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Cat. No. | Product Name | Target | Signaling Pathways |
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T3148 |
MK-571 sodium
L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid |
Leukotriene Receptor; LTR | GPCR/G Protein; Immunology/Inflammation |
MK-571 sodium (L-660711 sodium salt) 是一种可口服的选择性白三烯 D4受体拮抗剂,在豚鼠和人肺膜的 Ki 分别为0.22 和 2.1 nM。 | |||
T0173 |
Nylidrin hydrochloride
Buphenine HCl,布芬宁盐酸盐 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Nylidrin hydrochloride (Buphenine HCl) 是被动致敏大鼠腹腔肥大细胞中IgE 介导的组胺释放抑制剂,具有抗过敏的功效。它也是被动致敏的豚鼠肺切片中 IgG1 介导的组胺释放抑制剂。 | |||
T70193 |
APC-366 HCl
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APC-366 is a selective inhibitor of the mast cell tryptase that inhibits tryptase-induced histamine release from human tonsil and lung cells. | |||
TQ0032L |
Rosiptor acetate
AQX-1125,AQX 1125,AQX1125,AQX-1125 acetate |
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Rosiptor is a potent and selective SHIP1 activator. AQX-1125 inhibits Akt phosphorylation in SHIP1-proficient but not in SHIP1-deficient cells, reduces cytokine production in splenocytes, inhibits the activation of mast cells and inhibits human leukocyte | |||
T36713 |
Streptochlorin
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Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has diverse biological activities, including antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 20 μM. Streptochlorin (12 μg/ml) decreases viability of, as well as induces apoptosis and increases the productio... | |||
T82176 |
HR1
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HR1是一种乳突蛋白酶,可增加人红细胞膜渗透性,并能诱导细菌细胞质膜和肥大细胞质膜透化。 | |||
T36545 |
Prostaglandin D2 methyl ester
Prostaglandin D2 methyl ester |
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Prostaglandin D2 (PGD2) is the major eicosanoid product of mast cells and is produced in large quantities by hematopoietic PGD synthase during allergic and asthmatic anaphylaxis. It causes vasodilation, flushing, hypotension, and is an inhibitor of platelet aggregation. Prostaglandin D2 methyl ester (PGD2 methyl ester) is a more lipid-soluble, cell-permeable prodrug form of PGD2. It binds to the human and mouse PGD2 receptors (DP1 and CRTH2/DP2) with 5-10 fold lower affinity than PGD2. | |||
T38126 | PMX 53c | ||
Negative control for PMX 53. Active Analog also available. Subramanian et al (2011) PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol.Pharmacol. 79 1005 PMID:21441599 | |||
T37492 |
11-trans Leukotriene C4
11-trans Leukotriene C4 |
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11-trans Leukotriene C4 (11-trans LTC4) is a C-11 double bond isomer of LTC4. LTC4 undergoes slow temperature-dependent isomerization to 11-trans LTC4 during storage. 11-trans LTC4 is produced in smaller amounts relative to LTC4 in ionophore-stimulated HMC-1 cells (a human mast cell line) and equine eosinophils, but not in human neutrophils or RBL-1 cells. It is nearly equipotent with LTC4 for contraction of guinea pig parenchymal and ileum. In a radioligand binding assay using guinea pig ileum ... | |||
T35453 |
β-Defensin-4 (human) (trifluoroacetate salt)
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β-Defensin-4 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It induces migration of monocytes in vitro when used at a concentration of 10 nM but does not affect migration of neutrophils and eosinophils. β-Defensin-4 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes. It also stimulates calcium mobilization, migration, and pro... | |||
T35452 |
β-Defensin-3 (human) (trifluoroacetate salt)
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β-Defensin-3 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It inhibits the growth of the periodontopathogenic and cariogenic bacteria F. nucleatum, S. mutans, S. sobrinus, S. salivarius, and L. casei (MICs = 12.5-100 mg/l). It also inhibits the growth of S. aureus, S. pyogenes, P. aeruginosa, E. coli, and C. albicans. β-Defensin-3 stimulates gene expression and production of IL-6, IL-10, CXC... | |||
