Discovery of 1,2-Diol TRPV4 Antagonists with Efficacy in Organoid and Murine Models

Na Chen published a dataset on figshare in May 2026 detailing a series of optimized TRPV4 antagonist compounds. The data includes results from a single-point TRPV4 Ca2+ influx assay and validation in 3D myocardial organoids and a murine TAC pressure-overload model. The dataset is 3.2 MB and available in PDB format under a CC-BY-NC-4.0 license.

Use Cases

• Structure-activity relationship (SAR) analysis based on the series of active analogues generated from AH001.
• Validation of anti-fibrotic drug candidates based on phenotypic suppression in oxygen–glucose deprivation-induced 3D myocardial organoids.
• Assessment of in vivo efficacy based on cardiac function improvement in a murine transverse aortic constriction (TAC) pressure-overload model.
• Identification of promising lead compounds based on reported IC50 values for fibrosis-associated phenotypes.

Strengths

• Includes in vitro assay data (TRPV4 Ca2+ influx assay at 5 μM) and in vivo model results.
• Reports a specific phenotypic IC50 value of 6.45 μM for compound 26 in the organoid model.
• Data is structured around a focused series of compounds derived from a known antagonist (AH001).

Limitations

• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.
• Data may reflect experimental bias inherent to the specific organoid and murine models used.

Provenance

Source

Na Chen via figshare

Collection Method

Structure-guided optimization and experimental validation.

Freshness

Last updated 2026-05-14 15:07:00; freshness should be verified.