1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. Terbogrel

Terbogrel (Synonyms: BIBV 308SE)

Cat. No.: HY-19189
Handling Instructions

Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.

For research use only. We do not sell to patients.

Terbogrel Chemical Structure

Terbogrel Chemical Structure

CAS No. : 149979-74-8

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Description

Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.

IC50 & Target

IC50: apr 10 nM (thromboxane A2 receptor), appr 10 nM (thromboxane A2 synthase)[1]

In Vitro

Pretreatment of platelets with terbogrel 1 μM completely inhibits thrombin-induced thromboxane A2 formation (2±1 ng/mL) but does not result in any inhibition of platelet aggregation. Terbogrel (1 μM) completely inhibits U46619-induced platelet aggregation, and the IC50 value is 10 nM. Terbogrel inhibits both platelet aggregation and thromboxane A2 formation with an IC50 of about 10 nM[1]. Terbogrel inhibits the thromboxane A2 synthase in human gel-filtered platelets with an IC50 value of 4.0 ± 0.5 nM. Terbogrel blocks the thromboxane A2/endoperoxide receptor on washed human platelets with an IC50 of 11 ± 6 nM (n = 2) and with an IC50 of 38 ± 1 nM (n = 15) in platelet-rich plasma. Terbogrel inhibits the collagen-induced platelet aggregation in human platelet-rich plasma and whole blood with an IC50 of 310 ± 18 nM (n = 8) and 52 ± 20 nM (n = 6), respectively[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Terbogrel (0.1−3.0 mg/kg) demonstrates an impressive antithrombotic efficacy in rabbits. Terbogrel (10 mg/kg, po) is rapidly and well (90%) absorbed with a systemic availability of about 30% in rats[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

405.49

Formula

C₂₃H₂₇N₅O₂

CAS No.

149979-74-8

SMILES

O=C(O)CCC/C=C(C1=CC=CC(/N=C(NC#N)/NC(C)(C)C)=C1)/C2=CC=CN=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

TerbogrelBIBV 308SEProstaglandin ReceptorInhibitorinhibitorinhibit

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Terbogrel
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HY-19189
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