T38306 |
tetranor-PGDM
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Prostaglandin D2 is synthesized by hematopoietic-type PGD-synthase (H-PGDS) in mast cells and is released in large quantities during allergic and asthmatic anaphylaxis. PGD2 is also produced in the brain by lipocalin-PGD-synthase also known as β-trace. In the brain, PGD2 produces normal physiological sleep and lowering of body temperature. Further pharmacological actions include inhibition of platelet aggregation and relaxation of vascular smooth muscle. tetranor-PGDM is a major metabolite of PG... | |||
T68701 |
Abarelix acetate
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Abarelix acetate is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist. It increases histamine release from rat peritoneal mast cells in vitro and from a human skin model ex vivo. In vivo, abarelix decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.3 Abarelix (2 mg/kg) also transiently decreases plasma testosterone levels in intact rats, with levels returning to baseli... | |||
T35731 |
Deethylindanomycin
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Deethylindanomycin is a polyether antibiotic that has been found in S. setonii. It is active against a variety of Gram-positive bacteria, including various strains of S. aureus and Streptococcus, as well as one strain of S. pneumoniae (MICs = 4, 4, and 2 μg/ml, respectively). It is also active against coccidia in vitro, inhibiting E. tenella development, but is inactive against E. tenella infection in chicks when administered at a dose of 200 μg/g in the diet. Deethylindanomycin acts as an ionop... | |||
T78641 | ER-27319 | Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
ER-27319为吖啶酮衍生物,高效选择性抑制SYK,阻断其酪氨酸磷酸化和活性。本化合物阻止抗原刺激下人及大鼠肥大细胞释放过敏介质,IC50约为10 μM,适用于过敏性疾病研究。 | |||
T73665 |
Bufrolin
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Bufrolin,作为Cromoglycate(组胺释放抑制剂)的类似物,是一种高效的GPR35激动剂,能够促进β-arrestin-2与人GPR35a或大鼠GPR35之间的相互作用。此外,Bufrolin亦可作为抗过敏性肥大细胞稳定剂,有效抑制内化肽诱导的抗炎反应,并且在内化肽连接药剂的药物递送研究中,被作为抗炎剂使用。 | |||
T37262 |
14,15-Leukotriene E4
14,15-Leukotriene E4 |
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Leukotrienes (LTs) are a group of acute inflammatory mediators derived from arachidonic acid in leukocytes. The majority of these metabolites are formed through the 5-lipoxygenase (5-LO) pathway. 14,15-LTE4 is a metabolite of 14,15-LTC4 and 14,15-LTD4, an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-LOs on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. These metabolites are classified as eoxins because they are formed mostly by eosinophils... | |||
T37980 |
N-methyl Leukotriene C4
N-methyl Leukotriene C4 |
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Produced by neutrophils, macrophages, mast cells, and by transcellular metabolism in platelets, leukotriene C4 (LTC4) is the parent cysteinyl leukotriene formed by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4, however, is rapidly metabolized to LTD4 and LTE4, which makes the characterization of LTC4 pharmacology difficult. N-methyl Leukot... | |||
T37604 | ITK inhibitor | ||
Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminome... | |||
T37261 |
14,15-Leukotriene D4
14,15-Leukotriene D4 |
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14,15-Leukotriene D4 (14,15-LTD4) is a member of an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-lipoxygenases (15- and 12-LOs) on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. 14,15-LTD4 is classified as an eoxin (EXD4), because it is formed mostly by eosinophils. However, mast cells and nasal polyps can synthesize 14,15-LTD4 as well. Little is known about the physiological actions of 14,15-LTD4. It has weak contractile activity on both ... | |||
