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Search results for: Anti rabbit Antithrombin

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#32470586   2020/05/26 To Up

Antibacterial, anticoagulant and cytotoxic evaluation of biocompatible nanocomposite of chitosan loaded green synthesized bioinspired silver nanoparticles.

Present work reports the green synthesis of chitosan functionalized silver nanoparticles (CS-AgNPs) using ethanolic buds extract of Sygyzium aromaticum. CS-AgNPs were characterized physically, evaluated for antibacterial, anticoagulant and antiplatelet activities, and toxicity profile. The physical characterization of CS-AgNPs was done by UV/vis, SEM, TEM, FTIR and EDX. The sphericity was found uniform. FTIR and EXD showed noninterfering few impurities. The antibacterial activity against VRSA (ZI, 23.2 ± 0.51 mm) and MRSA (ZI, 25.8 ± 0.32 mm) were determined. The rise in bleeding and thromboplastin was observed highly significant while increased in prothrombin and activated partial prothrombin time in significant manner at both the doses of CS-AgNPs (0.025 mg/kg and 0.05 mg/kg). Reduction in the levels of fibrinogen was also highly significant. Platelet aggregation decreased at high dose of CS-AgNPs i.e. 55.14 ± 8.25% (arachidonic acid) and 13.06 ± 2.17% (collagen). Thrombin antithrombin (TAT) complex activity was found highest for CS-AgNPs. Cytotoxicity was assessed using HeLa cell lines (LC; 125 μg/ml) and brine shrimp lethality tests (LC 518 μg/ml). The work suggests that green synthesized chitosan functionalized silver nanoparticles may be utilized as an effective antibacterial agent and anticoagulant with low toxicity. The current findings will open a new window for nanomedicine development and future clinical application.
Muhammad Arif Asghar, Rabia Ismail Yousuf, Muhammad Harris Shoaib, Muhammad Asif Asghar

2064 related Products with: Antibacterial, anticoagulant and cytotoxic evaluation of biocompatible nanocomposite of chitosan loaded green synthesized bioinspired silver nanoparticles.

5 G100 assays1 kit1 kit20 ul5 x 50 Pieces/case 1 mg1,000 tests100 tests100ul

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#32289860   2020/04/14 To Up

Effects of Native Fucosylated Glycosaminoglycan, Its Depolymerized Derivatives on Intrinsic Factor Xase, Coagulation, Thrombosis, and Hemorrhagic Risk.

A native fucosylated glycosaminoglycan from sea cucumber (nHG), mainly branched with Fuc, exhibited potent anticoagulant activity by intrinsic tenase iXase (FIXa-FVIIIa complex) and antithrombin-dependent factor IIa (FIIa) inhibition, but also had the effects of FXII activation and platelet aggregation. For screening a selective iXase inhibitor, depolymerized nHG (dHG-1 ∼ -6) and a pure octasaccharide (oHG-8) were prepared. Like nHG, dHG-1 ∼ -6 and oHG-8 could potently inhibit iXase, and competitive binding assay indicated that dHG-5 and oHG-8 could bind to FIXa. Nevertheless, dHG-5 and oHG-8 had no effects on FXII and platelet activation. nHG, dHG-5, and oHG-8 could significantly prolong the activated partial thromboplastin time of human, rat, and rabbit plasma. In the rat deep venous thrombosis model, dHG-5 and oHG-8 showed potent antithrombotic effects in a dose-dependent manner, while the thrombus inhibition rate of nHG at high dose was markedly reduced. Additionally, dHG-5 and oHG-8 did not increase bleeding at the doses up to 10-fold of the effectively antithrombotic doses compared with nHG and low molecular weight heparin in the mice tail-cut model. Considering that dHG-5 possesses strong anti-iXase and antithrombotic activities, and its preparation process is simpler and its yield is higher compared with oHG-8, it might be a promising antithrombotic candidate.
Lutan Zhou, Na Gao, Huifang Sun, Chuang Xiao, Lian Yang, Lisha Lin, Ronghua Yin, Zi Li, Hongbin Zhang, Xu Ji, Jinhua Zhao

2210 related Products with: Effects of Native Fucosylated Glycosaminoglycan, Its Depolymerized Derivatives on Intrinsic Factor Xase, Coagulation, Thrombosis, and Hemorrhagic Risk.

20 IU1. KU60 IU40 IU2 100 1mgOne 96-Well Strip Micropl100.00 ug10 0.5mg1000IU

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#31481052   2019/09/03 To Up

In vivo assessment of anticoagulant and antiplatelet effects of Syzygium cumini leaves extract in rabbits.

Syzygium cumini (L.) Skeels. is one of the very popular traditionally used medicinal plants with numerous pharmacological activities including antioxidant, hypoglycemic and anti-inflammatory. However, actions of S. cumini on blood coagulation and other parameters of blood were poorly pharmacologically studied. Therefore, aim of this present investigation is to examine the effects of methanolic extract of S. cumini on blood coagulation and anticoagulation factors in healthy white albino rabbits at different doses.
Ahad Abdul Rehman, Azra Riaz, Muhammad Arif Asghar, Muhammad Liaquat Raza, Shadab Ahmed, Kamran Khan

2380 related Products with: In vivo assessment of anticoagulant and antiplatelet effects of Syzygium cumini leaves extract in rabbits.

