Thrombin

Base Information

• Chemical Name: Thrombin
• CAS No.: 9002-04-4
• Molecular Formula: NULL
• Molecular Weight: 0
• Hs Code.: 30021099

Synonyms:Blood-coagulationfactor II, activated; Blood-coagulation factor IIa; E.C. 3.4.21.5; E.C.3.4.4.13; Factor IIa; Thrombase; Thrombin JMI; Thrombin-C; Thrombinar;Thrombofort; Thrombostat; Topical; Tropostasin

Chemical Property of Thrombin

Chemical Property:

• Appearance/Colour: Powder
• Melting Point: 47.7 °C
• PSA: 0.00000
• LogP: 0.00000
• Storage Temp.: −20°C
• Solubility.: H2O: 1 mL/vial clear to slightly hazy, colorless solution

Purity/Quality:

99%min ^*data from raw suppliers

Thrombin ^*data from reagent suppliers

Safty Information:

• Hazard Codes: Xn,B,Xi
• Statements: 36/37/38-42
• Safety Statements: 22-24/25-36/37-26-24

MSDS Files:

SDS file from LookChem

Total 1 MSDS from other Authors

Useful:

• General Description: Thrombin is a serine protease critical for blood coagulation and a key therapeutic target for antithrombotic drugs. Recent research has focused on developing non-covalent thrombin inhibitors with improved oral bioavailability and pharmacokinetic profiles by incorporating P₃-heterocycles and P₁-bicyclic arginine surrogates. These inhibitors, designed to overcome the limitations of traditional anticoagulants, demonstrate high potency and selectivity, highlighting the importance of optimizing interactions between P₄-hydrophobes, P₃-heterocycles, and P₁-arginine mimics for effective thrombin inhibition.

Refernces

Non-covalent thrombin inhibitors featuring P₃-heterocycles with P₁-bicyclic arginine surrogates

10.1016/S0960-894X(02)00585-1

The research aimed to develop novel, potent, and orally bioavailable thrombin inhibitors to address the limitations of existing antithrombotic drugs like heparin and warfarin. Thrombin, a serine protease, plays a central role in blood clotting and is a key target for antithrombotic therapy. The study focused on designing and synthesizing a series of non-covalent inhibitors (NC1–NC44) featuring P1-bicyclic arginine mimics with weakly basic properties (calcd pKa 3.6–8.6) to improve oral bioavailability and pharmacokinetic profiles. These inhibitors incorporated various P4-aromatics and P3-heterocyclic dipeptide surrogates to enhance potency and selectivity. The researchers used a combination of P3-pyridones, pyridazinones, and diverse P1-heteroaromatic arginine surrogates such as indazoles, benzimidazoles, and benzotriazoles. The results showed that several of these inhibitors demonstrated high potency (Ki values ranging from 2.5 to 33 nM) and selectivity against thrombin, with some candidates (NC17–20 and NC24–31) exhibiting excellent pharmacokinetic properties in dogs. The study concluded that the balance between P4-hydrophobe, P3-heterocycle, and P1-arginine mimic is crucial for achieving high potency and efficacy.

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