Disitertide (P144) prevents TGF-β1-dependent inhibition of MV1Lu proliferation in vitro and markedly reduces binding of TGF-β1 to its receptors. Disitertide blocks TGF-β1-dependent stimulation of a reporter gene under the control of human α2(I) collagen promoter.
In vivo, treatment with Disitertide at low doses causes a significant inhibition of HSC activation and a marked reduction in liver fibrosis in a rat model of chronic exposure to CCl4. A dose as low as 70 μg of the 15-mer peptide Disitertide, given to rats (300 g body weight) on alternate days, decreases fibrogenesis significantly during chronic exposure to CCl4.
Pathol Oncol Res. 2021 Apr 29;27:1609761.
MiR-543 Inhibits the Migration and Epithelial-To-Mesenchymal Transition of TGF-β-Treated Endometrial Stromal Cells via the MAPK and Wnt/β-Catenin Signaling Pathways
Disitertide purchased from AbMole
Molecular Weight | 1580.82 |
Formula | C68H109N17O22S2 |
CAS Number | 272105-42-7 |
Solubility (25°C) | DMSO 10 mg/mL |
Storage | -20°C, protect from light, dry, sealed |
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.
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