149979-74-8
149979-74-8 structure
- Name: Terbogrel
- Chemical Name: (E)-6-[3-[(N'-tert-butyl-N-cyanocarbamimidoyl)amino]phenyl]-6-pyridin-3-ylhex-5-enoic acid
- CAS Number: 149979-74-8
- Molecular Formula: C23H27N5O2
- Molecular Weight: 405.49300
- Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
- Create Date: 2018-06-21 10:13:32
- Modify Date: 2024-01-09 20:56:24
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Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.
| Name | (E)-6-[3-[(N'-tert-butyl-N-cyanocarbamimidoyl)amino]phenyl]-6-pyridin-3-ylhex-5-enoic acid |
|---|---|
| Synonyms |
Terbogrel
Terbogrel (USAN/INN) BIBV 308 BIBV-308-SE |
| Description | Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM. |
|---|---|
| Related Catalog | |
| 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]. |
| 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]. |
| References |
| Density | 1.13g/cm3 |
|---|---|
| Boiling Point | 601.3ºC at 760mmHg |
| Molecular Formula | C23H27N5O2 |
| Molecular Weight | 405.49300 |
| Flash Point | 317.4ºC |
| Exact Mass | 405.21600 |
| PSA | 110.40000 |
| LogP | 4.86918 |
| Vapour Pressure | 2.63E-15mmHg at 25°C |
| Index of Refraction | 1.579 |
| Storage condition | 2-8℃ |