Biological Information

Background Information:

Human factor VIIa is a vitamin K-dependent plasma serine protease generated by proteolysis of zymogen FVII. FVIIa binds with high affinity to tissue factor forming the tissue factor/Factor VIIa complex. This complex with factor VIIa as the catalytic subunit initiates the extrinsic coagulation pathway by activation of factor X, factor IX and additional factor VII.

Family:

Protease

Sub Family:

Chymotrypsin

Class:

Serine Peptidase

Protein Name:

Factor VIIa

Uniprot Number:

P08709

Protein Aliases:

Proconvertin; Serum prothrombin conversion accelerator (SPCA)

Gene Name:

F7

Gene ID:

2155

Gene Aliases:

eptacog alfa; FVII coagulation protein; factor VII

Accession Number:

NM_000131

Organism:

Human

Construct Details:

Endogenous

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrofluorimetry

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Human plasma coagulation factor VIIa is used. Test compound and/or vehicle is preincubated with 3 μg/mL enzyme in modified 50 mM Tris-HCl buffer pH 7.6 for 15 minutes at 25˚C. The reaction is initiated by addition of 100 μM Boc-LTR-AMC for another 60-minute incubation period. Determination of the amount of AMC formed is read spectrofluorometrically at excitation 360 nm and emission 465 nm. Compounds are screened at 10 μM.

Substrate:

100 μM Boc-LTR-AMC

Incubation:

60 min at 25°C

Control Inhibitor:

PCI-27483

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 μM

Test Sample Requirements:

Minimum for 1) Screen: 25 μL of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μL of 10 mM stock -OR- 1 mg (pre-weighed).

Minimum Order Quantity:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

5311176

Name

PPACK

Measurement

1.1μM - IC50

PubChem ID

135425273

Name

PCI-27483

Measurement

0.032μM - IC50

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei