Size | Price | |
---|---|---|
50mg | ||
100mg | ||
250mg |
Heparin is an anticoagulant agent and a highly sulfated polysaccharide/glycosaminoglycan. It has the highest negative charge density of any known biological molecules. Heparin significantly inhibits exosome-cell interactions. As an anticoagulant, it can interact with diverse proteins for numerous important biological activities.
ln Vitro |
Because it quickens the pace at which antithrombin inhibits serine proteases in the coagulation cascade, heparin is a very effective anticoagulant medication. Complex linear polymers, heparin and its structurally related counterpart heparan sulfate, are made up of a combination of chains of varying lengths and sequences. Peptides having complementary binding sites with a high positive charge density have the closest interactions with heparin. The secondary structures of heparin and heparan sulfate are primarily linear helical, with carboxyl and sulfo groups appearing along the polysaccharide backbone at specific intervals and directions. Heparin and DNA are both highly charged linear polymers that have polyelectrolyte properties. Heparin's main mechanism of anticoagulant action is thought to be through its interaction with AT III, which amplifies AT-III-mediated inhibition of coagulation factors such as factor Xa and thrombin. The bimolecular rate constant for thrombin inhibition is increased by 2000 times when heparin, AT III, and thrombin form a ternary complex. Tissue mast cell granules, which are intimately linked to immunological responses, are the primary location of heparin. Heparin stabilizes FGF-FGFR binding by forming wide interactions with FGFR-1 and FGF-2. Heparin appears to encourage FGFR dimerization since it also interacts with FGFR-1 of the nearby FGF-FGFR complex [1].
|
---|---|
References |
[1]. Capila I, et al. Heparin-protein interactions. Angew Chem Int Ed Engl. 2002 Feb 1;41(3):391-412.
[2]. Anurag Purushothaman, et al. Fibronectin on the Surface of Myeloma Cell-derived Exosomes Mediates Exosome-Cell Interactions. J Biol Chem. 2016 Jan 22;291(4):1652-63. |
Molecular Formula |
C26H42N2O37S5
|
---|---|
Molecular Weight |
1134.89
|
Exact Mass |
1134.007
|
CAS # |
9005-49-6
|
Related CAS # |
Heparin sodium salt;9041-08-1;Heparin Lithium salt;9045-22-1;Heparin sodium salt (MW 15kDa);9041-08-1
|
SMILES |
CC(NC1C(OC(C(C1O)OC2OC(C(O)=O)C(C(C2OS(=O)(O)=O)O)OC3OC(C(C(C3NS(=O)(O)=O)OS(=O)(O)=O)OC4OC(C(O)=O)C(C(C4OS(=O)(O)=O)O)O)CO)COS(=O)(O)=O)O)=O
|
InChi Key |
HTTJABKRGRZYRN-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C26H42N2O37S5/c1-4(30)27-7-9(31)13(6(56-23(7)39)3-55-67(43,44)45)58-26-19(65-70(52,53)54)12(34)16(20(62-26)22(37)38)60-24-8(28-66(40,41)42)15(63-68(46,47)48)14(5(2-29)57-24)59-25-18(64-69(49,50)51)11(33)10(32)17(61-25)21(35)36/h5-20,23-26,28-29,31-34,39H,2-3H2,1H3,(H,27,30)(H,35,36)(H,37,38)(H,40,41,42)(H,43,44,45)(H,46,47,48)(H,49,50,51)(H,52,53,54)
|
Chemical Name |
6-((5-acetamido-4,6-dihydroxy-2-((sulfooxy)methyl)tetrahydro-2H-pyran-3-yl)oxy)-3-((5-((6-carboxy-4,5-dihydroxy-3-(sulfooxy)tetrahydro-2H-pyran-2-yl)oxy)-6-(hydroxymethyl)-3-(sulfoamino)-4-(sulfooxy)tetrahydro-2H-pyran-2-yl)oxy)-4-hydroxy-5-(sulfooxy)tetrahydro-2H-pyran-2-carboxylic acid
|
Synonyms |
FraxiparinHeparin M-118Certoparin M118Dalteparin ThromboliquineEparinaParvoparinAdomiparin M 118Bemiparin Nadroparine
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
---|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.8811 mL | 4.4057 mL | 8.8114 mL | |
5 mM | 0.1762 mL | 0.8811 mL | 1.7623 mL | |
10 mM | 0.0881 mL | 0.4406 mL | 0.8811 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.