59 Results for "

constriction

" in MedChemExpress (MCE) Product Catalog:
Products (59)

59 Results for "constriction" in MCE Product Catalog:

Cat. No.: HY-135871A
Target:  

AAK1

Research Areas:  

Neurological Disease

BMT-124110 formic is a potent, selective AAK1 inhibitor, with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-124110 formic inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively .
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Cat. No.: HY-159088
CAS No.: 3050912-29-0
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
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Cat. No.: HY-161539
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg) .
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Cat. No.: HY-W740014
CAS No.: 139264-35-0
Synonyms: 183C91; DZT
Target:  

5-HT Receptor

Research Areas:  

Neurological Disease

N-Desmethyl Zolmitriptan (183C91; DZT) is the active metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist Zolmitriptan (HY-B0229). N-Desmethyl Zolmitriptan (183C91; DZT) is an agonist of 5-HT1B receptors and induces constriction in isolated human cerebral arteries (EC50=100 nM).
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Cat. No.: HY-148625
CAS No.: 917089-10-2
Research Areas:  

Cardiovascular Disease

PDE9-IN-2 (compound 6) is a PDE9 inhibitor that improves heart failure.
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Cat. No.: HY-168214
CAS No.: 2315450-35-0
Target:  

Potassium Channel

Research Areas:  

Neurological Disease

Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally active agonist for KV7.2/7.3 channel (KCNQ2/3) with an EC50 of 1.03 μM. Kv7.2/Kv7.3 agonist 1 exhibits analgesic efficacy in mice chronic constriction injury (CCI) model and mice Streptozotocin (HY-13753)-induced diabetic peripheral neuropathic pain (DPNP) model, with ED50 of 12.02 and 9.63 mg/kg .
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Cat. No.: HY-123382
CAS No.: 1695551-19-9
Target:  

Drug Isomer

GSK-1482160 isomer is the isomer of GSK-1482160 (HY-19888). GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI).
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Cat. No.: HY-107692R
CAS No.: 174635-53-1
SB 218795 (Standard) is the analytical standard of SB 218795 (HY-107692). This product is intended for research and analytical applications. SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit .
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Cat. No.: HY-110268
CAS No.: 1029521-30-9
Target:  

CXCR

Research Areas:  

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) .
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Cat. No.: HY-106798
CAS No.: 111073-18-8
Synonyms: A-57219; SCH 40054
Target:  

Adrenergic Receptor

Research Areas:  

Cardiovascular Disease

Nemazoline hydrochloride (A-57219 hydrochloride) is selective α-adrenergic agent with α1-agonist/α2-antagonist activity, which is used as a nasal decongestant. Nemazoline hydrochloride produces decongestion by α1-mediated contraction of capacitance vessels, but not compromises blood flow by virtue of α2-antagonism. Nemazoline hydrochloride also blocks endogenous noradrenaline-mediated α 2-constriction of the resistance vessels .
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Cat. No.: HY-165571
CAS No.: 378242-00-3
Target:  

Carboxypeptidase

Research Areas:  

