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Cat. No. | Product Name | Target | Signaling Pathways |
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T26519 |
Ablukast
Ro 23-3544,阿鲁司特 |
Leukotriene Receptor | GPCR/G Protein |
Ablukast (Ro 23-3544) 是白三烯受体的选择性拮抗剂,也是LTD4受体拮抗剂。可改善 LTC4 和抗原诱导的支气管狭窄。 | |||
T3185 |
R112
(E)-Elafibranor |
Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
R112 ((E)-Elafibranor) 是ATP 竞争性的 Syk 激酶抑制剂,它能够抑制Syk 激酶活性,Ki=6 nM,IC50=226 nM。 | |||
T16280 |
Nedocromil
FPL 59002,尼多克罗 |
Leukotriene Receptor; Prostaglandin Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Nedocromil (FPL 59002) 对多种介质的作用或形成有抑制作用,包括组胺,前列腺素 D2和白三烯 C4。 | |||
T14326 |
AS-35
|
Others | Others |
AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum. With IC50 values of 8 nM, 4 nM and 3 nM, respectively. It has antiallergic activities. | |||
T16739 |
RG-12525
NID 525 |
Leukotriene Receptor; PPAR | DNA Damage/DNA Repair; GPCR/G Protein; Metabolism |
RG-12525(NID 525) 是一种可口服且具有选择性和竞争性的白三烯 D (LTD)拮抗剂,对 LTC4,LTD4 和 LTE4 诱导的豚鼠薄壁带收缩有抑制作用,IC50 值分别为 2.6 nM,2.5 nM 和 7 nM。RG-12525 对 CYP3A4 有抑制作用, Ki 值为 0.5 µM。RG-12525 是一种新型高效的 PPAR-γ 激动剂(IC50 值约为 60 nM),具有物种特异性,可用于研究哮喘。 | |||
T67959 |
Pirodomast
|
Thrombin; Serine Protease | Proteases/Proteasome |
Pirodomast 是血栓素 A(TXA2)合成酶抑制剂。Pirodomast 能抑制白三烯(LT)D4、C4、E4 的形成和血栓素 B2(TXB2)的活性,但对组胺、甲氧胆碱、血清素、LTC4 或血小板活化因子诱导的豚鼠支气管痉挛的拮抗作用较弱或无效。Pirodomast 在体外对豚鼠气管只有微弱的松弛活性。Pirodomast 是一种潜在的抗过敏化合物,在体外可抑制胰蛋白酶的蛋白水解活性,在体内可阻止抗原诱发过敏绵羊的即时和晚期哮喘反应,抑制抗原诱导的过敏绵羊对组胺和卡巴胆碱的气道高反应性。 | |||
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 ... | |||
T37620 |
Leukotriene C4 methyl ester
|
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Leukotriene C4 (LTC4) is the parent cysteinyl-leukotriene produced by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. LTC4 is produced by neutrophils, macrophages, and mast cells, and by transcellular metabolism in platelets. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute all... | |||
T10054 | CI-949 | Others | Others |
CI-949 is an allergic mediator release inhibitor, which inhibits leukotriene C4/D4 (LTC4/LTD4), histamine, and thromboxane B2 (TXB2) release (IC50s: 0.5 μM, 11.4 μM and 0.1 μM). | |||
T11860 | LM-1484 | Others | Others |
LM-1484 displays a higher affinity for 3H-LTC4 sites and is an antagonist of CysLT1 receptor. | |||
T71053 |
AHR-5333 mandelate
|
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AHR-5333 mandelate is an anti-allergy compound which has been shown to protect against antigen-induced anaphylactic collapse and ascaris antigen-induced skin hypersensitivity. AHR-5333 mandelate has also been shown to inhibit 5-HETE, LTB4 and LTC4 synthesis. | |||
T13879 |
(S)-Verapamil hydrochloride
(S)-(-)-Verapamil hydrochloride |
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
(S)-Verapamil hydrochloride is an inhibitor of leukotriene C4 (LTC4) and calcein transport by MRP1,and leads to the death of potentially resistant tumor cells. | |||
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... | |||
T71499 |
NZ-107
|
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NZ-107 is an LTB4, LTC4 and LTD4 antagonist. | |||
T0694 |
Pranlukast
普鲁司特,ONO-1078,普仑司特 |
Leukotriene Receptor; IL Receptor; Others; TNF; NF-κB; LTR | Apoptosis; GPCR/G Protein; Immunology/Inflammation; NF-κB; Others |
