TBC-11249
Sitaxsentan sodium
CAS: 210421-74-2
Molecular Formula: C18H14ClN2NaO6S2
TBC-11249 - Names and Identifiers
| Name | Sitaxsentan sodium |
| Synonyms | CS-338 Thelin TBC-11249 TBC-11251 sodium sitaxentan sodiuM SITAXSENTAN SODIUM Sitaxsentan sodium 4-Chloro-3-methyl-5-[2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]-3-thienylsulfonamido]isoxazole sodium salt Sodium (4-chloro-3-methyl-1,2-oxazol-5-yl)-[2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophen-3-yl]sulfonylazanide |
| CAS | 210421-74-2 |
| InChI | InChI=1/C18H14ClN2O6S2.Na/c1-9-5-13-14(26-8-25-13)7-11(9)6-12(22)17-15(3-4-28-17)29(23,24)21-18-16(19)10(2)20-27-18;/h3-5,7H,6,8H2,1-2H3;/q-1;+1/rC18H14ClN2NaO6S2/c1-9-5-13-14(27-8-26-13)7-11(9)6-12(23)17-15(3-4-29-17)30(24,25)21(22)18-16(19)10(2)20-28-18/h3-5,7H,6,8H2,1-2H3 |
TBC-11249 - Physico-chemical Properties
| Molecular Formula | C18H14ClN2NaO6S2 |
| Molar Mass | 476.89 |
| Solubility | H2O: soluble10mg/mL (clear solution) |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | room temp |
| Use | Sitaxentan sodium salt |
| In vitro study | Sitaxentan sodium inhibits ET-1-induced stimulation of phosphoinositide turnover with a Ki of 0.69 nM and a pA2 of 8.0. |
| In vivo study | Sitaxentan sodium has a serum half-life in the rat and the dog of 6 hours - 7 hours and 60−100% oral bioavailability. Orally administered Sitaxentan sodium is rapidly absorbed in both the rat and the dog with a t1/2(abs) of 0.7 hours and 0.3 hours, respectively. Peak plasma concentrations occurred between 2 hours and 3 hours postdosing in the rat and between 45 minutes and 90 minutes in the dog. The pulmonary vasoconstrictor response to acute hypoxia (10% O2 for 90 minutes) is prevented with Sitaxentan sodium (5 mg/kg infused i.v. 10 minutes prior to the onset of hypoxia). Sitaxentan sodium delivered i.v. 50 minutes after the onset of hypoxia reverses the established pulmonary vasoconstriction. Sitaxsentan blocks increased plasma endothelin levels. Sitaxsentan dose dependently (10 mg/kg and 50 mg/kg per day in the drinking water) attenuates right ventricular systolic pressure, right heart hypertrophy, and pulmonary vascular remodeling observed 3 weeks after a single subcutaneous injection of monocrotaline. Systemic administration of the ETA receptor antagonist Sitaxentan sodium significantly attenuates cerebral vasospasm after subarachnoid hemorrhage (SAH). Sitaxentan sodium reduces the development of hypoxic pulmonary vasoconstriction (HPV) in the pig. In addition, bolus injection of Sitaxentan sodium reverses already established HPV. |
TBC-11249 - Risk and Safety
| WGK Germany | 3 |
| RTECS | XN0296600 |
TBC-11249 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.097 ml | 10.485 ml | 20.969 ml |
| 5 mM | 0.419 ml | 2.097 ml | 4.194 ml |
| 10 mM | 0.21 ml | 1.048 ml | 2.097 ml |
| 5 mM | 0.042 ml | 0.21 ml | 0.419 ml |
Last Update：2024-01-02 23:10:35
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View History
TBC-11249
(1,10-菲啰啉)双(三苯基磷)硝酸铜 二氯甲烷络合物
Dimethylcyclohexylethoxy isobutylpropanoate
2-Hydroxyethylthiomethylbenzene
3-(N,N-Dimethylaminomethyl)-5-methyl-2-hexanone oxalate
8-甲氧基-2-(三氟甲基)喹啉-5-羧酸
(6-ETHYL-4-OXO-3-PHENYL-3,4-DIHYDRO-THIENO[2,3-D]PYRIMIDIN-2-YLSULFANYL)-ACETIC ACID
(S)-1-Boc-2-isopropyl-piperazine (HCL)
4-AMINO-7-CHLORO-2-METHYLQUINOLINE
Cyclopenta(C,D)Pyrene
(1,10-菲啰啉)双(三苯基磷)硝酸铜 二氯甲烷络合物
Dimethylcyclohexylethoxy isobutylpropanoate
2-Hydroxyethylthiomethylbenzene
3-(N,N-Dimethylaminomethyl)-5-methyl-2-hexanone oxalate
8-甲氧基-2-(三氟甲基)喹啉-5-羧酸
(6-ETHYL-4-OXO-3-PHENYL-3,4-DIHYDRO-THIENO[2,3-D]PYRIMIDIN-2-YLSULFANYL)-ACETIC ACID
(S)-1-Boc-2-isopropyl-piperazine (HCL)
4-AMINO-7-CHLORO-2-METHYLQUINOLINE
Cyclopenta(C,D)Pyrene