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Results for "

hypersensitive pain

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Adenosine Receptor (1) Adrenergic Receptor (1) Akt (1) Apoptosis (1) c-Myc (1) Calcium Channel (3) CXCR (2) Endogenous Metabolite (3) Epigenetic Reader Domain (1) ERK (1) HDAC (1) iGluR (2) Interleukin Related (2) Keap1-Nrf2 (2) Mas-related G-protein-coupled Receptor (MRGPR) (2) Melanocortin Receptor (2) Monoamine Oxidase (2) nAChR (1) Neurotensin Receptor (1) NF-κB (1) NO Synthase (1) P2X Receptor (1) p38 MAPK (1) Potassium Channel (2) Reactive Oxygen Species (ROS) (1) Reference Standards (2) Sigma Receptor (2) TNF Receptor (1) TRP Channel (1) TSPO (1)
By Research Areas:	Cancer (3) Inflammation/Immunology (15) Metabolic Disease (2) Neurological Disease (20)

By Targets:

5-HT Receptor (2)

Adenosine Receptor (1)

Adrenergic Receptor (1)

Akt (1)

Apoptosis (1)

c-Myc (1)

Calcium Channel (3)

CXCR (2)

Endogenous Metabolite (3)

Epigenetic Reader Domain (1)

ERK (1)

HDAC (1)

iGluR (2)

Interleukin Related (2)

Keap1-Nrf2 (2)

Mas-related G-protein-coupled Receptor (MRGPR) (2)

Melanocortin Receptor (2)

Monoamine Oxidase (2)

nAChR (1)

Neurotensin Receptor (1)

NF-κB (1)

NO Synthase (1)

P2X Receptor (1)

p38 MAPK (1)

Potassium Channel (2)

Reactive Oxygen Species (ROS) (1)

Reference Standards (2)

Sigma Receptor (2)

TNF Receptor (1)

TRP Channel (1)

TSPO (1)

By Research Areas:

Cancer (3)

Inflammation/Immunology (15)

Metabolic Disease (2)

Neurological Disease (20)

Inhibitors & Agonists

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-10035

TTA-P2 2 Publications Verification T-Type calcium channel inhibitor	Calcium Channel	Neurological Disease
TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC₅₀ = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy < sup>[4] .

HY-18099

S1RA 3 Publications Verification E-52862	Sigma Receptor 5-HT Receptor	Neurological Disease
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with K_is of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT_2B receptor (K_i= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .

HY-100375

Diroximel fumarate 4 Publications Verification ALKS 8700; BIIB098	Keap1-Nrf2	Inflammation/Immunology
Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) proagent in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS). Diroximel fumarate is a Nrf2 activator that alleviate MGO-induced pain hypersensitivity .

HY-106199

Adenosine A1 receptor activator T62 1 Publications Verification	Adenosine Receptor	Neurological Disease Inflammation/Immunology
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-P1726

MSG606	Melanocortin Receptor	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
MSG606 is a selective melanocortin 1 receptor (MC1R) antagonist. MSG606 can abolish the neuroprotective effects of BMS-470539 (HY-15616) (MC1R agonist). MSG606 can inhibit cancer cell proliferation and transition from the G1 to the S phase. MSG606 can delay pain hypersensitivity and reduce cholesterol levels. MSG606 can be used for the researches of cancer, inflammation, neurological and metabolic disease, such as breast cancer and subarachnoid hemorrhage (SAH) .

HY-N5025

Bullatine A	P2X Receptor Apoptosis ERK p38 MAPK c-Myc NF-κB Reactive Oxygen Species (ROS)	Neurological Disease Inflammation/Immunology Cancer
Bullatine A, a diterpenoid alkaloid, is a potent P2X7 antagonist. Bullatine A possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A inhibits ATP-induced BV-2 cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A suppresses glioma cell growth by targeting SIRT6. Bullatine A specifically attenuates pain hypersensitivity in rats. Bullatine A attenuates LPS (HY-D1056)-induced systemic inflammatory response by inhibiting the ROS/JNK/NF-κB pathway in mice. Bullatine A improves despair behavior in Chronic chronic social defeat stress (CSDS) mice. Bullatine A can be used for the study of inflammation, glioblastoma (GBM) and depression .

HY-148244

MS47134 1 Publications Verification	Mas-related G-protein-coupled Receptor (MRGPR)	Others
MS47134 is a potent and selective MRGPRX4 agonist with an EC₅₀ value of 149 nM. MS47134 can be used for research of pain, itch and mast cell-mediated hypersensitivity .

