Cat. No. | Product Name | Target | Signaling Pathways |
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T10057 |
LTD4 antagonist 1
|
Others | Others |
LTD4 antagonist 1 is a potent and orally active antagonist of leukotriene D4 (LTD4; Ki: 0.57 nM). | |||
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... | |||
T30828 |
CGP 35949
CGP-35949,Cgp-35949,Cgp35949,CGP35949 |
Leukotriene Receptor | GPCR/G Protein |
CGP 35949是一种具有磷脂酶抑制活性的LTD4拮抗剂。 | |||
T27979 |
Masilukast
ICI-D-3523,ZD-3523,ICI D-3523,MCC-847,SA-09012,D-3523 |
Leukotriene Receptor | GPCR/G Protein |
Masilukast(MCC-847) 是一种口服的白三烯D4 (LTD4) 受体拮抗剂,可用于研究与炎症相关的疾病。 | |||
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. | |||
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。 | |||
T27877 |
LY 163443
LY163443,LY-163443 |
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LY 163443 is an dual receptor antagonist of LTD4 and LTE4. | |||
T10501 |
YM158 free base
YM-57158 |
Others | Others |
YM158 free base is a potent and selective antagonist of TXA2 and LTD4 receptor (pA2s: about 8.81 and 8.87). | |||
T10873 |
CP-96486
|
Others | Others |
CP-96486 is a potent and orally active antagonist of leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor (Kis: 20 and 24 nM). | |||
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。 | |||
T37493 |
11-trans Leukotriene D4
11-trans Leukotriene D4 |
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11-trans Leukotriene D4 (11-trans LTD4) is a C-11 double bond isomer of LTD4. LTD4 undergoes slow temperature-dependent isomerization to 11-trans LTD4 during storage. 11-trans LTD4 retains about 10-25 % of the potency for contraction of guinea pig ileum, trachea and parenchyma compared to LTD4. It exhibits an ED50 ranging between 12-60 nM for contraction of guinea pig trachea. | |||
T27912 |
LY 290324
LY-290324,LY290324 |
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LY 290324 is an orally active, potent and selective antagonist of cysteinyl leukotriene (LTD4) receptor. | |||
T15647 |
Tipelukast
MN 001,KCA 757 |
Leukotriene Receptor | GPCR/G Protein |
Tipelukast (KCA 757) 是一种新型可口服的白三烯受体 (leukotriene receptor) 拮抗剂,是具有抗炎活性,可减少纤维化,下调 TIMP-1、1 型胶原蛋白。Tipelukast 可用于研究哮喘疾病。 | |||
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). | |||
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). | |||
T71499 |
NZ-107
|
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NZ-107 is an LTB4, LTC4 and LTD4 antagonist. | |||
T10872L |
CP 96021
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5-HT Receptor | GPCR/G Protein; Neuroscience |
CP 96021是一组5-HT1受体和5-HT2受体拮抗剂,具有抗炎特性,是治疗胃肠道和呼吸道哮喘的非自身抗溃疡化合物。 | |||
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 ... | |||
T40870 |
Leukotriene E4
LTE4 |
Endogenous Metabolite | Metabolism |
Leukotriene E4 (LTE4)(LTE4)通过 二肽酶对LTD4 上的作用生成,是过敏性休克慢反应物质(SRS-A)的成分之一。LTE4 存在于血浆和尿液中,可用于检测哮喘。 | |||
T19674 |
Verlukast
MK 0679,MK-679,L 668,019,MK 679,L 668019,L-668,019 |
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Verlukast is an (R)-enantiomer of MK-571 and a potent and selective LTD4 receptor antagonist. Verlukast showed [3H]leukotriene D4 binding in guinea-pig (IC50 = 3.1 +/- 0.5 nM) and human (IC50 = 8.0 +/- 3.0 nM) lung homogenates and dimethyl sulfoxide diffe | |||
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。 | |||
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。 | |||
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。 | |||
T37652 |
5(S),6(R)-DiHETE
|
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5(S),6(R)-DiHETE is a dihydroxy polyunsaturated fatty acid and a nonenzymatic hydrolysis product of leukotriene A4 (LTA4). Mouse liver cytosolic epoxide hydrolase catalyzes the conversion of LTA4 to 5(S),6(R)-DiHETE. It is a weak LTD4 receptor agonist in guinea pig lung membranes. It induces guinea pig ileum contraction with an ED50 value of 1.3 μM. | |||
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] | |||
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... | |||
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... | |||
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... |