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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.

For research use only. We do not sell to patients.

CAS No.: 2307429-54-3
Formula: C₁₁H₂₂N₄O₃
Molecular Weight: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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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
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Biological Activity

Description

All TGF-β Receptor Isoforms :

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
Molecular Weight 258.32
Formula C₁₁H₂₂N₄O₃
SMILES

NC(C(C)(C)NC([C@@H](NC(C)=O)CCCN)=O)=O
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Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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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How should lyophilized recombinant proteins be reconstituted and stored?

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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Biological Activity
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- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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SRI-35241

All TGF-β Receptor Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

SRI-35241 Related Classifications

HY-182612 Related Classifications