cyslt1

LM-1484 displays a higher affinity for 3H-LTC4 sites and is an antagonist of CysLT1 receptor.

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。

Quininib is a regulator of Ocular Angiogenesis. Quininib significantly inhibits angiogenic tubule formation in HMEC-1 cells, angiogenic sprouting in aortic ring explants and retinal revascularisation in OIR mice.

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

CAY10789 (化合物 6) 是有效的CysLT1R 拮抗剂 ，IC50值为2.80 μM。CAY10789 也是一种GPBAR1激动剂 ，EC50为3 μM。CAY10789 显著降低 U937 细胞对 HAEC 的粘附并降低 TNF-α 的表达。CAY10789 表现出有前途的代谢稳定性和出色的药代动力学。 CAY10789 可用于结肠炎、代谢综合征和其他 GPBAR1 CysLT1R 相关疾病的研究。

CAY10788 is an antagonist of CysLT1 receptor.

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。

MK 571 (L660711) 是一种具有口服活性的 CysLT1 受体拮抗剂。

KP496 is a selective, dual antagonist for Thromboxane A2 receptor and Leukotriene D4 receptor.

CP-199331, 一种cysLT1受体拮抗剂，与市面上的cysLT1受体拮抗剂zafirlukast和pranlukast具有同等效力。在大鼠和猴子中表现出良好的药代动力学特性，并且在猴子中未观察到CP-85,958所见的肝毒性。

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 CysLT1和 CysLT2的 IC50值大致相同，用于抑制白三烯反应。

CysLT1 leukotriene receptor antagonist

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

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.

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 Leukotriene C4 (N-methyl LTC4) is a synthetic analog of LTC4 that is not readily metabolized to LTD4 and LTE4.It acts as a potent and selective CysLT2 receptor agonist exhibiting EC50 values of 122 and > 2,000 nM at the human CysLT2 and CysLT1 receptors, respectively. It has essentially the same potency as LTC4 at both the human and murine receptors CysLT2 receptors. N-methyl LTC4 is potent and active in vivo, causing vascular leak in mice overexpressing the human CysLT2 receptor but not in CysLT2 receptor knockout mice.

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

FPL-55712 is a CysLT1 leukotriene receptor antagonist.

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.

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。

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1（CysLT1 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。