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Organic compounds in which a hydrogen atom or more has been replaced by a halogen atom in an alkane molecule (saturated hydrocarbon chain). Halogen atoms include bromine, chlorine, fluorine, and iodine. Compounds may be in closed ring configurations.
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RN-1665 is an orally active TRPV4 antagonist that exhibits excellent selectivity for related TRP receptors such as TRPV1, TRPV3, and TRPM8. RN-1665 is a TRPV4 probe for focus screens, with IC50s of 0.26 μM and 0.39 μM for hTRPV4 and rTRPV4 from human and rat, respectively.
IC50 for human TRPV4 is 0.26 μM.
IC50 for rat TRPV4 is 0.39 μM.
Antagonist activity at human TRPV4 receptor expressed in HEK293 cells assessed as inhibition of EC80 of 4alpha-PDD-stimulated calcium flux after 10 minutes.
Antagonist activity at rat TRPV4 receptor expressed in HEK293 cells assessed as inhibition of EC80 of 4alpha-PDD-stimulated calcium flux after 10 minutes.
Pharmacokinetic analysis has been performed in Wistar rats.
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TEPC466 is a novel TEPP-46-based aggregation-induced emission (AIE) probe that shows high selectivity and sensitivity for detecting the PKM2 protein via the AIE effect. It can be used for PKM2 detection and has been successfully applied in imaging the PKM2 protein in colorectal cancer cells with low toxicity. It is a useful tool for cancer diagnosis and research.
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