中文名称:

地司特泰

中文同义词:

L-苏氨酰-L-丝氨酰-L-亮氨酰-L-ALPHA-天冬氨酰-L-丙氨酰-L-丝氨酰-L-异亮氨酰-L-异亮氨酰-L-色氨酰-L-丙氨酰-L-蛋氨酰-L-蛋氨酰-L-谷氨酰胺酰-L-天冬酰胺;地司特泰;地司特肽;TGF-Β1抑制剂(DISITERTIDE)

英文名称:

Disitertide

英文同义词:

disitertide;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;P144 Peptide;P144;P144 PEPTIDE;TSLDASIIWAMMQN;DISITERTIDE, >98%;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-

CAS号:

272105-42-7

分子式:

C68H109N17O22S2

分子量:

1580.84

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

272105-42-7.mol

沸点 

1968.7±65.0 °C(Predicted)

密度 

1.327

酸度系数(pKa)

3.15±0.10(Predicted)

生物活性

Disitertide (P144) TFA 是转化生长因子 TGFβ1 的多肽抑制剂，特异性的阻断其与受体间的相互作用。Disitertide (P144) 也是PI3K 的抑制剂和凋亡 (apoptosis) 诱导剂。

体外研究

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, induces apoptosis as well as anoikis in A172 and U-87 MG GBM cell lines. Western Blot Analysis Cell Line: Mouse embryo osteoblast precursor MC3T3-E1 cells. Concentration: 100 μg/mL. Incubation Time: 4 h. Result: Significantly suppressed the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells compared with the miR-590 group.

Cell Line:

Mouse embryo osteoblast precursor MC3T3-E1 cells.

Concentration:

100 μg/mL.

Incubation Time:

4 h.

Result:

Significantly suppressed the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells compared with the miR-590 group.

体内研究

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.

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.