Thromboxane Synthase (CYP5A1) Human CYP450 Enzymatic LeadHunter Assay - TW

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Thromboxane A2 (TxA2) is a potent platelet activator which serves to amplify the response to weak agonists such as ADP, epinephrine, and low concentrations of collagen and thrombin. Upon cell activation, phospholipase released arachidonic acid is converted by cyclooxygenase to unstable endoperoxides (PGG2 or PGH2) which are in turn converted to TxA2 by thromboxane synthase. The endoperoxides and TxA2 generated by aggregating platelets could produce a profound vasoconstriction largely restricted to the area of the vessel immediately adjacent to the platelet plug; e.g., vasospasm associated with coronary or cerebral infarction. An enhanced production of TxA2 is associated with the pathogenesis of various thrombotic and ischemic disorders.

Family:

CYP450

Sub Family:

CYP5/7/8

Protein Name:

Thromboxane Synthase

Uniprot Number:

P24557

Protein Aliases:

cytochrome P450, family 5, subfamily A, polypeptide 1

Gene Name:

TBXAS1

Gene ID:

6916

Gene Aliases:

CYP5|CYP5A1|THAS|TXS|TXAS|TS

Accession Number:

NM_001061

Organism:

Human

Construct Details:

Endogenous

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

EIA

Measured Response:

Absorbance

Testing Information

Procedure Summary:

Human platelet thromboxane A2 synthase is used. Test compound and/or vehicle is preincubated with 20 μg/ml enzyme‡ in Tris-HCl buffer pH 7.4 for 15 minutes at 25⁰C. The reaction is initiated by addition of 10 μM prostaglandin H2 for another 3 minute incubation period and terminated by further addition of 1N HCl. An aliquot is removed and determine the amount of thromboxane B2 formed spectrophotometrically by EIA kit. Compounds are screened at 10 μM.

Substrate:

10 µM PGH₂

Incubation:

3 min at 25°C

Control Inhibitor:

1-(7-Carboxyheptyl)-Imidazole

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

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:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

53001

Name

DAZOXIBEN

Measurement

0.0056μM - IC50

PubChem ID

Name

1-(7-Carboxyheptyl)-Imidazole

Measurement

0.01μM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

Inhibitors of TxA2 biosynthesis may be of benefit in the treatment of ischemic heart diseases, cerebral infarction, arteriosclerosis and diabetic disorders.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei