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Cat. No. | Product Name | Target | Signaling Pathways |
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T10911 |
H3 receptor antagonist 1
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Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist. | |||
T27445 |
GSK-1004723
GSK 1004723 |
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GSK-1004723 is a novel antagonist of histamine H(1) and H(3) receptor. It represents a potential novel therapy for allergic rhinitis. | |||
T36722 |
Deltorphin II (trifluoroacetate salt)
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Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid... | |||
T35836 |
PMX-205 (trifluoroacetate salt)
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PMX-205 is a cyclic hexapeptide that acts as a potent antagonist of C5a receptor (C5aR; IC50= 31 nM).1It is orally active and blocks inflammatory signaling and symptoms in animal models of colitis and allergic asthma.2,3PMX-205 is also brain penetrant and reduces neuroinflammation and neurodegeneration in an animal model of Alzheimer's disease.4 1.March, D.R., Proctor, L.M., Stoermer, M.J., et al.Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Rela... | |||
T35772 |
Emestrin
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Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities.1,2,3,4,5 It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 μg/ml, respectively).2 Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 μM in a radioligand binding assay using isolated human monocytes).3 Emestr... | |||
T38145 | Eltoprazine | ||
Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A/1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of no... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T35667 |
Napyradiomycin A1
Napyradiomycin A1 |
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Napyradiomycin A1is a fungal metabolite originally isolated fromC. rubraand has diverse biological activities.1,2It is active againstS. aureus,M. luteus,B. anthracis,C. bovis, andM. smegmatis(MICs = 1.56-12.5 μg/ml).1Napyradiomycin A1is an estrogen receptor antagonist (IC50= 4.2 μM in rat uterine homogenates).2It also inhibits mitochondrial NADH:ubiquinone oxidoreductase (complex I) and succinate:ubiquinone oxidoreductase (complex II) activities in bovine heart homogenates (IC50s = 20 and 9.7 μM... |