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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
18 Results for "
mechanical hypersensitivity
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "mechanical hypersensitivity" in MCE Product Catalog:
3
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S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .
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2 Cited Publications
Synonyms: T-Type calcium channel inhibitor
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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] .
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1 Cited Publications
Synonyms: R-75231; R88021
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Draflazine (R-75231) is a ENT1 inhibitor. Draflazine (R-75231) completely reverses the hypersensitivity in the complete Freund’s adjuvant (CFA) model of mechanical hyperalgesia and the carrageenan inflammation model of thermal and mechanical hyperalgesia .
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1 Cited Publications
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DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects .
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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 .
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AB21 hydrochloride is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 hydrochloride has the effect of reducing mechanical hypersensitivity .
Cat. No.: HY-117731
CAS No.: 2113664-14-3
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UKH-1114 is a selective TMEM97 (a sigma-2 receptor) agonist with a Ki 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 .
Cat. No.: HY-167862A
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UCM-05194 (ammonium) is a lysophosphatidic acid receptor 1 (LPA1) agonist. UCM-05194 (ammonium) induces calcium mobilization in LPA1-expressing RH7777 cells (EC50 = 0.24 µM). UCM-05194 (ammonium) induces neurite retraction and migration in LPA1-overexpressing B103 rat neuroblastoma cells. UCM-05194 (ammonium) attenuates acetic acid-induced writhing and hind paw mechanical hypersensitivity in mice .
Cat. No.: HY-149854
CAS No.: 3026677-23-3
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AB21 is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 has the effect of reducing mechanical hypersensitivity .
Cat. No.: HY-149854A
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AB21 oxalate is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 oxalate has the effect of reducing mechanical hypersensitivity .
Cat. No.: HY-149863
CAS No.: 3017181-08-4
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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 .
Cat. No.: HY-119519
CAS No.: 300689-25-2
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OB-2 is a STOML3 oligomerization blocker. OB-2 reverses pathological mechanical hypersensitivity. OB-2 can be used for research of painful diabetic neuropathy in mice .
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Cat. No.: HY-P5914
CAS No.: 2569291-86-5
Synonyms: WaTx
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Cat. No.: HY-P5914A
Synonyms: WaTx TFA
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Cat. No.: HY-168166
CAS No.: 2489231-47-0
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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 .
Cat. No.: HY-10035R
CAS No.: 1072018-68-8
Synonyms: T-Type calcium channel inhibitor (Standard)
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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> .
Cat. No.: HY-110268
CAS No.: 1029521-30-9
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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) .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
