Ac-Gly-BoroPro |
| カタログ番号GC32883 |
Ac-Gly-boroproは、23nmのKiを伴う選択的な線維芽細胞活性化タンパク質（FAP）阻害剤である[1，2]。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 886992-99-0
Sample solution is provided at 25 µL, 10mM.
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Ac-Gly-boroproは、23nmのKiを伴う選択的な線維芽細胞活性化タンパク質（FAP）阻害剤である[1，2]。他のプロリンぺプチダーゼと比較してFAPを選択的に阻害する。 [3，4]。これはがん関連の繊維芽細胞および活性化の繊維芽細胞の重要なバイオマーカーである。FAPはAc-Gly-Boroproの層状濃度と容易に反応し、定常状態の阻害レベルに急速に到達する（Ki = 23±3nm）[2]。
Ac-Gly-Boropro（10μM； 24時間または48時間）は人の歯周靭帯幹細胞（HPDLSCS）の増殖と移動を阻害できる。[5]Ac-Gly-Boropro（20μm; 7日間は）破骨細胞の分化を阻害できる[6]。
Ac-Gly-Boropro（500μg/kg； 35日間；腹腔内注射）は卵巣摘出卵巣症を伴う卵巣症を緩和し、骨の形成を促進でき、鼠の吸着剤を阻害できる[6]。Ac-Gly-Boropro（40μg/kg; 4週間；関節内注射）は内側のメニスカス（DMM）鼠モデルの不安定化における軟骨浸食、軟骨下骨肥厚、骨糞の形成を大幅に改善できる[7]。
References:
[1] HENDERSON J M, XIANG M S W, HUANG J C, et al. Dipeptidyl Peptidase Inhibition Enhances CD8 T Cell Recruitment and Activates Intrahepatic Inflammasome in a Murine Model of Hepatocellular Carcinoma [J]. Cancers (Basel), 2021, 13(21):
[2] HU Y, MA L, WU M, et al. Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7 [J]. Bioorg Med Chem Lett, 2005, 15(19): 4239-42.
[3] ZHAO L, CHEN J, PANG Y, et al. Fibroblast activation protein-based theranostics in cancer research: A state-of-the-art review [J]. Theranostics, 2022, 12(4): 1557-69.
[4] KIM S M, JANG Y J. Enzymatic activity of fibroblast activation protein-alpha is essential for TGF-beta1-induced fibroblastic differentiation of human periodontal ligament cells [J]. Exp Cell Res, 2024, 442(2): 114230.
[5] HE J, FANG B, SHAN S, et al. Mechanical stiffness promotes skin fibrosis through FAPalpha-AKT signaling pathway [J]. J Dermatol Sci, 2024, 113(2): 51-61.
[6] WEI H, XU Y, WANG Y, et al. Identification of Fibroblast Activation Protein as an Osteogenic Suppressor and Anti-osteoporosis Drug Target [J]. Cell Rep, 2020, 33(2): 108252.
[7] FAN A, WU G, WANG J, et al. Inhibition of fibroblast activation protein ameliorates cartilage matrix degradation and osteoarthritis progression [J]. Bone Res, 2023, 11(1): 3.
| キナーゼ実験 [３]: | |
準備方法 | AC-Gly-boroproによるプロテアーゼの阻害のKI値は緊密な結合競合阻害剤の分析のための進行曲線の方法を使用して決定される。さまざまな濃度のAc-gly-boroproはアラニンプロリン-7-アミノ-4-メチルカウマリンの存在下で、線維芽細胞活性化のタンパク質（FAP（1.0NM））およびジペプチジルペプチダーゼ4（DPP-4（0.1NM））と反応する（ALA-PRO-AFC（ALA-PRO-DELIDC））各プロテアーゼが監視されている。反応にはプロテアーゼ阻害剤複合体が遊離阻害剤を有意に枯渇させないように、プロテアーゼ濃度よりも少なくとも20倍大きい阻害剤の濃度が含まれている。 |
反応条件 | 23nM; 150s, 300s, 450s, 600s |
アプリケーション | AC-Gly-Boroproは、FAPの活性を迅速に効果的に阻害できる。 |
| 細胞実験[１]: | |
細胞株 | 人の歯周靭帯幹細胞（HPDLSC） |
準備方法 | PDL線維芽細胞分化の誘導のために、HPDLSCをα-MEMで培養し、10ng/ml TGF-β1を含んでいる5％FBSを含む。 |
反応条件 | 10μM; 24hまたは 48h |
アプリケーション | AC-Gly-boroproは、細胞の増殖と移動を阻害できる。 |
| 動物実験 [２]: | |
動物モデル | C57BL/6J野生型鼠 |
準備方法 | 8週齢の野生型の鼠に500mg/kg AC-Gly-Boroproの毎日の腹腔内注射を投与しました。 |
投与形態 | 500mg/kg; 35日;腹腔内注射 |
アプリケーション | Ac-Gly-boroproは骨形成を促進し、体内では骨吸収を阻害する。 |
References: | |
| Cas No. | 886992-99-0 | SDF | |
| Canonical SMILES | Ac-Gly-{boroPro} | ||
| Formula | C8H15BN2O4 | M.Wt | 214.03 |
| 溶解度 | DMSO : ≥ 50 mg/mL (233.61 mM) | Storage | Store at -20°C, protect from light, stored under nitrogen |
| 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 | 4.6722 mL | 23.3612 mL | 46.7224 mL |
| 5 mM | 934.4 μL | 4.6722 mL | 9.3445 mL |
| 10 mM | 467.2 μL | 2.3361 mL | 4.6722 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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 ddH2O, 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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