HY-117731

UKH-1114	Sigma Receptor	Neurological Disease
UKH-1114 is a selective TMEM97 (a sigma-2 receptor) agonist with a K_i values of 1279 and 46 nM for σ1R and σ2R/TMEM97, respectively. UKH-1114 exhibits exceptional selectivity with negligible affinity for over 50 other receptors and channels. UKH-1114 effectively relieves spared nerve injury (SNI)-induced mechanical hypersensitivity with a long-lasting duration and without motor impairment. UKH-1114 can be used for neuropathic pain research .

HY-175231

ST171	5-HT Receptor	Neurological Disease
ST171 is a bitopic 5-HT1AR agonist with an K_i of 0.41  nM. ST171 selectively activates G_i/o signaling pathway and inhibits 5-HT1AR-mediated cAMP accumulation without G_s activation and marginal β-arrestin recruitment. T171 reduces hypersensitivity in chronic neuropathic and inflammatory pain mice model. ST171 can be used for pain research .

HY-110099

(±)-NBI-74330	CXCR	Inflammation/Immunology
(±)-NBI-74330 is a potent and selective CXCR3 antagonist. (±)-NBI-74330 not only reduces tactile and thermal hypersensitivity but also enhances the analgesic properties of morphine. (±)-NBI-74330 can reduce microglial cell activation, increase astroglial cell activation, and downregulate the expression of some CXCR3 ligands in a rat neuropathic pain model .

HY-143880

MRGPRX1 agonist 4	Mas-related G-protein-coupled Receptor (MRGPR)	Neurological Disease
MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC₅₀ value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain .

HY-P10767

MD01-67	Neurotensin Receptor	Neurological Disease
MD01-67 is a selective macrocyclic compound targeting the neurotensin receptor type 2 (NTS2), with K_i of 2.9 nM. MD01-67 exhibits analgesic and tactile hypersensitivity reducing activity in rats acute/persistent/chronic inflammatory pain models .

HY-P1726A

MSG606 TFA	Melanocortin Receptor	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
MSG606 TFA is a selective melanocortin 1 receptor (MC1R) antagonist. MSG606 TFA can abolish the neuroprotective effects of BMS-470539 (HY-15616) (MC1R agonist). MSG606 TFA can inhibit cancer cell proliferation and transition from the G1 to the S phase. MSG606 TFA can delay pain hypersensitivity and reduce cholesterol levels. MSG606 TFA can be used for the researches of cancer, inflammation, neurological and metabolic disease, such as breast cancer and subarachnoid hemorrhage (SAH) .

HY-175340

Kv7.2/Kv7.3 activator-3	Potassium Channel TSPO	Neurological Disease
Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC₅₀ values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with K_i values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons .

HY-P5874

Myr-TAT-CBD3	Calcium Channel	Inflammation/Immunology
Myr-TAT-CBD3 is CRMP2-CaV2.2 interaction inhibitor. Myr-tat-CBD3 can significantly attenuate carrageenan-induced thermal hypersensitivity and reverse thermal hypersensitivity induced in a rat model of postoperative pain. Myr-TAT-CBD3 can be used to study inflammation and postoperative pain .

HY-117518A

Paranyline hydrochloride	Endogenous Metabolite	Inflammation/Immunology
Paranyline hydrochloride is an anti-inflammatory agent with topical antiallodynic activity .

HY-149863

DDO-8926	Epigenetic Reader Domain	Neurological Disease
DDO-8926 is a potent and selective BET inhibitor that can significantly reduce mechanical hypersensitivity by inhibiting the expression of pro-inflammatory cytokines and reducing excitability for neuropathic pain research .

HY-101440A

Indantadol hydrochloride CHF-3381	iGluR Monoamine Oxidase	Neurological Disease
Indantadol hydrochloride (CHF-3381) is an orally active, non-selective NMDA antagonist and MAO inhibitor. Indantadol hydrochloride blocks the binding of [³H]-MK-801 to NMDA receptors in a non-competitive manner, with an IC₅₀ of 8.1 μM. Indantadol hydrochloride completely inhibits dopamine release caused by NMDA. Indantadol hydrochloride protects neurons, with an ED₅₀ of 35 μM. Indantadol hydrochloride has anticonvulsant and anti-high pain hypersensitivity activities .

