Bivalirudin - CAS:128270-60-0

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Bivalirudin (Synonyms:比伐卢定)

目录号 : KCM10925 CAS No. : 128270-60-0 纯度 : ≥98%

Data Sheet SDS 产品使用指南

Bivalirudin is an inhibitor of α- and ζ-thrombin (Ks = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities. It is selective for α- and ζ-thrombin, lacking activity at trypsin and γ-thrombin, which lacks clotting activity, at a >1,000-fold excess of bivalirudin. Bivalirudin inhibits α-thrombin-stimulated activation of the clotting factors Factor X, Factor V, and prothrombin in contact-activated plasma at a concentration of 0.1 μM. Administration of bivalirudin (0.5-1.5 mg/kg, i.v.) reduces platelet deposition in a rat carotid endarterectomy model in a dose-dependent manner. Formulations containing bivalirudin have been used to prevent ischemic events during angioplasty for thrombus-containing lesions.

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5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock

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生物活性

Bivalirudin, a hirudin analog and anticoagulant, is a direct thrombin inhibitor. Bivalirudin inhibits thrombin-mediated fibrinogen cleavage, coagulation factor activation, and platelet activation by reversibly binding to thrombin. In addition, Bivalirudin also has certain effects of anti-virus, anti-inflammation, and vascular endothelial barrier function protection. Bivalirudin can be used for the research of thrombotic diseases and others[1].

IC₅₀&Target

IL-6 IL-5

体外研究

Bivalirudin (30 μg/mL; 10 min) inhibited the increase in S1PR2 expression and cell permeability induced by Thrombin in HUVECs, and reversed the abnormal distribution of cytoskeletal proteins and β - catenin [1].

Western Blot Analysis

Cell Line:	HUVECs treated Thrombin
Concentration:	30 μg/mL
Incubation Time:	10 min
Result:	Inhibited the level of S1PR2.

体内研究

Bivalirudin (2 mg/kg; intravenous injection; Once every other day; 2 weeks) exhibits anti respiratory syncytial virus activity in newborn C57BL/6 mice [2].
Bivalirudin (2 mg/kg; intravenous injection; Single dose can inhibit thrombus formation in mice.

Animal Model:	C57BL/6 mice aged 5-7 days old treated respiratory syncytial virus (RSV)
Dosage:	2 mg/kg
Administration:	Intravenous injection; every other day; 2 weeks
Result:	Significantly reduced cellular infiltration, inflammatory cytokines (e.g., IL-5, IL-6, CXCL1), and abnormal clotting parameters (e.g., D-dimer, soluble thrombomodulin) in RSV-infected lungs. Normalized viral copy numbers and reversed histopathological changes such as nuclear pyknosis in pneumocytes.

Animal Model:	P2Y₁₂^-- and WT mice with thrombosis induced by perfusion through type III collagen- or tissue factor-coated capillary chambers, and P2Y₁₂^+- mice with mesenteric artery injury induced by 12.5% FeCl₃ solution
Dosage:	2 mg/kg
Administration:	Intravenous injection; single dose
Result:	Significantly inhibited thrombus volume in P2Y₁₂^-- mice in the type III collagen-induced thrombosis model but had no significant effect in wild-type mice. Inhibited thrombosis in both WT and P2Y₁₂^-- mice in the tissue factor-induced thrombosis model. Delayed the time of thrombus appearance and vessel occlusion, but could not completely prevent vessel occlusion in wild-type mice in the FeCl₃-induced mesenteric artery injury model in P2Y₁₂^+- mice.

分子式

C₉₈H₁₃₈N₂₄O₃₃

分子量

2180.29

CAS号

128270-60-0

中文名称

比伐卢定

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

H2O : 10 mg/mL (4.59 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.4587 mL	2.2933 mL	4.5865 mL
5 mM	---	---	---
10 mM	---	---	---

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)。-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。

纯度： ≥98%

Data Sheet

SDS

产品使用指南

[1]. Ye H, et al. Bivalirudin Attenuates Thrombin-Induced Endothelial Hyperpermeability via S1P/S1PR2 Category: Original Articles. Front Pharmacol. 2021 Aug 3;12:721200.

[2]. Zhuang S, et al. Bivalirudin exerts antiviral activity against respiratory syncytial virus-induced lung infections in neonatal mice. Acta Pharm. 2022 Apr 13;72(3):415-425.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

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第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

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工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器