SRI-35241 

SRI-35241 is a thrombospondin TSP-1 inhibitor with a pIC₅₀ of 8.12 nM against human targets. SRI-35241 inhibits the binding of TSP-1 to latent transforming growth factor-β-associated peptide (LAP) and blocks the activation of TGF-β. SRI-35241 shows a certain time-dependent property, with a plasma half-life of 1.8 h after intravenous administration. SRI-35241 can be used for the research of multiple myeloma and fibrotic diseases^[1].

SRI-35241 inhibits thrombospondin 1-mediated TGF-β activation in human myeloma cells with a pIC₅₀ of 8.12 nM^[1].
SRI-35241 (10 nM; 10 min) inhibits binding of recombinant LAP to recombinant thrombospondin 1 type 1 repeats (P123) by ~85% at 10 nM in an indirect binding ELISA assay^[1].
SRI-35241 has a half-life of 170 min in rat liver microsomes and >300 min in human liver microsomes, indicating improved microsomal stability compared to the parent compound^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SRI-35241 exhibits improved in vivo plasma stability compared to the parent compound, with a 1.9 hour half-life via i.v. administration and a 7 hour half-life via i.p. administration, resulting in sustained plasma levels above its pIC₅₀^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

258.32

C₁₁H₂₂N₄O₃

2307429-54-3

NC(C(C)(C)NC([C@@H](NC(C)=O)CCCN)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Suto MJ, et al. Identification of Inhibitors of Thrombospondin 1 Activation of TGF-β. ACS Med Chem Lett. 2020;11(6):1130-1136. Published 2020 May 7.