Category: 1450824-22-2

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1450824-22-2, Name is TD 139, molecular formula is C28H30F2N6O8S. In a Article£¬once mentioned of 1450824-22-2, Computed Properties of C28H30F2N6O8S

Galectin-3-Binding Glycomimetics that Strongly Reduce Bleomycin-Induced Lung Fibrosis and Modulate Intracellular Glycan Recognition

Discovery of glycan-competitive galectin-3-binding compounds that attenuate lung fibrosis in a murine model and that block intracellular galectin-3 accumulation at damaged vesicles, hence revealing galectin-3?glycan interactions involved in fibrosis progression and in intracellular galectin-3 activities, is reported. 3,3?-Bis-(4-aryltriazol-1-yl)thiodigalactosides were synthesized and evaluated as antagonists of galectin-1, -2, -3, and -4 N-terminal, -4 C-terminal, -7 and -8 N-terminal, -9 N-terminal, and -9 C-terminal domains. Compounds displaying low-nanomolar affinities for galectins-1 and -3 were identified in a competitive fluorescence anisotropy assay. X-ray structural analysis of selected compounds in complex with galectin-3, together with galectin-3 mutant binding experiments, revealed that both the aryltriazolyl moieties and fluoro substituents on the compounds are involved in key interactions responsible for exceptional affinities towards galectin-3. The most potent galectin-3 antagonist was demonstrated to act in an assay monitoring galectin-3 accumulation upon amitriptyline-induced vesicle damage, visualizing a biochemically/medically relevant intracellular lectin?carbohydrate binding event and that it can be blocked by a small molecule. The same antagonist administered intratracheally attenuated bleomycin-induced pulmonary fibrosis in a mouse model with a dose/response profile comparing favorably with that of oral administration of the marketed antifibrotic compound pirfenidone.

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Emerging targets for the treatment of idiopathic pulmonary fibrosis

Idiopathic pulmonary fibrosis (IPF) is a chronic, progressive lung disease characterized by scarring of the lung interstitium that likely occurs because of repetitive wounding of the alveolar epithelium, followed by incomplete healing of the injury. IPF is a disease of high, unmet medical need due to an exceptionally poor prognosis combined with a lack of effective treatment options capable of altering its progression. There is an urgent need for the development of novel pharmacological agents capable of providing significant efficacy while modifying the natural course of the disease. Herein, we describe emerging targets for the treatment of IPF and progress in the development of small-molecule modulators against them. Targets for which there is limited pharmacologic validation or against which only biologic modalities exist are excluded.

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Treatment of pulmonary fibrosis 1 1 times (by machine translation)

[Problem] for the treatment of pulmonary fibrosis, safety and good tolerability compound, a compound of the pharmaceutical composition, the composition and method of administration. [Solution] a method for the treatment of pulmonary fibrosis in human use, the compound represented by the formula below, said compound-containing pharmaceutical compositions, the administration of dry powder inhaler or by administration of the composition and method. The compound is, the narrowest portion of human lung tissue, especially small bronchi and alveoli, which dosing 1 1, 1 1 amount times, preferably 0.15 – 50 mg. [Drawing] no (by machine translation)

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics