Disitertide TFA (Synonyms: P144 TFA) |
Catalog No.GC60782
One-Click Copy Product Info
|
Disitertide TFA는 변형 성장 인자 β1 (TGF-β1) 수용체 유형 I의 특이적 억제제이다.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Disitertide TFA는 변형 성장 인자 β1 (TGF-β1) 수용체 유형 I의 특이적 억제제이다. Disitertide는 TGF-β1 수용체에 결합해서 TGF-β1 신호전달 경로를 차단하고 세포외 기질의 침착과 섬유화 반응을 억제해서 섬유화의 진행을 늦추거나 역전시킨다[2-3]. Disitertide는 주로 다양한 기관의 섬유화 질환을 치료하기 위해 사용된다[4].
LINC00941을 과발현하는 HCT-116 세포에서 Disitertide (10μM; 12h)로 처리된 세포는 ZO-1과 E-캐드헤린의 mRNA와 단백질 수준이 증가되었다[5]. LN229 세포에서 Disitertide (100µg/mL; 10d) 자극 후 SKI 유전자 발현이 현저하게 억제되었다[6]. MGC803 세포에서 Disitertide (20μM; 48h)는 TGFβ1 신호를 차단하고 MFSD2A 결핍이 CD8+ T 세포에 미치는 억제 효과를 효과적으로 구제한다[7].
섬유화 토끼 모델에서 Disitertide (3.5mg/kg; 정맥 주사; 72시간)로 처리된 그룹의 근육의 거시적 및 미시적 형태가 보존되었고 세포외 기질 섬유화가 감소되었다[8].
References:
[1]. Neuzillet C, Tijeras-Raballand A, Cohen R, et al. Targeting the TGFβ pathway for cancer therapy[J]. Pharmacology & therapeutics, 2015, 147: 22-31.
[2]. Yang J, Zhuang Y, Liu J. Upregulation of microRNA‑590 in rheumatoid arthritis promotes apoptosis of bone cells through transforming growth factor‑β1/phosphoinositide 3‑kinase/Akt signaling[J]. International Journal of Molecular Medicine, 2019, 43(5): 2212-2220.
[3]. He W, Liang B, Wang C, et al. MSC-regulated lncRNA MACC1-AS1 promotes stemness and chemoresistance through fatty acid oxidation in gastric cancer[J]. Oncogene, 2019, 38(23): 4637-4654.
[4]. Miwa S, Yokota M, Ueyama Y, et al. Discovery of selective transforming growth factor β type II receptor inhibitors as antifibrosis agents[J]. ACS Medicinal Chemistry Letters, 2021, 12(5): 745-751.
[5]. Wu N, Jiang M, Liu H, et al. LINC00941 promotes CRC metastasis through preventing SMAD4 protein degradation and activating the TGF-β/SMAD2/3 signaling pathway[J]. Cell Death & Differentiation, 2021, 28(1): 219-232.
[6]. Kubelt C, Hellmold D, Esser D, et al. Insights into gene regulation under temozolomide-promoted cellular dormancy and its connection to stemness in human glioblastoma[J]. Cells, 2023, 12(11): 1491.
[7]. Zhang B, Wang C M, Wu H X, et al. MFSD2A potentiates gastric cancer response to anti‐PD‐1 immunotherapy by reprogramming the tumor microenvironment to activate T cell response[J]. Cancer Communications, 2023, 43(10): 1097-1116.
[8]. Cruz-Morande S, Dotor J, San-Julian M. P144 a transforming growth factor beta inhibitor peptide, generates antifibrogenic effects in a radiotherapy induced fibrosis model[J]. Current Oncology, 2022, 29(4): 2650-2661.
| 세포 실험 [1]: | |
세포 라인 | LINC00941-과발현 HCT-116 세포 |
제조 방법 | TGF-β1 또는 Disitertide 처리 전에 세포는 80%의 세포 융합을 달성하기 위해 10% 태아 소 혈청과 1% 페니실린/스트렙토마이신이 함유된 DMEM 배양기로 배양되었습니다. 다음으로 세포는 TGF-β1 (0.2ng/mL) 또는 Disitertide (10μM)로 12시간 동안 처리되었습니다. |
반응 조건 | 10μM; 12 시간 동안 |
응용 분야 | Disitertide로 처리된 LINC00941 과발현 HCT-116 세포는 ZO-1과 E-캐드헤린의 mRNA와 단백질 수준이 증가되었습니다. |
| 동물 실험 [2]: | |
동물 모형 | 섬유화 토끼 모형 |
제조 방법 | 조작 전 Disitertide는 -80℃에서 보관되었습니다. 펩타이드 병은 실온에서 온도를 조절한 다음 카본산의 디아조늄염 0.1M pH 9.5 버퍼로 소생시키고 균일한 용액이 얻어질 때까지 초음파 처리되었습니다. Disitertide는 토끼의 귀 가장자리 정맥에 10mg씩 투여되었고 버퍼 10mL로 희석되었습니다 (약 3.5mg/kg). |
제형 | 3.5mg/kg; iv; 72시간 동안 |
응용 분야 | Disitertide로 처리된 그룹의 근육의 거시적 및 미시적 형태가 보존되었고 세포외 기질 섬유화가 감소되었습니다. |
References: | |
| Cas No. | SDF | ||
| Synonyms | P144 TFA | ||
| Formula | C70H110N17O24S2F3 | M.Wt | 1694.84 |
| Solubility | Storage | -20°C, protect from light | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 590 μL | 2.9501 mL | 5.9003 mL |
| 5 mM | 118 μL | 590 μL | 1.1801 mL |
| 10 mM | 59 μL | 295 μL | 590 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >96.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)