T69383 |
NBI-42902
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NBI-42902 is a potent inhibitor of peptide radioligand binding to the human GnRH receptor (K(i) = 0.56 nm). Tritiated NBI-42902 binds with high affinity (K(d) = 0.19 nm) to a single class of binding sites and can be displaced by a range of peptide and nonpeptide GnRH receptor ligands. In vitro experiments demonstrate that NBI-42902 is a potent functional, competitive antagonist of GnRH stimulated IP accumulation, Ca(2+) flux, and ERK1/2 activation. It did not stimulate histamine release from rat... | |||
T80234 |
SFNGGP-NH2
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SFNGGP-NH2是一种具有生物活性的肽。PAR-3是一种与凝血酶高亲和力结合的受体,其mRNA在人类皮肤肥大细胞中得到表达。研究指出,蛋白酶激活受体(PAR)在瘙痒反应中的作用涉及组胺依赖性及独立途径。虽然PAR-3本身不直接诱发瘙痒,却可能与PAR-4共同促发此症状。它们的共同表达可增强凝血酶的效应,这表明PAR-3单独时不进行跨膜信号传导,而是作为激活PAR-4的协同因子。 | |||
T36618 |
Rupatadine
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Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in hu... |
Cat. No. | Product Name | Target | Signaling Pathways |
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TN1516 |
Cnidicin
蛇床素,4,9-双[(3-甲基-2-丁烯-1-基)氧基]-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮 |
NOS; NO Synthase | Immunology/Inflammation |
Cnidicin 是一种香豆素,对肥大细胞脱颗粒及 RAW 264.7 细胞产生一氧化氮具有抑制作用。 | |||
T5S2343 |
Acetylshikonin
乙酰紫草素,Acetyl shikonin |
Others; P450; AChE | Metabolism; Neuroscience; Others |
Acetylshikonin 来源于紫草根,具有抗癌、抗炎作用。它是一种 AChE 抑制剂,具有很强的抗凋亡活性。它是一种非选择性的细胞色素 P450抑制剂,对所有 P450 亚型抑制的 IC50值范围为 1.4-4.0 μM。 | |||
T3S0027 |
Picropodophyllotoxin
AXL 1717,Picropodophyllin,苦鬼臼毒素 |
IGF-1R | Tyrosine Kinase/Adaptors |
Picropodophyllotoxin (AXL 1717) 是一种环木脂素生物碱,存在于五月树(Podophyllum peltatum) 中,是一种具有潜在抗肿瘤活性的胰岛素样生长因子 1 受体 (IGF1R) 的小分子抑制剂。它特异性抑制 IGF1R 的活性并下调细胞表达,而不干扰其他生长因子受体的活性,例如胰岛素受体、表皮生长因子、血小板衍生生长因子、成纤维细胞生长因子和肥大/干细胞生长因子 (KIT) )。该药剂在抑制肿瘤细胞增殖和诱导肿瘤细胞凋亡方面显示出有效的活性。 IGF1R 是一种在多种人类癌症中过度表达的受体酪氨酸激酶,在多种癌细胞的生长和存活中起关键作用。 | |||
T80998 |
Thapsigargicin
Thapsigargicine |
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Thapsigargicin(Thapsigargicine)作为肥大细胞和白细胞的激活剂,能诱导大鼠腹膜肥大细胞及人嗜碱性粒细胞释放组胺,并提升完整人血小板中的细胞质游离钙水平。 | |||
TN5647 |
Confluentin
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Confluentin has antimicrobial activity against the gram-positive bacteria.Confluentin significantly inhibits compound 48/80-induced histamine release from rat peritoneal mast cells. Confluentin also shows weak cytotoxicity against four human tumor cell li | |||
T25687 |
Leukotriene C4
白三烯C4,LTC4,Leukotriene C |
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Leukotriene C4 is the conjugation product of Leukotriene A4 and glutathione. It is the major arachidonic acid metabolite in human mast cells, macrophages, and antigen-sensitized lung tissue. It stimulates mucus secretion in the lung and produces contracti | |||
TN3325 |
9-O-Feruloyl-5,5'-dimethoxylariciresinol
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IL Receptor; TNF | Apoptosis; Immunology/Inflammation |
(+)-9'-O-trans-feruloyl-5,5'-dimethoxylariciresinol may have anti-allergic inflammatory effect, it can inhibit release of histamine from mast cells. It shows cytotoxicity against a small panel of human tumor cell lines, with ED50 values of 9.86 to approxi | |||
T37272 |
9(S),12(S),13(S)-TriHOME
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9(S),12(S),13(S)-TriHOME is a linoleic acid-derived oxylipin that has diverse biological activities.1,2,3,4It has been found in various plants and is produced in human eosinophils in a 15-lipoxygenase-dependent, soluble epoxide hydrolase-independent manner.1,59(S),12(S)13(S)-TriHOME inhibits antigen-induced β-hexosaminidase release from RBL-2H3 mast cells (IC50= 28.7 μg/ml).2It inhibits LPS-induced nitric oxide (NO) production in BV-2 microglia (IC50= 40.95 μM).3In vivo, 9(S),12(S),13(S)-TriHOME... |