1 mg1 mg48 samples400 ug400 ug96 tests100 1 g5mg

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#31394258   2019/08/05 To Up

A systems pharmacokinetic/pharmacodynamic model for concizumab to explore the potential of anti-TFPI recycling antibodies.

Concizumab is a humanized monoclonal antibody in clinical investigation directed against membrane-bound and soluble tissue factor pathway inhibitor (mTFPI and sTFPI) for treatment of hemophilia. Concizumab displays a non-linear pharmacokinetic (PK) profile due to mTFPI-mediated endocytosis and necessitates a high dose and frequent dosing to suppress the abundant sTFPI, a negative regulator of coagulation. Recycling antibodies that can dissociate bound mTFPI/sTFPI in endosomes for degradation and rescue antibody from degradation have a potential in reducing the dose by extending antibody systemic persistence and sTFPI suppression. We developed a systems PK/pharmacodynamics (PD) model with nested endosome compartments to simulate the effect of decreased antibody binding to mTFPI/sTFPI in endosomes on antibody clearance and sTFPI suppression for exploring the potential of anti-TFPI recycling antibodies in reducing the dose. A dynamic model-building strategy was taken. A reduced PK/PD model without the endosome compartments was developed to optimize unknown target turnover parameters using concizumab PK data. The optimized parameters were then employed in the systems PK/PD model for simulations. The obtained systems PK/PD model adequately described the PK of concizumab in rabbits, monkeys, and humans and the PD in humans. The systems PK/PD model predicted that an anti-TFPI recycling antibody with a 100-fold higher mTFPI/sTFPI dissociation constant in endosomes than concizumab can extend sTFPI suppression from 12 days to 1 month. Thus, the systems PK/PD model provides a quantitative platform for guiding the engineering and translational development of anti-TFPI recycling antibodies.
Dongfen Yuan, Frederik Rode, Yanguang Cao

2462 related Products with: A systems pharmacokinetic/pharmacodynamic model for concizumab to explore the potential of anti-TFPI recycling antibodies.

1 mg1 mL0.1 mg0.1 mg0.1 mg50 100 μg1 mg0.5 ml1 mL0.2 mg

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#31382076   2019/08/02 To Up

Evaluation of a Novel Collagen Hemostatic Matrix: Comparison of Two Hemostatic Matrices in a Rabbits Jejunal Artery Injury Model.

We evaluated the hemostatic efficacy and immunogenicity of CollaStat compared with FloSeal in a rabbit jejunal artery injury model.
Min Jhi Kim, Jung-Han Kim, Jee Soo Kim, Jun-Ho Choe

2066 related Products with: Evaluation of a Novel Collagen Hemostatic Matrix: Comparison of Two Hemostatic Matrices in a Rabbits Jejunal Artery Injury Model.

24 tests0.2 mg100 μg18 kgs1 ml1.00 flask100 μg1 ml1.00 flask96 samples200 24 tests

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#30376878   2018/10/30 To Up

Anti-thrombotic effect of a factor Xa inhibitor TAK-442 in a rabbit model of arteriovenous shunt thrombosis stimulated with tissue factor.

Arterial thrombosis is triggered by tissue factor, which is a transmembrane glycoprotein can be released into the blood circulation after plaque rupture. Animal models with reflecting ruptured plaque lesions will be useful to understand efficacy of anticoagulant. In this study, we sought to improve a common arteriovenous shunt model in rabbits, aiming for a model of thrombosis stimulated with tissue factor, and to investigate the anti-thrombotic effect of a direct factor Xa inhibitor TAK-442 in the model.
Emiko Shinozawa, Masaki Kawamura

1610 related Products with: Anti-thrombotic effect of a factor Xa inhibitor TAK-442 in a rabbit model of arteriovenous shunt thrombosis stimulated with tissue factor.

100 μg20 100.00 ug100 100ul100ul20 100ug Lyophilized100ug100ug Lyophilized100ug100 μg

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#29914049   2018/06/15 To Up

Anticoagulant Activities of Indobufen, an Antiplatelet Drug.

Indobufen is a new generation of anti-platelet aggregation drug, but studies were not sufficient on its anticoagulant effects. In the present study, the anticoagulant activity of indobufen was determined by monitoring the activated partial thromboplastin time (APTT), prothrombin time (PT), and thrombin time (TT) in rabbit plasma. We evaluated the anticoagulant mechanisms on the content of the platelet factor 3,4 (PF3,4), and the coagulation factor 1, 2, 5, 8, 10 (FI, II, V, VIII, X) in rabbits, as well as the in vivo bleeding time and clotting time in mice. The pharmacodynamic differences between indobufen and warfarin sodium, rivaroxaban, and dabigatran were further studied on thrombus formation and the content of FII and FX in rats. Animal experiments showed that intragastric-administrated indobufen can significantly reduce the APTT, PT, TT, PF3, FI, II, V, VIII, and X plasma contents. Its inhibitory effect on plasma FII was better than thrombin inhibitor dabigatran with effect on FX better than FXa inhibitor rivaroxaban. These results suggest that indobufen has some anticoagulant effects as strong as some conventional anticoagulants. The mechanism may be related to both exogenous and endogenous coagulation system.
Jia Liu, Dan Xu, Nian Xia, Kai Hou, Shijie Chen, Yu Wang, Yunman Li

1381 related Products with: Anticoagulant Activities of Indobufen, an Antiplatelet Drug.

