of some plant pathogenic as well as saprophytic fungi. Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity. Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway.
  • HY-16781
    Grapiprant

    CJ-023423; RQ-00000007; AAT-007

    Prostaglandin Receptor Metabolic Disease Endocrinology
    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[3] .
  • HY-13954
    A 839977

    P2X Receptor Neurological Disease Inflammation/Immunology
    A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.
  • HY-12844
    Ro 64-6198

    Opioid Receptor Neurological Disease
    Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia.
  • HY-100933
    MY-5445

    Phosphodiesterase (PDE) Cancer Inflammation/Immunology Cardiovascular Disease
    MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a Ki of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect.
  • HY-110302
    6'-GNTI dihydrochloride

    Opioid Receptor Neurological Disease
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.
  • HY-135412
    N-Methyl Duloxetine hydrochloride

    Sodium Channel Neurological Disease
    N-Methyl Duloxetine hydrochloride is an analgesic. N-Methyl Duloxetine (hydrochloride) elicits both tonic and use-dependent block of neuronal Na + channels.
  • HY-119243
    LY2794193

    mGluR Neurological Disease
    LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 Ki=0.927 nM,EC50=0.47 nM; hmGlu2 Ki=412 nM,EC50=47.5 nM).
  • HY-136363
    MDR-652

    TRP Channel Neurological Disease
    MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity.
  • HY-11079
    A-803467

    Sodium Channel Inflammation/Immunology Neurological Disease
    A-803467 is a potent and selective tetrodotoxin-resistant Nav1.8 sodium channel blocker (IC50=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter.
  • HY-115681
    (2R/S)-6-PNG

    6-Prenylnaringenin

    Calcium Channel Neurological Disease
    (2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca 2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice.
  • HY-N0451
    Acacetin

    5,7-Dihydroxy-4'-methoxyflavone

    Apoptosis Autophagy Cancer Inflammation/Immunology Neurological Disease
    Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Tephroseris kirilowii (Turcz.) Holub. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research.
  • HY-117626
    LP-935509

    Others Inflammation/Immunology Neurological Disease
    LP-935509 is a selective, ATP-competitive and brain-penetrant inhibitor of adapter protein-2 associated kinase 1 (AAK1) with an IC50 and a Ki of 3.3 nM and 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 is highly brain-penetrant and reverses fully established pain behavior following the SNL procedure.
  • HY-115510
    SPR inhibitor 3

    SPRi3

    Others Inflammation/Immunology
    SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels.
  • HY-135816
    CK2/PIM1-IN-1

    Casein Kinase Pim Cancer Inflammation/Immunology
    CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1, with IC50s of 3.787 μM and 4.327 μM for CK2 and PIM1, respectively. CK2/PIM1-IN-1 is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.
  • HY-110143
    CLP257

    Potassium Channel Neurological Disease
    CLP257 is a selective K +-Cl cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.
  • HY-B0683S
    Limaprost-d3

    PGE synthase Inflammation/Immunology Cardiovascular Disease
    Limaprost-d3 (17α,20-dimethyl-δ2-PGE1-d3) is the deuterium labeled Limaprost. Limaprost (OP1206) is a PGE1 analogue and a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost pain relief, has antianginal effects, and can be used for ischaemic symptoms research.
  • HY-122575
    Aurintricarboxylic acid

    P2X Receptor Influenza Virus Topoisomerase MicroRNA Apoptosis Infection Inflammation/Immunology Neurological Disease
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM.
  • HY-W014421
    AP-18

    TRP Channel Neurological Disease
    AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM.
  • HY-108425A
    AMG8380

    Sodium Channel Neurological Disease
    AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM.
  • HY-B0161A
    Duloxetine hydrochloride

    (S)-Duloxetine hydrochloride; LY-248686 hydrochloride

    Serotonin Transporter Neurological Disease
    Duloxetine hydrochloride ((S)-Duloxetine hydrochloride) is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).
  • HY-B0161
    Duloxetine

    (S)-Duloxetine; LY248686

    Serotonin Transporter Neurological Disease
    Duloxetine is a serotonin-norepinephrine reuptake inhibitor with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).
  • HY-135871
    BMT-124110

