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Cat. No.: HY-182612

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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.

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CAS No.: 2307429-54-3
Formule: C₁₁H₂₂N₄O₃
Masse moléculaire:258.32

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

SRI-35241 Chemical Structure

CAS No.: 2307429-54-3

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Activité biologique
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Activité biologique

Description

Voir tous les produits spécifiques à Isoform TGF-β Receptor :

In Vitro

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.

In Vivo

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.

Chemical Information

CAS No. 2307429-54-3
Masse moléculaire 258.32
Formule C₁₁H₂₂N₄O₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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. [Content Brief]

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1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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SRI-35241

Voir tous les produits spécifiques à Isoform TGF-β Receptor

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Chemical Information

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Références

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SRI-35241 Related Classifications

HY-182612 Related Classifications