Bivalirudin TFA
(Synonyms: 三氟醋酸比伐卢定) 目录号 : GC35528
A thrombin inhibitor
Cas No.:1191386-55-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Bivalirudin is an inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities.1 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.2 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.3 Formulations containing bivalirudin have been used to prevent ischemic events during angioplasty for thrombus-containing lesions.4
1.Witting, J.I., Bourdon, P., Brezniak, D.V., et al.Thrombin-specific inhibition by and slow cleavage of hirulog-1Biochem J.283(Pt 3)737-743(1992) 2.Ofosu, F.A., Fenton, J.W., II, Maraganore, J.M., et al.Inhibition of the amplification reactions of blood coagulation by site-specific inhibitors of α-thrombinBiochem J.283(Pt 3)893-897(1992) 3.Hamelink, J.K., Tang, D.B., Barr, C.F., et al.Inhibition of platelet deposition by combined hirulog and aspirin in a rat carotid endarterectomy modelJ. Vasc. Surg.21(3)492-498(1995) 4.Shah, P.B., Ahmed, W.H., Ganz, P., et al.Bivalirudin compared with heparin during coronary angioplasty for thrombus-containing lesionsJ. Am. Coll. Cardiol.30(5)1264-1269(1997)
| Cas No. | 1191386-55-6 | SDF | |
| 别名 | 三氟醋酸比伐卢定 | ||
| Canonical SMILES | O=C(O)C(F)(F)F.[{d-Phe}-PRPGGGGNGDFEEIPEEYL] | ||
| 分子式 | C100H138DF3N24O35 | 分子量 | 2295.31 |
| 溶解度 | Water: 100 mg/mL (43.57 mM); DMSO: ≥ 31 mg/mL (13.51 mM) | 储存条件 | -20°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.4357 mL | 2.1784 mL | 4.3567 mL |
| 5 mM | 0.0871 mL | 0.4357 mL | 0.8713 mL |
| 10 mM | 0.0436 mL | 0.2178 mL | 0.4357 mL |
| 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） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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，
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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Thrombin cleaves IL-33 and modulates IL-33-activated allergic lung inflammation
Allergy 2022 Jul;77(7):2104-2120.PMID:34995358DOI:10.1111/all.15210.
Background: Organisms have orchestrated coagulation and immune systems. Although a link between inflammation and haemostasis has been reported in asthma, the interaction mechanism has not been completely elucidated. Here, we investigated the direct link between the mammalian immune and coagulation systems. Methods: Mice were administered protease or antigens intranasally to induce airway inflammation with or without thrombin inhibitors treatment. The effects of thrombin and its inhibitors on interleukin (IL)-33 were investigated both in vivo and in vitro. Peripheral blood mononuclear cells (PBMCs) and plasma from asthma patients are collected to verify the correlation between thrombin and group 2 innate lymphocytes (ILC2s). Results: Low-molecular-weight heparin (LMWH, an indirect inhibitor of thrombin) restrained both papain- and fungus-induced type 2 immune responses in mice by inhibiting IL-33 cleavage. Upon examining the potential thrombin protease consensus sites, we found that IL-33 was directly cleaved by thrombin at specific amino acids (R48 and R106) to generate a mature form of IL-33 with potent biological activity. In addition, we found that Bivalirudin TFA (a direct inhibitor of thrombin) inhibited a variety of type 2 inflammatory responses, such as those in house dust mite (HDM)- and ovalbumin (OVA)-mediated pulmonary inflammation models. We found that plasma thrombin-antithrombin complex (TATc) levels in asthma patients were positively associated with the number and function of IL-33-responder group 2 innate lymphocytes (ILC2s) among peripheral blood mononuclear cells (PBMCs) from asthma patients. Conclusion: The data suggested that thrombin inhibitors administration could be effective in treating lung inflammation by regulating ILC2s via IL-33 maturation, indicating that targeting thrombin is a potential way to treat allergic diseases.