SB273005

製品コードS7540 バッチS754001

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

C₂₂H₂₄F₃N₃O₄

分子量

451.44

CAS No.

205678-31-5

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

90 mg/mL (199.36 mM)

Ethanol (warmed with 50ºC water bath)

16 mg/mL (35.44 mM)

Water

Insoluble

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.
	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。	4.500mg/ml (9.97mM)
	5% DMSO 1 95% Corn oil 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。	0.500mg/ml (1.11mM)

* <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	SB273005 is a potent integrin inhibitor with K_i of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.
in vitro	In vitro, SB273005 inhibits human osteoclast-mediated bone resorption with IC50 of 11 nM. ^[1] In blood containing MDA-MB-231 cells, a combination of this compound and lamifiban inhibits tumor cell adhesion to vascular extracellular matrix (ECM). ^[3]
in vivo	In rat models of bone resorption and osteoporosis, SB273005 (30 mg/kg, p.o.) inhibits the parathyroid hormone-stimulated calcemic response, and inhibits bone loss. ^[1] In rat with adjuvant-induced arthritis, this compound (60 mg/kg, p.o.) significantly reduces the symptoms of adjuvant-induced arthritis. ^[2] This compound (1000 mg/kg/day, p.o.) causes acute, transient necrosis of vascular smooth muscle cell (VSMC) in aorta and renal arteries of mice. ^[4] In pregnant mice, this compound reverses the reduction of Th1 cell-produced IL-2 levels and the increase of Th2 cell-derived IL-10 levels. ^[5]

製品説明

SB273005 is a potent integrin inhibitor with K_i of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.

in vitro

In vitro, SB273005 inhibits human osteoclast-mediated bone resorption with IC50 of 11 nM. ^[1]

In blood containing MDA-MB-231 cells, a combination of this compound and lamifiban inhibits tumor cell adhesion to vascular extracellular matrix (ECM). ^[3]

in vivo

In rat models of bone resorption and osteoporosis, SB273005 (30 mg/kg, p.o.) inhibits the parathyroid hormone-stimulated calcemic response, and inhibits bone loss. ^[1]

In rat with adjuvant-induced arthritis, this compound (60 mg/kg, p.o.) significantly reduces the symptoms of adjuvant-induced arthritis. ^[2]

This compound (1000 mg/kg/day, p.o.) causes acute, transient necrosis of vascular smooth muscle cell (VSMC) in aorta and renal arteries of mice. ^[4]

In pregnant mice, this compound reverses the reduction of Th1 cell-produced IL-2 levels and the increase of Th2 cell-derived IL-10 levels. ^[5]

プロトコル(参考用のみ)

キナーゼアッセイ	Binding assay
キナーゼアッセイ	Binding affinity for human αvβ3 and αvβ5 is determined in a competitive binding assay employing 3H-SK&F 107260 as the displaced ligand. The Ki values represent the means of values determined in two to three separate experiments.
細胞アッセイ	細胞株	A375 cells
	濃度	100 nM
	反応時間
	実験の流れ
動物実験	動物モデル	Thyroidectomized−parathyroidectomized (TPTx) rat model of bone resorption, and ovariectomized (Ovx) rat model of osteoporosis
	投薬量	30 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/10633035/
https://pubmed.ncbi.nlm.nih.gov/11212150/
https://pubmed.ncbi.nlm.nih.gov/15679053/

https://pubmed.ncbi.nlm.nih.gov/18098042/
https://pubmed.ncbi.nlm.nih.gov/24926365/
https://pubmed.ncbi.nlm.nih.gov/36229674/

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カスタマーフィードバック

: Data from [Data independently produced by , , Int J Oncol, 2017, 50(5):1899-1914]

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：

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Graphene-based 3D-Printed nanocomposite bioelectronics for monitoring breast cancer cell adhesion [ Biosens Bioelectron, 2023, 226:115113]	PubMed: 36764127
E-cadherin Force Transmission and Stiffness Sensing [ ODU Digital Commons , 2023, 30426293]	PubMed: none
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A temperature-regulated circuit for feeding behavior [ Nat Commun, 2022, 13(1):4229]	PubMed: 35869064
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CCN1 interacts with integrins to regulate intestinal stem cell proliferation and differentiation [ Nat Commun, 2022, 13(1):3117]	PubMed: 35660741

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。