Pranlukast (ONO-1078) 是一种半胱氨酰白三烯受体 1 拮抗剂,可拮抗或减少支气管痉挛,用于哮喘研究。 | |||
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... | |||
T13855 |
Quinotolast sodium
FR71021 |
Others | Others |
Quinotolast sodium inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner in the concentration range of 1-100 μg/mL. | |||
T38128 |
Leukotriene D4
Leukotriene D4 MaxSpec® Standard,LTD4 |
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Leukotriene D4 (LTD4) is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) produced by the metabolism of LTC4 by γ-glutamyl transpeptidase. It is the first cysteinyl-leukotriene metabolite of LTC4 . Like LTC4, LTD4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute hypersensitivity. LTD4 is equipotent to LTC4 in its biological activities, except that LTD4 is nearly 100-fold more effective in the contraction of... | |||
T28251 |
ONO-8809
ONO8809 |
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ONO-8809 is a thromboxane A2 receptor antagonist. ONO-8809 inhibited the LTC4-induced airway hyperresponsiveness to histamine in a dose-dependent manner. Macrophage accumulation and matrix metalloproteinase-9 (MMP-9) activity in the stroke-negative area i | |||
T63291 |
Pranlukast hemihydrate
|
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Pranlukast hemihydrate 是选择性的、高效的、竞争性的 leukotriene 拮抗剂。Pranlukast 能够抑制 [3H]LTE4 (Ki: 0.63±0.11 nM),[3H]LTD4 (Ki: 0.99±0.19 nM)和 [3H]LTC4 (Ki: 5640±680 nM)与肺膜结合。 | |||
T38062 |
N-acetyl Leukotriene E4
N-acetyl Leukotriene E4 |
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N-acetyl LTE4 is the major inactive metabolite of LTE4 found in bile. This route of metabolism is prominent in the rat, but of minor importance in humans. N-acetyl LTE4 is 100 times less potent than LTC4 as a vasoconstricting agent. In healthy human subjects urinary excretion of N-acetyl LTE4 is about 1.5 nmol/mol creatinine, which is considerably less than that of LTE4 (12 nmol/mol creatinine). | |||
T38129 |
Leukotriene F4
LTF4 |
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LTF4 is a cysteinyl-leukotriene produced in vitro, but not reported to date in vivo. It is formed by the incubation of LTE4 with γ-glutamyl transpeptidase and glutathione. LTF4 is a weak agonist in its ability to contract vascular smooth muscle. [1] The rank order of potency of the cysteinyl-leukotrienes to contract vascular smooth muscle is LTD4 > LTC4 > LTE4 >> LTF4. [1] [2] | |||
T37331 |
Pyrrophenone
|
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The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs). Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively). Its action is reversible and selective, as py... | |||
T10872 | CP-96021 hydrochloride | Others | Others |
CP-96021 hydrochloride is a potent and orally active antagonist of leukotriene D4 (LTD4)/platelet activating factor receptor (Kis: 34 nM and 37 nM). |
Cat. No. | Product Name | Target | Signaling Pathways |
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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 | |||
T5714 |
5-O-Demethylnobiletin
5-DEMETHYLNOBILETIN,去甲基川陈皮素 |
Leukotriene Receptor; Lipoxygenase | GPCR/G Protein; Metabolism |
5-O-Demethylnobiletin (5-DEMETHYLNOBILETIN) 是从黄芪中分离出的多甲氧基黄酮,具有抗炎活性,可通过直接抑制 5-LOX 发挥作用,IC50为 0.1 μM。 |