p 80

PDE4 inhibitor

Cgp 8065 is a filaricidal compound, a dithiocarbamate-derivative of amoscanate.

CP 80080 weakly enhances topoisomerase II-mediated DNA cleavage.

UFP 803 acetate 是一种有效的 urotensin-II (UT) 受体配体。 UFP-803 显示较低残留激动剂的活性。

Sotagliflozin (LP-802034) 是有效的SGLT1 2抑制剂，用作抗糖尿病剂。

NSP-805 是一种强心剂，是一种选择性的 phosphodiesterase 3 抑制剂，具有舒张血管的作用。

TP808是一种高度通用的中间体，可用于多种四环素类抗生素的构建。

CP-809101 hydrochloride 是选择性 5-HT2C 受体激动剂，对于人类 5-HT2C 5-HT2B 5-HT2A 受体。

VER-82576 (NVP-BEP800) 是一种可口服的，选择性的 Hsp90抑制剂，对 Hsp90β 的 IC50值为 58 nM，对 Hsp90 家族成员 Trap-1 和 Grp94 的选择性超过 70 倍。

UFP-803 TFA 是有效的urotensin-II receptor (UT)配体。UFP-803 TFA 具有较低的残留激动剂活性，因此它可以作为研究UT 系统在生理学和病理学中作用的重要工具。

Urotensin-II (UT) receptor ligand; behaves as a silent antagonist in most in vitro assays and in vivo, but does retain small residual agonist activity under certain conditions in some assays. Competitively antagonizes U-II induced contractions in the rat

CP-809101 is an effective and selective 5-HT2C receptor agonist (pEC50: 9.96 7.19 6.81 for human 5-HT2C 5-HT2B 5-HT2A receptors).

BQR-695 (NVP-BQR695) 是一种磷脂酰肌醇 4-激酶抑制剂，对于人类和疟原虫 PI4KIIIβ 的 IC50值分别为 80 和 3.5 nM。

Compound 48 80 trihydrochloride (C48 80 trihydrochloride) 是 N-甲基对甲氧基苯乙胺和甲醛发生缩合反应后的混合物。Compound 48 80 trihydrochloride 是一种肥大细胞 (mast cell) 脱颗粒剂和组胺 (histamine) 释放剂。Compound 48 80 trihydrochloride 对人血小板磷脂酰肌醇特异性磷脂酶 C (phosphatidylinositol-specific phospholipase C) 活性有抑制作用。

AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1). IC50 value: 80 nM [1] Target: DGAT1 in vitro: Plasma AZD7687 exposure was measured repeatedly. AZD7687 markedly reduced postprandial TAG excursion with a steep concent

β-Defensin-2 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius.2β-Defensin-2 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes.3It also stimulates calcium mobilization, migration, and proliferation of keratinocytes when used at concentrations of 30, 10, and 40 μg/ml, respectively. β-Defensin-2 induces IL-31 production by human peripheral blood-derived mast cellsin vitrowhen used at a concentration of 10 μg/ml and by rat mast cellsin vivofollowing a 500 ng intradermal dose.4Expression of β-defensin-2 is increased in psoriatic skin and chronic wounds.5,6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 3.Niyonsaba, F., Ushio, H., Nakano, N., et al.Antimicrobial peptides human β-defensins stimulate epidermal keratinocyte migration, proliferation and production of proinflammatory cytokines and chemokinesJ. Invest. Dermatol.127(3)594-604(2007) 4.Niyonsaba, F., Ushio, H., Hara, M., et al.Antimicrobial peptides human β-defensins and cathelicidin LL-37 induce the secretion of a pruritogenic cytokine IL-31 by human mast cellsJ. Immunol.184(7)3526-3534(2010) 5.Huh, W.-K., Oono, T., Shirafuji, Y., et al.Dynamic alteration of human β-defensin 2 localization from cytoplasm to intercellular space in psoriatic skinJ. Mol. Med. (Berl.)80(10)678-684(2002) 6.Butmarc, J., Yufit, T., Carson, P., et al.Human β-defensin-2 expression is increased in chronic woundsWound Repair Regen.12(4)439-443(2004)

Previridicatumtoxin is a fungal metabolite that has been found inP. aethiopicumand has diverse biological activities.1,2It is an intermediate in the biosynthesis of the mycotoxin viridicatumtoxin . Previridicatumtoxin is active against methicillin-resistantS. aureus(MRSA) and vancomycin-resistantE. faecalis(IC50s = 4.4 and 4.8 μM, respectively), as well asC. albicansandS. cerevisiae(MIC = 32 μg ml for both).2,1It is cytotoxic to NCI H460, KB-3-1, and SW620 cancer cells (IC50s = 5.3, 4.1, and 6 μM, respectively).2 1.Chooi, Y.H., Wang, P., Fang, J., et al.Discovery and characterization of a group of fungal polycyclic polyketide prenyltransferasesJ. Am. Chem. Soc.134(22)9428-9437(2012) 2.Shang, Z., Salim, A.A., Khalil, Z., et al.Viridicatumtoxins: Expanding on a rare tetracycline antibiotic scaffoldJ. Org. Chem.80(24)12501-12508(2015)

Aspergillin PZ is a fungal metabolite originally isolated from A. awamori. It induces morphological deformation of P. oryzae conidia when used at a concentration of 89 nM. Aspergillin PZ is active against S. epidermidis (MIC = 20 μM) but not S. aureus, E. coli, or B. cereus (MICs = >20 μM). It is cytotoxic to HL-60 promyelocytic leukemia cells (IC50 = 56.61 μM) but not THP-1 acute monocytic leukemia or PC3 prostate cancer cells (IC50s = >80 μM).

ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s), effectively targeting hGX with an IC50 of 80 nM. It efficiently inhibits the phosphorylation of ERK1 2 and p-38. sPLA2s, belonging to the disulfide-rich, Ca2+-dependent enzyme family, catalyze the hydrolysis of glycero-phospholipids at the sn-2 position, resulting in the release of a fatty acid and a lysophospholipid. ROC-0929 holds promise in researching inflammation-related diseases.

Compound 48 80, also known as Poly-p-methoxyphenethylmethylamine, is a commonly utilized mast cell activator in animal and tissue models. This compound exerts its effect by stimulating trimeric G-proteins at the mast cell membrane, triggering degranulation through both phospholipase C and D pathways.

Kumatakenin 是一种从丁香中分离得到的黄酮类天然产物，可诱导卵巢癌细胞凋亡。

Tripeptide substance P (SP) antagonist (IC50 = 90 μM). Also inhibits binding of SP to Mas-related GPCR (MRGPR) X2. Inhibits SP-induced IgE-independent degranulation of mast cells in vitro. Inhibits compound 48 80-induced MRGPRX2 activation and scratching