2901868-37-7
Chemical Structure
PIPE-791
- CAS No.: 2901868-37-7
- Formula:C24H29F2N3O5
- Molecular Weight:477.50
InChIKey: QYPPPLPDAQVCOC-WKILWMFISA-N
SMILES: COC1=NC(OC(F)F)=C(NC(N([C@@H]2CC[C@@H](C(O)=O)CC2)C3=CC=CC=C3C(C)C)=O)C=C1
Biological Activity: PIPE-791 is an orally active, blood-brain barrier-permeable selective antagonist of LPAR1. PIPE-791 inhibits LPA-induced calcium mobilization, collagen expression, histamine release, and the activation of fibroblasts, microglia and macrophages. PIPE-791 induces oligodendrocyte precursor cell differentiation, myelination and remyelination, and increases the number of microglia in the retina of normotensive rats. PIPE-791 protects mature oligodendrocytes from cytokine-induced death, reduces the levels of pulmonary fibrosis markers and alleviates neuroinflammation in preclinical models. PIPE-791 can be used in the research of glaucoma, neuroinflammatory diseases, chronic osteoarthritis pain, idiopathic pulmonary fibrosis and multiple sclerosis[1][2][3][4].
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PIPE-791 | PIPE-791 is an orally active, blood-brain barrier-permeable selective antagonist of LPAR1. PIPE-791 inhibits LPA-induced calcium mobilization, collagen expression, histamine release, and the activation of fibroblasts, microglia and macrophages. PIPE-791 induces oligodendrocyte precursor cell differentiation, myelination and remyelination, and increases the number of microglia in the retina of normotensive rats. PIPE-791 protects mature oligodendrocytes from cytokine-induced death, reduces the levels of pulmonary fibrosis markers and alleviates neuroinflammation in preclinical models. PIPE-791 can be used in the research of glaucoma, neuroinflammatory diseases, chronic osteoarthritis pain, idiopathic pulmonary fibrosis and multiple sclerosis. | |||||||||||||||||||||
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References
- [1]. Kocherlakota S, et al. Pharmacological Blockade of LPAR1 Does Not Provide Neuroprotection in a Rat Model of Ocular Hypertensive Glaucoma. Translational vision science & technology. 2026 Jan 05;15(1):11. [Content Brief]
- [2]. Chen A, et al. Discovery of , A Potent and Brain-Penetrant Lysophosphatidic Acid Receptor 1 Antagonist with Slow Tight Binding Characteristics for the Treatment of Neuroinflammatory Disorders. Journal of medicinal chemistry. 2026 Jul 09;69(13):15888-15927. [Content Brief]
- [3]. Poon M, et al. The LPAR1 antagonist, PIPE-791 produces antifibrotic effects in models of lung fibrosis. Respiratory research. 2025 Aug 31;26(1):265. [Content Brief]
- [4]. Poon MM, et al. Discovery of a brain penetrant small molecule antagonist targeting LPA1 receptors to reduce neuroinflammation and promote remyelination in multiple sclerosis. Scientific reports. 2024 May 08;14(1):10573. [Content Brief]
