30 Results for "

analgesic efficacy

" in MedChemExpress (MCE) Product Catalog:
Products (30)

30 Results for "analgesic efficacy" in MCE Product Catalog:

5
5 Cited Publications
Cat. No.: HY-P1290
CAS No.: 121932-06-7
Synonyms: PKI-(6-22)-amide
Target:  

PKA

Research Areas:  

Neurological Disease

PKA Inhibitor Fragment (6-22) amide is a highly potent and specific competitive inhibitor of PKA, with Ki values of 1.7 nM and 1.6 nM against human and bovine PKA catalytic subunits, respectively. The IC50 of PKA Inhibitor Fragment (6-22) amide targeting bovine PKA is 8.6 nM. PKA Inhibitor Fragment (6-22) amide effectively abolishes PKA activity in mouse brain and spinal cord, and exerts in vivo efficacy via intracerebroventricular administration. PKA Inhibitor Fragment (6-22) amide significantly reverses low-dose morphine analgesic tolerance in mice and blocks photoaffinity labeling of cAMP-dependent protein kinase. PKA Inhibitor Fragment (6-22) amide can be applied to research in fields related to the mechanism of morphine analgesic tolerance and skin wound healing .
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1
1 Cited Publications
Cat. No.: HY-N5084
CAS No.: 205370-59-8
Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside is a TRPV1 antagonist and HDAC7 inhibitor. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside blocks TRPV1-mediated calcium influx, suppresses phosphorylation of p65, IκBα, p38, JNK, and ERK1/2, inhibiting NF-κB and MAPK signaling cascades. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside reduces production and gene expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside exhibits potent analgesic activity, elevates thermal pain threshold and mechanical pain threshold in murine models. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside restores CD8 + T cell infiltration into bladder cancer tumors and improves bladder cancer immunotherapy efficacy. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside can be used for the researches of painand bladder cancer .
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Cat. No.: HY-118952A
CAS No.: 1834610-75-1
Purity:  99.38%
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

PF-06456384 trihydrochloride is an extremely potent and selective Nav1.7 sodium channel blocker (IC50: 0.01 nM for hNaV1.7; 75 nM for rNaV1.7; <0.1 nM for mNaV1.7). PF-06456384 trihydrochloride shows no significant analgesic efficacy in the mouse Formalin pain model .
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Cat. No.: HY-107405
CAS No.: 1211866-85-1
Purity:  99.67%
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain .
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Cat. No.: HY-146334
CAS No.: 2966044-07-3
Purity:  99.25%
DFBTA is an orally active and potent ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain .
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Cat. No.: HY-115597
CAS No.: 2413939-89-4
Purity:  98.90%
Target:  

Calcium Channel

Research Areas:  

Neurological Disease

BTT-266 is an antagonist forcalcium channel, through suppression of the CaVα1-AID-CaVβ3 interaction, with a Ki of 1.4 μM. BTT-266 modulates the activation of voltage-dependent CaV2.2. BTT-266 exhibits analgesic efficacy against neuropathic pain in rats model .
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Cat. No.: HY-103212A
CAS No.: 147663-20-5
Purity:  95.35%
Synonyms: B-HT 933 hydrochloride; Oxazoloazepin hydrochloride
Target:  

Adrenergic Receptor

Research Areas:  

Cardiovascular Disease

Azepexole hydrochloride (B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride) is a selective agonist for α 2-adrenoceptor, with pKi of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions with IC50 of 78.72 nM. Azepexole hydrochloride exhibits antitussive and analgesic efficacy .
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Cat. No.: HY-103461
CAS No.: 1143578-94-2
Purity:  99.70%
Target:  

FAAH

Research Areas:  

Neurological Disease

FAAH-IN-6 (compound 21d) is a potent, orally active and cross the blood-brain barrier fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 0.72, 0.28 nM for hFAAH, rFAAH, respectively. FAAH-IN-6 shows dose-dependent analgesic efficacy in animal models of both neuropathic and inflammatory pain .
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Cat. No.: HY-P991622
MNAC13 is a kind of mouse IgG1 chimeric antibody, targeting to human TrkA. MNAC13 inhibits the NGF dependent signaling pathway by specifically binding to TrkA receptors. MNAC13 has good analgesic effect and long-lasting efficacy. MNAC13 can be used for researches on inflammatory and chronic pain .
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Cat. No.: HY-135495
CAS No.: 1642113-59-4
AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing .
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Cat. No.: HY-16525
CAS No.: 701909-57-1
XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating α2-adrenergic receptor at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research .
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Cat. No.: HY-107085
CAS No.: 67489-39-8
Target:  

COX

Research Areas:  

Inflammation/Immunology

Talmetacin exhibits anti-inflammatory and analgesic efficacy .
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Cat. No.: HY-169215
Target:  

COX

Research Areas:  

Neurological Disease

Anti-inflammatory agent 93 (compund 2g) is an imidazole derivative of Schiff base with analgesic and anti-inflammatory activities. Anti-inflammatory agent 93 targets COX-2 receptor and produces 89% analgesic efficacy in mice at 100 mg/kg .
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Cat. No.: HY-N12398
CAS No.: 52617-25-1
Psychotridine is a natural alkaloid isolated from Psychotria colorata, reveals an analgesic activity in nervous system and an inhibitory efficacy towards platelet aggregation .
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Cat. No.: HY-116149
CAS No.: 1335145-56-6
Target:  

nAChR

Research Areas:  

Others

A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.
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Cat. No.: HY-111258
CAS No.: 869499-38-7
GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain .
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Cat. No.: HY-115133
CAS No.: 1008529-42-7
Target:  

TRP Channel

Research Areas:  

Neurological Disease

ABT-116 is an orally active antagonist of transient receptor potential vanilloid type 1 (TRPV1). ABT-116 has analgesic efficacy. ABT-116 can be used for the research of neurological disease .
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Cat. No.: HY-120481
CAS No.: 1184847-16-2
Target:  

FAAH

Research Areas:  

Neurological Disease

JNJ-40413269 is an inhibitor for FAAH, that inhibits human FAAH and rats FAAH with IC50 of 28 nM and 270 nM. JNJ-40413269 exhibits analgesic efficacy in rat spinal nerve ligation model and exhibits good pharmacokinetic characteristics in rats .
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Cat. No.: HY-P1253
CAS No.: 59004-96-5
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

α-Endorphin (human) is a neuropeptide, that acts on the central nervous system (CNS) and peripheral nervous system (PNS). α-Endorphin (human) binds μ-opioid receptor, and exhibits analgesic efficacy. α-Endorphin (human) regulates sexual behaviors and pleasure felling .
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Cat. No.: HY-167734
CAS No.: 114716-16-4
Synonyms: AY-30715
Target:  

COX

Research Areas:  

Inflammation/Immunology

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