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272105-42-7

272105-42-7 Structure

272105-42-7 Structure
IdentificationBack Directory
[Name]

Disitertide
[CAS]

272105-42-7
[Synonyms]

disitertide
P144 Peptide
TSLDASIIWAMMQN
DISITERTIDE, >98%
P144;P144 PEPTIDE
Disitertide,P144,P144 Peptide, >98%
L-Asparagine, 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-Threonyl-L-seryl-L-leucyl-L-alpha-aspartyl-L-alanyl-L-seryl-L-isoleucyl-L-isoleucyl-L-tryptophyl-L-alanyl-L-methionyl-L-methionyl-L-glutaminyl-L-asparagine
[Molecular Formula]

C68H109N17O22S2
[MOL File]

272105-42-7.mol
[Molecular Weight]

1580.84
Chemical PropertiesBack Directory
[Boiling point ]

1968.7±65.0 °C(Predicted)
[density ]

1.327
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : ≥ 200 mg/mL (126.52 mM);Water : < 0.1 mg/mL (insoluble)
[form ]

Solid
[pka]

3.15±0.10(Predicted)
[color ]

White to off-white
[InChI]

InChI=1/C68H109N17O22S2/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)/t32-,33-,34-,35-,36+,40-,41-,42-,43-,44-,45-,46-,47-,48-,52-,53-,54-/s3
[InChIKey]

IUYPEUHIWDMJLM-INGCBPSVNA-N
[SMILES]

C(C1=CNC2=CC=CC=C12)[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@H](C(=O)O)CC(=O)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](N)[C@H](O)C |&1:10,14,19,27,35,44,55,56,63,64,71,77,82,90,98,104,106,r|
Hazard InformationBack Directory
[Description]

Disitertide is an inhibitor of TGF-β1. It 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. 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.
[Biological Activity]

Disitertide (P144) TFA is a polypeptide inhibitor of transforming growth factor TGFβ1, specifically blocking its interaction with the receptor. Disitertide (P144) is also an inhibitor of PI3K and an inducer of apoptosis.
[in vitro]

Disitertide (100 μg/mL) suppresses the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells.
Disitertide (TGF-β1 inhibitor) abrogates the MACC1- AS1 expression in GC cells, suggesting that targeting TGFβ signaling pathway may be a potential strategy to inhibit MSC-induced stemness and chemoresistance.
Disitertide (P144, 10 μg/mL to 200 μg/mL) affects proliferation,

Western Blot Analysis

< td class="col2"> Significantly suppressed the protein expression levels of PI3K and p-Akt, and induced the protein expression of Bax in MC3T3-E1 cells compared with the miR-590 group. table>
Cell Line: Mouse embryo osteoblast precursor MC3T3-E1 cells.
Concentration:
Concentration: 100 μg/mL.
Incubation Time: 4 h.
Result:
[in vivo]

Disitertide (Topical application, 300 μg/mL) may promote scar maturation and clinical improvement of hypertrophic scar morphology features in an “in vivo” model in nude mice after two weeks of treatment.

Animal Model: Human hypertrophic scars were implanted in 60 nude mice.
Dosage: 300 μg/mL was added the Lipogel.
Administration: Topical application daily administered.
Result: Successful shedding was achieved in 83,3% of the xenografts.
[storage]

Store at -20°C
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