Neurological Disease

E2072 is a selective, orally active competitive inhibitor of glutamate carboxypeptidase II (GCPII) with a Ki of 10 nM. E2072 alleviates established thermal hyperalgesia in a rat model of chronic constriction injury. E2072 prevents oxaliplatin-induced reductions in nerve conduction velocity and amplitude in mice. E2072 is applicable to research related to neuropathic pain and neuropathy .
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Cat. No.: HY-19545AR
CAS No.: 125941-87-9
Synonyms: R-(+)-SCH-23390 hydrochloride (Standard)
SCH-23390 hydrochloride (Standard) is the analytical standard of SCH-23390 hydrochloride (HY-19545A). This product is intended for research and analytical applications. SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM .
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Cat. No.: HY-110036AR
CAS No.: 1202865-22-2
Synonyms: L768242 hydrochloride (Standard)
GW405833 hydrochloride (Standard) is the analytical standard of GW405833 (hydrochloride) (HY-110036A). This product is intended for research and analytical applications. GW405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values ​​of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values ​​of 16.1 μM and 4772 nM for CB1. GW405833 hydrochloride also exhibits non-competitive CB1 antagonist, exerting its analgesic effect through a CB1 receptor (rather than CB2) dependent mechanism. GW405833 hydrochloride can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 hydrochloride inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF) .
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Cat. No.: HY-110036R
CAS No.: 180002-83-9
Synonyms: L768242 (Standard)
GW-405833 (Standard) is the analytical standard of GW-405833 (HY-110036). This product is intended for research and analytical applications. GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values ​​of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values ​​of 16.1 μM and 4772 nM for CB1. GW-405833 also exhibits non-competitive CB1 antagonist, exerting its analgesic and and anti-inflammatory effect through a CB1 receptor (rather than CB2) dependent mechanism. GW-405833 can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF) .
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Cat. No.: HY-156953
CAS No.: 1210803-60-3
Target:  

EBI2/GPR183

Research Areas:  

Neurological Disease

GPR183 antagonist-4 is a potent and selective GPR183 antagonist with an IC50 of 8.31 nM. GPR183 antagonist-4 inhibits receptor activation-mediated calcium signaling by antagonizing GPR183, and exhibits efficacy in ameliorating neuropathic pain-related allodynia. GPR183 antagonist-4 is useful for research on GPR183 signaling and neuropathic pain .
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Cat. No.: HY-187141
CAS No.: 69052-92-2
Target:  

COX

1,1,2-Triphenylhex-1-ene is an orally active COX-2 inhibitor with an IC50 of 7.9 μM against ovine COX-2. 1,1,2-Triphenylhex-1-ene attenuates inflammation by inhibiting COX-2. 1,1,2-Triphenylhex-1-ene relieves abdominal contractions. 1,1,2-Triphenylhex-1-ene can be used in research related to inflammation and pain .
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Cat. No.: HY-101290AR
CAS No.: 2231664-45-0
BMT-090605 (hydrochloride) (Standard) is the analytical standard of BMT-090605 (hydrochloride) (HY-101290A). This product is intended for research and analytical applications. BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 hydrochloride can be used for the research of neuropathic pain .
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Cat. No.: HY-181515
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

KOR agonist 8 (Compound 8a) is a κ-opioid receptor (KOR) agonist and an analgesic agent, with a Ki value of 5.3 nM for human KOR, and EC50 values of 43.1 nM and 9236 nM for human KOR. It exhibits subtype selectivity for MOR/KOR and DOR/KOR. KOR agonist 8 is applicable for pain-related research .
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Cat. No.: HY-W097625R
CAS No.: 26964-24-9
6-Methoxyflavone (Standard) is the analytical standard of 6-Methoxyflavone (HY-W097625). This product is intended for research and analytical applications. 6-Methoxyflavone is an orally active methoxyflavone. 6-Methoxyflavone suppresses neuroinflammation in microglia through the inhibition of TLR4/MyD88/p38 MAPK/NF-κB dependent pathways and the activation of HO-1/NQO-1 signaling. 6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway and activates the PERK/EIF2a/ATF4/CHOP pathway in HeLa cells. 6-Methoxyflavone acts as a Flumazenil (HY-B0009)-insensitive positive allosteric modulator at human recombinant α1β2γ2L and α2β2γ2L GABAα receptors. 6-Methoxyflavone inhibits NFAT Translocation into the nucleus and suppresses T cell activation. 6-Methoxyflavone partially restores chronic ethanol-induced behavioral deficits in mice. 6-Methoxyflavone antagonizes chronic constriction injury and diabetes associated neuropathic nociception expression. 6-Methoxyflavone can be used for the study of cancer, inflammation and neurological diseases .
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