2020058-38-0
Chemical Structure
S‐Y048
- CAS 番号: 2020058-38-0
- Formula:C27H31Cl2NO3
- Molecular Weight:488.45
InChIKey: XGNFPJZMWOIDAH-SFHVURJKSA-N
SMILES: OC(C[C@@H](C)CC(C(C1=C2)=C(CCCCCCC3=CC(Cl)=CC=C3)N(C)C1=CC=C2Cl)=O)=O
Biological Activity: S-Y048 is an orally active OXE receptor-selective antagonist with picomolar-level IC50 values (0.02-30 nM) and pIC50 values of (10.47-10.81) against human receptors. S-Y048 selectively blocks the 5-oxo-ETE signaling pathway, inhibits actin polymerization, calcium mobilization, leukocyte migration, as well as allergen-induced leukocyte infiltration in skin and lung tissues, and reduces mucin-producing bronchial epithelial cells. S-Y048 undergoes benzyl, N-methyl and α-hydroxylation reactions to form metabolites in monkeys. S-Y048 can be used in research related to asthma, allergic asthma, allergic eosinophilic diseases, atopic dermatitis and allergic rhinitis[1][2][3][4].
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S‐Y048 | S-Y048 is an orally active OXE receptor-selective antagonist with picomolar-level IC50 values (0.02-30 nM) and pIC50 values of (10.47-10.81) against human receptors. S-Y048 selectively blocks the 5-oxo-ETE signaling pathway, inhibits actin polymerization, calcium mobilization, leukocyte migration, as well as allergen-induced leukocyte infiltration in skin and lung tissues, and reduces mucin-producing bronchial epithelial cells. S-Y048 undergoes benzyl, N-methyl and α-hydroxylation reactions to form metabolites in monkeys. S-Y048 can be used in research related to asthma, allergic asthma, allergic eosinophilic diseases, atopic dermatitis and allergic rhinitis. | |||||||||||||||||||||
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- [1]. Cossette C, et al. Targeting the OXE receptor with a selective antagonist inhibits allergen-induced pulmonary inflammation in non-human primates. British journal of pharmacology. 2022 Jan;179(2):322-336. [Content Brief]
- [2]. Cossette C, et al. Metabolism of anti-inflammatory OXE (oxoeicosanoid) receptor antagonists by nonhuman primates. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2022 May 01;172:106144. [Content Brief]
- [3]. Miller LA, et al. Inhibition of allergen-induced dermal eosinophilia by an oxoeicosanoid receptor antagonist in non-human primates. British journal of pharmacology. 2020 Jan;177(2):360-371. [Content Brief]
- [4]. Ye Q, et al. Novel highly potent OXE receptor antagonists with prolonged plasma lifetimes that are converted to active metabolites in vivo in monkeys. British journal of pharmacology. 2020 Jan;177(2):388-401. [Content Brief]
Keywords
