Bexotegrast - CAS:2376257-44-0

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Bexotegrast

目录号 : KM24924 CAS No. : 2376257-44-0 纯度 : 98%

Data Sheet 产品使用指南

Bexotegrast is a potent inhibitor of ανβ6 integrin. Bexotegrast can be used for researching fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP) (extracted from patent WO2020210404A1, compound 5).

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock
10 mM * 1 mL in DMSO		In-stock

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生物活性

体外研究

Bexotegrass (PLN-74809; 1.82 µM; incubated for 7 days) significantly reduced the expression of type I collagen alpha I (COL1A1) mRNA by 54% in precision cut lung sections (PCLS). Bexotegrass showed a decrease of approximately 50% in Smad2 phosphorylation.

Bexotegrass (1.82 µM; incubation for 3 days) dose dependently reduced Col1a1 mRNA expression in PCLS prepared from fibrotic mouse lungs by up to 71%.

Bexotegrass completely inhibits the adhesion of normal human bronchial epithelial cells to LAP mediated by α v β 6 integrin, with an IC₅₀ of 39.3 nM.

体内研究

Bexotegrass (PLN-74809; oral; 100、250、500 mg/kg； Twice a day; Dose dependent reduction of interstitial fibrocollagen deposition in mice challenged with bleomycin from day 7 to day 21. Bexotegrass dose dependently blocks Smad3 phosphorylation.

Animal Model:	C57BL/6 mice
Dosage:	100, 250, and 500 mg/kg
Administration:	Orally; twice daily; from Day 7 to Day 21
Result:	Showed a dose-dependent, significant reduction in interstitial fibrillar collagen deposition in Bleomycin (3 units/kg)-challenged mice. Dose-dependently blocked Smad3 phosphorylation.

分子式

C₂₇H₃₆N₆O₃

分子量

492.61

CAS号

2376257-44-0

中文名称

Bexotegrast

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:?

DMSO : 100 mg/mL (203.00 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0300 mL	10.1500 mL	20.3000 mL
5 mM	0.4060 mL	2.0300 mL	4.0600 mL
10 mM	0.2030 mL	1.0150 mL	2.0300 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： PBS

Solubility: 12.5 mg/mL (25.38 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.08 mg/mL (4.22 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.22 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
3.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.22 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.22 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
4.

请依序添加每种溶剂：10% DMSO → 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.22 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.22 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。