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| Targets |
Factor Xa (FXa), a key serine protease in the coagulation cascade that converts prothrombin to thrombin. The substrate is not a drug but a tool compound that is specifically designed to be cleaved by FXa at the Arg-pNA bond, enabling measurement of FXa enzymatic activity.
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| ln Vitro |
Suc-Ile-Glu(gamma-pip)-Gly-Arg-pNA is a specific chromogenic substrate for FXa. The enzyme preferentially binds to and cleaves the Ile-Glu(gamma-pip)-Gly-Arg (IE(gamma-pip)GR) peptide sequence, releasing the p-nitroaniline (pNA) reporter group. The cleavage product pNA is quantified by colorimetric detection at 405 nm, and the rate of pNA release is directly proportional to FXa activity.
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| ln Vivo |
The substrate has no direct biological activity or pharmacodynamics in vivo. It is an exogenous tool compound used solely for in vitro diagnostic and research applications. While it does not exert systemic effects, its use in ex vivo assays can help measure FXa activity in plasma samples from preclinical or clinical studies investigating coagulopathies and anticoagulant drugs.
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| Enzyme Assay |
Typically, recombinant human Factor Xa is activated and diluted in a reaction buffer (e.g., 50 mM Tris-HCl, pH 7.4, 150 mM NaCl, 5 mM CaCl2) in a 96-well plate. The test compound (Suc-Ile-Glu(gamma-pip)-Gly-Arg-pNA hydrochloride) is added at varying concentrations. The reaction is initiated, and the release of pNA is measured kinetically at 405 nm for 5-30 minutes using a microplate reader. The Vmax is calculated to determine FXa activity or inhibitor potency.
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| Cell Assay |
This substrate is not typically used in live cell-based assays due to its inability to cross cell membranes. Instead, it is used in cell lysate assays. Cells are lysed, and the protein concentration of the lysate is normalized. The lysate is incubated with the FXa substrate in a suitable buffer. The release of pNA is measured at 405 nm, providing a measure of FXa-like activity in the cellular environment and allowing for the screening of cell-permeable FXa inhibitors.
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| Animal Protocol |
For ex vivo pharmacodynamics studies, plasma is collected from animals that have been treated with a potential anticoagulant. Citrated platelet-poor plasma (PPP) is mixed with the FXa substrate in a buffer containing calcium. The rate of pNA release is measured at 405 nm. A decrease in the rate compared to a vehicle control indicates successful inhibition of FXa activity by the tested compound in vivo.
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| ADME/Pharmacokinetics |
The compound is a synthetic peptide with a molecular weight of 797.3 g/mol and a molecular formula of C34H53ClN10O10. It has solubility in DMSO (3 mg/mL) and PBS (pH 7.2, 3 mg/mL). It is a stable solid and should be stored at -20degC, protected from light and moisture. As a reagent, it does not have a traditional PK profile because it is not administered systemically.
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| Toxicity/Toxicokinetics |
In standard research applications, Suc-Ile-Glu(gamma-pip)-Gly-Arg-pNA hydrochloride is used at non-toxic concentrations (typically 10-200 uM). It is not intended for human or veterinary use. Toxicological data are limited to standard laboratory safety precautions; it may cause eye, skin, or respiratory tract irritation upon direct contact. It is not considered an acutely hazardous substance at the concentrations used in typical assays.
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| References | |
| Additional Infomation |
This compound is a standard research grade chemical only and is not an FDA-approved drug. It has not entered clinical trials. Its primary value is in drug discovery as a reagent to monitor FXa activity in in vitro assays, aiding in the development of anticoagulants for thrombotic disorders such as acute coronary syndrome (ACS) and atrial fibrillation.
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| Molecular Formula |
C34H53CLN10O10
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|---|---|
| Molecular Weight |
797.30
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| Exact Mass |
796.363
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| CAS # |
1379822-04-4
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| PubChem CID |
156588991
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
21
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| Heavy Atom Count |
55
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| Complexity |
1340
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CCC(=O)N1CCCCC1)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)NC2=CC=C(C=C2)[N+](=O)[O-])NC(=O)CCC(=O)O.Cl
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| InChi Key |
UDIBETPIWZURPW-FTHVRPHQSA-N
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| InChi Code |
InChI=1S/C34H52N10O10.ClH/c1-3-21(2)30(42-26(45)14-16-29(48)49)33(52)41-25(13-15-28(47)43-18-5-4-6-19-43)31(50)38-20-27(46)40-24(8-7-17-37-34(35)36)32(51)39-22-9-11-23(12-10-22)44(53)54;/h9-12,21,24-25,30H,3-8,13-20H2,1-2H3,(H,38,50)(H,39,51)(H,40,46)(H,41,52)(H,42,45)(H,48,49)(H4,35,36,37);1H/t21-,24-,25-,30-;/m0./s1
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| Chemical Name |
4-[[(2S,3S)-1-[[(2S)-1-[[2-[[(2S)-5-(diaminomethylideneamino)-1-(4-nitroanilino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1,5-dioxo-5-piperidin-1-ylpentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acid;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| 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 | 1.2542 mL | 6.2712 mL | 12.5423 mL | |
| 5 mM | 0.2508 mL | 1.2542 mL | 2.5085 mL | |
| 10 mM | 0.1254 mL | 0.6271 mL | 1.2542 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.
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