100ug Lyophilized100ug Lyophilized0.1 mg500ml100.00 ug100 ul100ug Lyophilized100ug Lyophilized100 µg1 Set0.1 mg200ul

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#29845491   // To Up

Inhibition of Tissue Factor Pathway Inhibitor (TFPI) as a Treatment for Haemophilia: Rationale with Focus on Concizumab.

Replacement therapy with missing factor (F) VIII or IX in haemophilia patients for bleed management and preventative treatment or prophylaxis is standard of care. Restoration of thrombin generation through novel mechanisms has become the focus of innovation to overcome limitations imposed by protein replacement therapy. Tissue factor pathway inhibitor (TFPI) is a multivalent Kunitz-type serine protease inhibitor that regulates tissue factor (TF)-induced coagulation through a FXa-dependent feedback inhibition of the TF.FVIIa complex in plasma and on endothelial surfaces. Concizumab is a monoclonal, humanised antibody, specific for the second Kunitz domain of TFPI that binds and inhibits FXa, abolishing the inhibitory effect of TFPI. Concizumab restored thrombin generation in FVIII and FIX deficient plasmas and decreased blood loss in a rabbit haemophilia model. Phase 1 single and multiple dose escalation studies in haemophilia patients demonstrated a dose dependent decrease in TFPI levels and a pro-coagulant effect with increasing d-dimers and prothrombin fragment 1 + 2. A dose dependent increase in peak thrombin and endogenous thrombin potential was observed with values in the normal range when plasma TFPI levels were nearly undetectable. A few haemophilia patients in the highest dose cohorts with complete inhibition of plasma TFPI showed a decreased fibrinogen concentration with normal levels of anti-thrombin and platelets and no evidence of thrombosis. Pharmacokinetic parameters were influenced by binding to the target (TFPI), demonstrating target mediated drug disposition. A trend towards decreasing bleeding tendency was observed and this preventative effect is being studied in Phase 2 studies with additional data gathered to improve our understanding of the therapeutic window and potential for thrombosis.
Pratima Chowdary

2362 related Products with: Inhibition of Tissue Factor Pathway Inhibitor (TFPI) as a Treatment for Haemophilia: Rationale with Focus on Concizumab.

100 μg50 assays1,000 tests100 assays96 assays 100 assays

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#29793324   2017/12/01 To Up

Evaluation of the antithrombotic activity of Zhi-Xiong Capsules, a Traditional Chinese Medicinal formula, via the pathway of anti-coagulation, anti-platelet activation and anti-fibrinolysis.

Zhi-Xiong Capsules (ZXC) involving Hirudo, Ligusticum chuanxiong, Salvia miltiorrhiza, Leonurus artemisia, and Pueraria lobata, is an empirical prescription used in Chinese clinics applied for treating cerebral arteriosclerosis and blood-stasis in clinic. However, the mechanism of its antithrombotic activity has not been investigated until now. The present study was designed to investigate its antithrombotic effects, the mechanism of ZXC on anti-thrombus action and to identify the main chemical composition of ZXC using HPLC-DAD-ESI-IT-TOF-MS. Two animal models were used to evaluate the antithrombotic effect of ZXC, the arterial thrombosis model and a venous thrombosis model. ZXC prolonged the plasma recalcification time (PRT), the activated partial thromboplastin time (APTT), the thrombin time (TT) and the prothrombin time (PT) and clearly reduced the content of fibrinogen (FIB) obviously in the arterial thrombosis model. Furthermore, it markedly suppressed the level of TXB and up-regulated the level of 6-keto-PGF. In addition, it significantly up-regulated the level of t-PA and down-regulated the level of PAI-1 (p < 0.05). These results revealed that ZXC played a vital role in the prevention of thrombosis through interacting with multiple targets, including inhibition of coagulation and platelet aggregation and increasing thrombolysis. A total of 23 compounds were identified as the main components of ZXC by HPLC-DAD-ESI-IT TOF-MS.
Jingjing Zhou, Zehai Song, Mingshu Han, Baoxing Yu, Guanghui Lv, Na Han, Zhihui Liu, Jun Yin

2793 related Products with: Evaluation of the antithrombotic activity of Zhi-Xiong Capsules, a Traditional Chinese Medicinal formula, via the pathway of anti-coagulation, anti-platelet activation and anti-fibrinolysis.

100.00 ul1 ml100.00 ul100.00 ul1 ml0.1 mg

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