HY-168166

CHET3	Endogenous Metabolite	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-169780

(S)-AMG-628	TRP Channel	Neurological Disease Inflammation/Immunology
(S)-AMG-628 (Compound 16q) is the S-isomer of AMG-628 (HY-123374). (S)-AMG-628 is the orally active antagonist for TRPV1, that inhibits the Capsaicin (HY-10448)- and acid-induced Ca ²⁺-influx with IC₅₀ of 7 nM and 5 nM in CHO cell. (S)-AMG-628 ameliorates Capsaicin-induced rats flinching, and reverses the thermal hypersensitivity in CFA-(HY-153808) induced inflammatory pain models .

HY-118935

NGD9002 free base	Adrenergic Receptor	Inflammation/Immunology
NGD9002 free base is a new generation of selective corticotropin-releasing factor-1 (CRF-1) receptor antagonist with inhibitory activity on CRF-induced colonic function stimulation. NGD9002 free base can reduce CRF-induced fecal output response and show an inhibitory IC50 value of 4.3 mg/kg. NGD9002 free base can effectively block CRF-induced colonic secretory motility stimulation at the highest dose and reduce acute water avoidance-induced defecation. NGD9002 free base can also prevent the occurrence of pain hypersensitivity reactions to repeated colonic distension .

HY-15026

ATB 429	Endogenous Metabolite	Inflammation/Immunology
ATB-429, a novel H2S-releasing derivative of mesalamine, demonstrates significant anti-nociceptive and anti-inflammatory effects in models of irritable bowel syndrome (IBS). By releasing hydrogen sulfide (H2S), ATB-429 modulates colorectal distension-induced hypersensitivity in both healthy and postcolitic rats. It attenuates abdominal withdrawal responses and suppresses spinal c-Fos mRNA expression, indicating its potential to alleviate pain associated with gastrointestinal inflammation. Moreover, ATB-429 down-regulates colonic cyclooxygenase-2 and interleukin-1β mRNA expression, effects not observed with mesalamine alone. The mechanism involves ATP-sensitive K+ (KATP) channels, as evidenced by reversal of ATB-429's effects with glibenclamide. These findings suggest ATB-429 could offer therapeutic benefits for managing painful intestinal disorders linked to inflammation .

HY-10035R

TTA-P2 (Standard) T-Type calcium channel inhibitor (Standard)	Calcium Channel Reference Standards	Neurological Disease
TTA-P2 (Standard) is the analytical standard of TTA-P2 (HY-10035). This product is intended for research and analytical applications. TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy < sup> .

HY-N18367

Lemairamin Wgx-50	nAChR Interleukin Related Akt	Neurological Disease Inflammation/Immunology
Lemairamin (Wgx-50) is a hydroxylamine compound. Lemairamin can be isolated from the pericarps of the Zanthoxylum plants. Lemairamin activates α7nAChR, stimulates the expression of IL-10 and POMC. Lemairamin shows a decrease in Akt. Lemairamin attenuates DSS-induced intestinal inflammation. Lemairamin alleviates pain hypersensitivity .

HY-110268

NVP CXCR2 20	CXCR	Inflammation/Immunology
NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD) .

HY-101440

Indantadol CHF-3381 free base	iGluR Monoamine Oxidase	Neurological Disease
Indantadol (the free base of CHF-3381) is an orally active, non-selective NMDA antagonist and MAO inhibitor. Indantadol blocks the binding of [³H]-MK-801 to NMDA receptors in a non-competitive manner, with an IC₅₀ of 8.1 μM. Indantadol completely inhibits dopamine release caused by NMDA. Indantadol protects neurons, with an ED₅₀ of 35 μM. Indantadol has anticonvulsant and anti-high pain hypersensitivity activities .

HY-182777

HDAC6-IN-80	HDAC NO Synthase TNF Receptor Interleukin Related	Neurological Disease Inflammation/Immunology
HDAC6-IN-80 is an orally active, selective HDAC6 inhibitor with an IC₅₀ of 8.5 nM. HDAC6-IN-80 inhibits lipopolysaccharide-induced microglial activation, reduces the levels of iNOS, COX-2, TNF-α and IL-6, and alleviates sensory hypersensitivity behaviors. HDAC6-IN-80 can be used for the research of inflammatory pain and chemotherapy-induced peripheral neuropathy .

HY-100375R

Diroximel fumarate (Standard) ALKS 8700 (Standard); BIIB098 (Standard)	Reference Standards Keap1-Nrf2	Inflammation/Immunology
Diroximel fumarate (Standard) is the analytical standard of Diroximel fumarate (HY-100375). This product is intended for research and analytical applications. Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) proagent in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS). Diroximel fumarate is a Nrf2 activator that alleviate MGO-induced pain hypersensitivity .

Cat. No.	Product Name	Target	Research Area