| Bioactivity | PLN-1474 (compound 1) is an orally active and selective avß1 integrin inhibitor with an IC50 value of ＜50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or treating a fibrotic or cirrhotic disease or disorder[1]. | ||||||||||||
| Target | IC50: ＜50 nM (ανβ1), ＜50 nM (ανβ6) | ||||||||||||
| Invitro | PLN-1474 inhibits ανβ1 and ανβ6 with IC50s of ＜50 nM by solid phase assay[1]. | ||||||||||||
| In Vivo | PLN-1474 (10 μM) decreases the expression level of profibrotic genes, including COL1A1 and TIMP1 in liver[1].PLN-1474 significantly reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in a mouse model of liver fibrosis[1].PLN-1474 (6-12 weeks) prophylactically or therapeutically blocks SMAD3 phosphorylation and significantly decreases OHP levels, collagen gene expression, and collagen deposition examined histologically in the CDAHFD NASH mouse model[1]. | ||||||||||||
| Name | PLN-1474 | ||||||||||||
| CAS | 2408065-32-5 | ||||||||||||
| Formula | C24H37N3O4 | ||||||||||||
| Molar Mass | 431.57 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Anderson Kraig, et al. Combination treatment of liver diseases using integrin inhibitors. WO2021127483. 2021. |