A peptide inhibitor of TGF-β1-mediated activity
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Disitertide (ammonium salt)

Item No. 46128

Technical Information
Formal Name
L-threonyl-L-seryl-L-leucyl-L-α-aspartyl-L-alanyl-L-seryl-L-isoleucyl-L-isoleucyl-L-tryptophyl-L-alanyl-L-methionyl-L-methionyl-L-glutaminyl-L-asparagine, diammonium salt
CAS Number
3107565-51-2
Synonyms
  • P144
Molecular Formula
C68H109N17O22S2 • 2NH3
Formula Weight
Purity
≥95%
A solid
Peptide Sequence
TSLDASIIWAMMQN-OH
SMILES
C[C@@H](O)[C@H](N)C(N[C@@H](CO)C(N[C@@H](CC(C)C)C(N[C@@H](CC(O)=O)C(N[C@@H](C)C(N[C@@H](CO)C(N[C@@H]([C@@H](C)CC)C(N[C@@H]([C@@H](C)CC)C(N[C@H](C(N[C@@H](C)C(N[C@@H](CCSC)C(N[C@@H](CCSC)C(N[C@@H](CCC(N)=O)C(N[C@H](C(O)=O)CC(N)=O)=O)=O)=O)=O)=O)CC1=CNC2=CC=CC=C12)=O)=O)=O)=O)=O)=O)=O)=O.N.N
InChi Code
InChI=1S/C68H109N17O22S2.2H3N/c1-12-32(5)53(85-67(105)54(33(6)13-2)84-64(102)48(30-87)82-56(94)35(8)74-61(99)45(27-51(91)92)79-62(100)43(24-31(3)4)78-63(101)47(29-86)83-65(103)52(71)36(9)88)66(104)80-44(25-37-28-72-39-17-15-14-16-38(37)39)60(98)73-34(7)55(93)75-41(20-22-108-10)58(96)77-42(21-23-109-11)59(97)76-40(18-19-49(69)89)57(95)81-46(68(106)107)26-50(70)90;;/h14-17,28,31-36,40-48,52-54,72,86-88H,12-13,18-27,29-30,71H2,1-11H3,(H2,69,89)(H2,70,90)(H,73,98)(H,74,99)(H,75,93)(H,76,97)(H,77,96)(H,78,101)(H,79,100)(H,80,104)(H,81,95)(H,82,94)(H,83,103)(H,84,102)(H,85,105)(H,91,92)(H,106,107);2*1H3/t32-,33-,34-,35-,36+,40-,41-,42-,43-,44-,45-,46-,47-,48-,52-,53-,54-;;/m0../s1
InChi Key
LVWKFZKHDAJWBZ-ZVVBWPFJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Disitertide is a peptide inhibitor of TGF-β1-mediated activity that corresponds to amino acids 730-743 of the membrane proximal ligand-binding domain of human TGF-β receptor type 3 (TGFBR3), also known as beta-glycan.1,2 It inhibits the binding of TGF-β1 to TGF-β1 receptors in Mv 1 Lu mink lung epithelial cells by 95% at 200 µg/ml and rescues TGF-β1-inhibited growth in the same cells.1 Disitertide reduces TGF-β1-mediated reporter expression in primary human fetal skin fibroblasts at 50 and 100 µg/ml and decreases hepatic stellate cell (HSC) activation and liver fibrosis in a rat model of chronic liver injury. Topical application of disitertide reduces connective tissue growth factor (CTGF) levels and the number of myofibroblasts expressing α-smooth muscle actin (α-SMA) in the skin secretions of mice in a model of scleroderma and decreases dermal fibrosis in the same model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ezquerro, I.-J., Lasarte, J.-J., Dotor, J., et al. A synthetic peptide from transforming growth factor β type III receptor inhibits liver fibrogenesis in rats with carbon tetrachloride liver injury. Cytokine 22(1-2), 12-20 (2003).

    2. Santiago, B., Gutierrez-Cañas, I., Dotor, J., et al. Topical application of a peptide inhibitor of transforming growth factor-β1 ameliorates bleomycin-induced skin fibrosis. J. Invest. Dermatol. 125(3), 450-455 (2005).