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ITD-1

Cat. No. M9243
ITD-1 Structure
Size Price Availability Quantity
5mg USD 70  USD70 In stock
10mg USD 105  USD105 In stock
25mg USD 190  USD190 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

ITD-1 potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2. ITD-1 strongly inhibits TGFβ2 signaling with similar efficacy (92% vs. 99% respectively), but with lower potency compared to SB-431542, an ACVR1B/TGFBR1 kinase inhibitor (IC50= 850nM vs. 70nM respectively), and is a weak and partial inhibitor of Activin A signals. ITD-1 selectively enhances the differentiation of uncommitted mesoderm to cardiomyocytes, but not to vascular smooth muscle and endothelial cells.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 415.52
Formula C27H29NO3
CAS Number 1099644-42-4
Purity >99%
Solubility DMSO ≥ 50 mg/mL
Storage at -20°C
References

[1] Willems E, et al. Cell Stem Cell. Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells.

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Keywords: ITD-1 supplier, TGF-beta/Smad, inhibitors

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