Terbogrel
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.
- CAS No.: 149979-74-8
- Formula: C23H27N5O2
- Molecular Weight:405.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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TXA2/TP |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 149979-74-8
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Molecular Weight 405.49
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Formula C23H27N5O2
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SMILES
O=C(O)CCC/C=C(C1=CC=CC(/N=C(NC#N)/NC(C)(C)C)=C1)/C2=CC=CN=C2
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Synonyms
BIBV 308SE
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Muck S, et al. Effects of terbogrel on platelet function and prostaglandin endoperoxide transfer. Eur J Pharmacol. 1998 Feb 26;344(1):45-8. [Content Brief]
[2]. Soyka R, et al. Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors. J Med Chem. 1999 Apr 8;42(7):1235-49. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)