(S,S)-TAPI-1

製品コードS7434 バッチS743402

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₆H₃₇N₅O₅

分子量

499.60

CAS No.

171235-71-5

Solubility (25°C)*

体外

DMSO

99 mg/mL (198.15 mM)

Water (warmed with 50ºC water bath)

99 mg/mL (198.15 mM)

Ethanol

99 mg/mL (198.15 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.950mg/ml (9.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 99 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	(S,S)-TAPI-1 is an isomer of TAPI-1.TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors. TAPI-1 is also an inhibitor of Matrix Metalloproteinase (MMP).
in vitro	TAPI-1 prevents unstimulated and PMA-induced release of the soluble forms of TNF-alpha, p60 TNFR, and IL-6R from the monocytic cell line, THP-1, and from human peripheral blood monocytes. TAPI also inhibits LPS-induced shedding of the p60 TNFR and TNF-alpha from monocytes. ^[1] TAPI-1 inhibits TACE-dependent constitutive release of co-transfected APP(695). ^[2] TAPI-1 attenuates Ang II-induced EGFR transactivation and cell proliferation in human HSC line LI90. ^[3] TAPI-1 with the EGFR inhibitor AG1478 exhibits deactivated AREG/EGFR/ERK signaling pathway and reduces pro-inflammatory cytokines release in pSS salivary gland-derived epithelial cells. ^[4]
in vivo	TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors

製品説明

(S,S)-TAPI-1 is an isomer of TAPI-1.TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors. TAPI-1 is also an inhibitor of Matrix Metalloproteinase (MMP).

in vitro

TAPI-1 prevents unstimulated and PMA-induced release of the soluble forms of TNF-alpha, p60 TNFR, and IL-6R from the monocytic cell line, THP-1, and from human peripheral blood monocytes. TAPI also inhibits LPS-induced shedding of the p60 TNFR and TNF-alpha from monocytes. ^[1]

TAPI-1 inhibits TACE-dependent constitutive release of co-transfected APP(695). ^[2]

TAPI-1 attenuates Ang II-induced EGFR transactivation and cell proliferation in human HSC line LI90. ^[3]

TAPI-1 with the EGFR inhibitor AG1478 exhibits deactivated AREG/EGFR/ERK signaling pathway and reduces pro-inflammatory cytokines release in pSS salivary gland-derived epithelial cells. ^[4]

in vivo

TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors

プロトコル(参考用のみ)

細胞アッセイ	細胞株	LI90 cells
	濃度	20 μM
	反応時間	60 hours
	実験の流れ	Five thousand cells are seeded into each well of 96-well plates and their viability is assessed by CellTiter-Glo Luminescent Cell Viability assay. Upon serum deprivation for 24 h, the cells are treated with Ang II for 60 h with and without pretreatment with each inhibitor and antagonist. The assay substrates are then added to each well on the plate and the samples are evaluated using a luminometer.
動物実験	動物モデル	Male Sprague-Dawley rats
	投薬量	1 μg
	投与方法	i.c.v.

参考

https://pubmed.ncbi.nlm.nih.gov/7594530/
https://pubmed.ncbi.nlm.nih.gov/11463349/
https://pubmed.ncbi.nlm.nih.gov/24412389/

https://pubmed.ncbi.nlm.nih.gov/24664458/
https://pubmed.ncbi.nlm.nih.gov/31822434/
https://pubmed.ncbi.nlm.nih.gov/31154904/

+ 展开

カスタマーフィードバック

: Data from [Data independently produced by , , Sci Rep, 2017, 7:46315]

: Data from [Data independently produced by , , Biochim Biophys Acta Gen Subj, 2018, 1862(9):1988-1994]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

ADAM17 Inhibition Protects Cognition in Intermittent Hypoxia: The Role of TREM2 [ Nat Sci Sleep, 2025, 17:1915-1928]	PubMed: 40896259
Immune evasion in lung metastasis of leiomyosarcoma: upregulation of EPCAM inhibits CD8+ T cell infiltration [ Br J Cancer, 2024, 10.1038/s41416-024-02576-z]	PubMed: 38291183
Downregulation of PIK3IP1/TrIP on T cells is controlled by TCR signal strength, PKC, and metalloprotease-mediated cleavage [ J Biol Chem, 2024, 300(12):107930]	PubMed: 39454954
Semaphorin 7A promotes endothelial permeability and inflammation via plexin C1 and integrin β1 in Kawasaki disease [ BMC Pediatr, 2024, 24(1):285]	PubMed: 38678170
Multiplex interrogation of the NK cell signalome reveals global downregulation of CD16 signaling during lentivirus infection through an IL-18/ADAM17-dependent mechanism [ PLoS Pathog, 2023, 19(9):e1011629]	PubMed: 37669308
Epithelial cell adhesion molecule (EpCAM) regulates HGFR signaling to promote colon cancer progression and metastasis [ J Transl Med, 2023, 21(1):530]	PubMed: 37543570
Epithelial cell adhesion molecule (EpCAM) regulates HGFR signaling to promote colon cancer progression and metastasis [ J Transl Med, 2023, 21(1):530]	PubMed: 37543570
Multiplex interrogation of the NK cell signalome reveals global downregulation of CD16 signaling during lentivirus infection through an IL-18/ADAM17-dependent mechanism [ PLoS Pathog, 2023, 19(9):e1011629]	PubMed: 37669308
MiR-92a/KLF4/p110δ regulates titanium particles-induced macrophages inflammation and osteolysis [ Cell Death Discov, 2022, 8(1):197]	PubMed: 35418181
The collectrin-like part of the SARS-CoV-1 and -2 receptor ACE2 is shed by the metalloproteinases ADAM10 and ADAM17 [ FASEB J, 2022, 36(3):e22234]	PubMed: 35199397

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。