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Targets Recommended: Others

16

抑制剂 & 化合物

1

重组蛋白

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Cat. No. Product Name Target Signaling Pathways
T11388 Gemilukast

ONO-6950

Others Others
Gemilukast(ONO-6950) 是一种具有口服活性和有效性的半胱氨酰白三烯 1 和 2 受体 (CysLT1 和CysLT2) 双重抑制剂,抑制 LTC 4 诱导的支气管收缩,对人 CysLT1 和 CysLT2 有抑制作用,可用于治疗哮喘。
T7841 MK 571

MK-571钠盐,L660711,L-660711,MK-571

LTR Immunology/Inflammation
MK 571 (L660711) 是一种具有口服活性的 CysLT1 受体拮抗剂。
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。
T22668 Cinalukast

Others Others
CysLT1 leukotriene receptor antagonist
T68392 ONO-4310321

ONO-4310321 is a potent, orally available dual CysLT1 and CysLT2 receptor antagonist.
T11860 LM-1484

Others Others
LM-1484 displays a higher affinity for 3H-LTC4 sites and is an antagonist of CysLT1 receptor.
T37016 Iralukast (CGP 45715A)

Iralukast is a cysteinyl-leukotriene antagonist (CysLT) with a pKi of 7.8 for CysLT1.
T69278 FPL-55712

FPL-55712 is a CysLT1 leukotriene receptor antagonist.
T70330 ONO-2050297

ONO-2050297 is the first potent dual CysLT1 and CysLT2 antagonist with IC50 values of 0.017 μM (CysLT1) and 0.00087 μM (CysLT2), respectively.
T71273 CAY10788

CAY10788 is an antagonist of CysLT1 receptor.
T31043 CP-199330

UNII-V4WYK6T8QA,CP 199330,UNII-74573Q728X,CP-199330 sodium

CP-199330 is a cysteyl LT1 receptor antagonist with no hepatotoxicity and is equivalent to the commercially available CYSLT1 receptor antagonists Zafirlukast and Pranlukas.
T37386 Dihydro Montelukast

Dihydro montelukast is a potential impurity found in commercial montelukast preparations. Montelukast (sodium salt) is a potent and selective cysteinyl leukotriene 1 (CysLT1) receptor antagonist. Formulations containing montelukast are used for the treatment of asthma as well as for the symptoms associated with allergic rhinitis.
T72145 Montelukast dicyclohexylamine

MK0476 dicyclohexylamine

Montelukast (MK0476) dicyclohexylamine 是一种有效、选择性且具口服活性的半胱氨酸白三烯受体1 (CysLT1) 拮抗剂,用于哮喘和肝损伤预防研究。它在肠缺血-再灌注损伤中展现抗氧化作用,减轻心脏损伤,并降低嗜酸性粒细胞对哮喘气道的浸润。此外,亦被用于COVID-19的研究。
T83926 S-Geranylgeranyl-L-glutathione

GGG

S-Geranylgeranyl-L-glutathione是孤儿G蛋白偶联受体(GPCR)P2RY8的配体。该化合物在100 nM浓度下,选择性地诱导P2RY8而非鞘氨醇-1-磷酸受体2(S1P2)、GPR55、半胱氨酸白三烯受体1CysLT1 receptor)以及CysLT2 receptor的内吞作用。在10 nM浓度下,S-Geranylgeranyl-L-glutathione抑制了表达P2RY8的WEHI-231 B细胞淋巴瘤细胞和分离的人扁桃体生发中心B细胞由趋化因子(C-X-C motif)配体12(CXCL12)诱导的迁移。
T37980 N-methyl Leukotriene C4

N-methyl Leukotriene C4

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...
T21864 BAY-u 9773

BAY-u 9773 是 CysLT 受体(半胱氨酸白三烯受体)的非选择性拮抗剂,对于 CysLT1CysLT2的 IC50值大致相同,用于抑制白三烯反应。

化合物

Gemilukast
Cat.No: T11388
Synonym: ONO-6950
Target: Others
MK 571
Cat.No: T7841
Synonym: MK-571钠盐,L660711,L-660711,MK-571
Target: LTR
MK-571 sodium
Cat.No: T3148
Synonym: L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid
Target: Leukotriene Receptor, LTR
Cinalukast
Cat.No: T22668
Synonym:
Target: Others
ONO-4310321
Cat.No: T68392
Synonym:
Target:
LM-1484
Cat.No: T11860
Synonym:
Target: Others
Iralukast (CGP 45715A)
Cat.No: T37016
Synonym:
Target:
FPL-55712
Cat.No: T69278
Synonym:
Target:
ONO-2050297
Cat.No: T70330
Synonym:
Target:
CAY10788
Cat.No: T71273
Synonym:
Target:
CP-199330
Cat.No: T31043
Synonym: UNII-V4WYK6T8QA,CP 199330,UNII-74573Q728X,CP-199330 sodium
Target:
Dihydro Montelukast
Cat.No: T37386
Synonym:
Target:
Montelukast dicyclohexylamine
Cat.No: T72145
Synonym: MK0476 dicyclohexylamine
Target:
S-Geranylgeranyl-L-glutathione
Cat.No: T83926
Synonym: GGG
Target:
N-methyl Leukotriene C4
Cat.No: T37980
Synonym: N-methyl Leukotriene C4
Target:
BAY-u 9773
Cat.No: T21864
Synonym:
Target:
Cat. No. Product Name Species Expression System
TMPH-03749 CYSLTR1 Protein, Human, Recombinant (His)

Cysteinyl leukotriene receptor 1,G-protein coupled ...

Human E. coli
Receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with and without asthma. Stimulation by LTD4 results in the contraction and proliferation of smooth muscle, edema, eosinophil migration and damage to the mucus layer in the lung. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. The rank order of affinities for the leukotrienes is LTD4 >> LTE4 = LTC4 >> LTB4.

重组蛋白

CYSLTR1 Protein, Human, Recombinant (His)
Cat.No: TMPH-03749
Species: Human
Expression System: E. coli
TargetMol Loading
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