Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6264 |
Bosentan
Actelion,波生坦,Ro 47-0203,Benzenesulfonamide |
Endothelin Receptor | GPCR/G Protein |
Bosentan (Benzenesulfonamide) 是 endothelin-1 (ET)拮抗剂,在人的 SMC 细胞中,它能够作用于 ETA 受体(Ki:4.7 nM)和 ETB 受体(Ki:95 nM)。 | |||
T6265 |
Bosentan (hydrate)
波生坦水合物,Bosentan Hydrate,Benzenesulfonamide,Actelion,Ro 47-0203 |
Endothelin Receptor | GPCR/G Protein |
Bosentan hydrate (Ro 47-0203) 是endothelin-1 (ET)竞争性拮抗剂,在人SMC 细胞中,它能够作用于 ETA 受体(Ki:4.7 nM)和 ETB 受体(Ki:95 nM)。 | |||
T37351 |
Desmethyl Bosentan
|
||
Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan .1Desmethyl bosentan (25 μM) activates the pregnane X receptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in a reporter assay. 1.van Giersbergen, P.L.M., Gnerre, C., Treiber, A., et al.Bosentan, a dual endothelin receptor antagonist, activates the pregnane X nuclear receptorBr. J. Clin. Pharmacol.54(5)561-562(2002) | |||
T19360 |
Hydroxy bosentan
Ro 48-5033 |
Others | Others |
Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Hydroxy bosentan assists BOS pharmacologically, retaining 10%-20% activities. | |||
T11584 |
Hydroxy desmethyl Bosentan
Ro 64-1056 |
Others | Others |
Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver. | |||
T73820 |
Bosentan-d4
|
||
Bosentan-d4 是 Bosentan 的氘代物。Bosentan 是一种有效的endothelin-1 (ET)拮抗剂,在人的 SMC 细胞中,作用于ETA 和ETB 受体,Ki 值分别为 4.7 nM 和 95 nM。 | |||
T36008 |
Nebentan potassium
|
||
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan potassium inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. Nebentan potassium inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB re... | |||
T36007 |
Nebentan
|
||
Nebentan (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. Nebentan inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB receptors in a concentration dep... |