Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure. IC50 value: Target: ETA receptor
| Molecular Weight | 454.9 |
| Formula | C18H15ClN2O6S2 |
| CAS Number | 184036-34-8 |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Iain M MacIntyre, et al. Drugs Today (Barc). Sitaxsentan sodium for pulmonary hypertension
[3] Eric T Wittbrodt, et al. Ann Pharmacother. Sitaxsentan for treatment of pulmonary hypertension
| Related Endothelin Receptor Products |
|---|
| Endothelin 1 (swine, human) (TFA)
Endothelin 1 (swine, human) (TFA) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. |
| Atrial Natriuretic Peptide (ANP) (1-28), rat
Atrial Natriuretic Peptide (ANP) (1-28), rat is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner. |
| [Asn18] Endothelin-1, human
[Asn18] Endothelin-1, human is a peptide. |
| [Lys4] Sarafotoxin S6c
[Lys4] Sarafotoxin S6c, a sarafotoxin analogue, is a potent and partial agonist of endothelin receptor. |
| [Ala2] Endothelin-3, human
[Ala2] Endothelin-3, human is a linear analog of endothelin-3 (ET-3) where substitution of Ala for Cys residues. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