    Others Neurological Disease
    BMT-124110 is a potent, selective AAK1 inhibitor with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively.
  • HY-12152
    PNU-120596

    NSC 216666

    nAChR Inflammation/Immunology Neurological Disease
    PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC50 of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research.
  • HY-101290
    BMT-090605

    Others Neurological Disease
    BMT-090605 is a potent, selective AAK1 inhibitor, with an IC50 of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 45 and 60 nM, respectively.
  • HY-13106
    Olodanrigan

    EMA401; PD-126055

    Angiotensin Receptor Neurological Disease Endocrinology
    Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
  • HY-110220
    CIM0216

    TRP Channel Neurological Disease
    CIM0216, a synthetic TRPM3 ligand, acts as a potent and selective agonist of TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts in a TRPM3-dependent manner to induce pain and evoke neuropeptide release from sensory nerve terminals in vitro. CIM0216 is a powerful tool for studies of the physiological functions of TRPM3, and can be used for neurogenic inflammation research.
  • HY-B0527A
    Amitriptyline hydrochloride

    Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor Neurological Disease
    Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.
  • HY-108425B
    (Rac)-AMG8379

    (Rac)-AMG8380

    Sodium Channel Neurological Disease
    (Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379. AMG8379 is a potent, orally active and selective sulfonamide antagonist of NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively .
  • HY-B0161AS
    Duloxetine D3 hydrochloride

    (S)-Duloxetine D3 hydrochloride; LY248686 D3 hydrochloride

    Serotonin Transporter Neurological Disease
    Duloxetine D3 hydrochloride ((S)-Duloxetine D3 hydrochloride) is a deuterium labeled Duloxetine hydrochloride. Duloxetine hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).
  • HY-133529
    PA-8

    Others Inflammation/Immunology Neurological Disease
    PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC50 of 2 nM.
  • HY-B0336
    Pranoprofen

    COX Apoptosis PGE synthase Cancer Inflammation/Immunology
    Pranoprofen is a non-steroidal anti-inflammatory agent (NSAID) for the research of keratitis or other ophthalmology diseases. Pranoprofen inhibit COX-1 and COX-2 enzymes, thus blocking arachidonic acid converted to eicosanoids and reducing prostaglandins synthesis.
  • HY-11048
    NS11394

    GABA Receptor Neurological Disease
    NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.
  • HY-108425
    AMG8379

    Sodium Channel Neurological Disease
    AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM.
  • HY-136362
    ARRY-382

    c-Fms Cancer Inflammation/Immunology
    ARRY-382 is a potent, oral and highly selective inhibitor of CSF1R/c-Fms with an IC50 of 9 nM. ARRY-382 can be used for the research of advanced or metastatic cancers.
  • HY-126291
    GNE-616

    Sodium Channel Neurological Disease
    GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd 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-136208
    TAN-452

    Opioid Receptor Neurological Disease
    TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
  • HY-105285
    Piromelatine

    Neu-P11

    Melatonin Receptor 5-HT Receptor P2X Receptor TRP Channel Sodium Channel Neurological Disease
    Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.
  • HY-125777A
    α-Conotoxin Vc1.1 TFA

    nAChR Neurological Disease
    α-Conotoxin Vc1.1 TFA is a disulfide-bonded peptide isolated from Conus victoriae and is a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM, respectively, and has less inhibitory effect on other nAChR subtypes. α-Conotoxin Vc1.1 TFA has the potential for neuropathic pain reserach.
  • HY-17387
    (-)-Huperzine A

    Huperzine A

    AChE Apoptosis iGluR Neurological Disease
    (-)-Huperzine A (Huperzine A) is an alkaloid isolated from a Chinese club moss, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
  • HY-136535
    hTrkA-IN-1

    Trk Receptor Inflammation/Immunology
    hTrkA-IN-1 is a potent and orally active inhibitor of TrkA kinase with an IC50 of 1.3 nM, compound 2. extracted from patent WO2015175788. hTrkA-IN-1 can be used for the study of inflammatory disease, such as prostatitis, pelvic, et al.