Bosentan Hydrate (Ro 47-0203)

Alias: Ro-47-0203; Tracleer; Ro 47-0203; Ro47-0203; bosentan monohydrate; Ro47 0203; Ro-47 0203
Cat No.:V1509 Purity: ≥98%
Bosentan Hydrate (also known as Ro 47-0203; Ro47-0203; Ro-47-0203; Tracleer) is a potent, competitive and dual endothelin (ET) A/B receptor antagonist for ET-A and ET-B with anti-hypertensive activity.
Bosentan Hydrate (Ro 47-0203) Chemical Structure CAS No.: 157212-55-0
Product category: Endothelin Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
100mg
250mg
500mg
1g
5g
Other Sizes

Other Forms of Bosentan Hydrate (Ro 47-0203):

  • Bosentan
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Bosentan Hydrate (also known as Ro 47-0203; Ro47-0203; Ro-47-0203; Tracleer) is a potent, competitive and dual endothelin (ET) A/B receptor antagonist for ET-A and ET-B with anti-hypertensive activity. It inhibits ET-A and ET-B with Ki values of 4.7 nM and 95 nM, respectively. Bosentan is an authorized drug used as a vasodilator to treat pulmonary arterial hypertension. Bosentan is an ETBR and ETAR inhibitor. It is applied to the management of PAH, or pulmonary arterial hypertension. Bosentan prevents endothelin molecules from acting, which would otherwise encourage blood vessel narrowing and raise blood pressure.

Biological Activity I Assay Protocols (From Reference)
Targets
ET-A ( Ki = 4.7 nM ); ET-B ( Ki = 95 nM )
ln Vitro

In vitro activity: Bosentan competitively impedes the particular binding of [125 I]-labeled ET-1 on human placenta (ET-B receptors) and smooth muscle cells (ET-A receptors). On the trachea of pigs, bosentan also prevents specific ET-B ligands from binding. The selective ET-B agonist sarafotoxin S6C in the rat trachea and ET-1 in isolated rat aorta (ET-A) both induce contractions that are competitively inhibited by bosentan (pA2= 7.2 and 6.0, respectively), as is the endothelium-dependent relaxation to sarafotoxin S6C in the rabbit superior mesenteric artery (pA2= 6.7). Bosentan's specificity for ET receptors is demonstrated by the fact that it has no discernible effect on the binding of 40 other peptides, prostaglandins, ions, or neurotransmitters.[1]

ln Vivo
Bosentan has no intrinsic agonist activity and a long half-life of action, inhibiting the presser response to big ET-1 both intravenously and orally. Additionally, bosentan blocks the presser and depressor effects of sarafotoxin S6C and ET-1. Bosentan has a pharmacological profile that makes it a potentially helpful medication for the treatment of clinical conditions linked to vasoconstriction.[1] The first oral non-peptide mixed ETA/B-receptor antagonist is called bosentan. Rats with CHF who have received long-term Bosentan treatment have significantly improved in terms of survival, hemodynamics, and cardiac remodeling. The degree to which bosentan lowers arterial blood pressure is comparable to that of an ACE inhibitor. When bosentan is administered to rats with CHF following an acute MI, it significantly lowers arterial blood pressure and has an additive effect with ACE inhibitors. In patients with congestive heart failure (CHF), both acute and long-term use of bosentan reduces peripheral and pulmonary vascular resistance while increasing cardiac output.[2]
Cell Assay
The trypan blue exclusion test is used to determine the viability of cells. Bosentan is applied to human dermal fibroblasts at the recommended concentrations (10, 20 and 40 μM). Viability of the cells is assessed after 24 and 48 hours. Using a hematocytometer, the number of stained (dead) and unstained (viable) cells is determined.
Animal Protocol
Rats: Rats that are two months old—DSS and Wistar—are employed. Doses ranging from 0.1 to 100 mg/kg (Macitentan) or 3 to 600 mg/kg (Bosentan) are used to measure the pharmacological effects on heart rate (HR), mean arterial pressure (MAP), or mean pulmonary arterial pressure (MPAP), and up to 120 hours after a single gavage. 1) Macitentan is given on top of the maximum effective dose of Bosentan determined by the dose-response curve in order to assess whether Macitentan can offer greater pharmacological activity compared to Bosentan. Secondly, the maximum effective dose of Macitentan is topped off with the same dose of Bosentan. Tmax of the first tested compound is the point at which the second compound's maximal effective dose is given.
References

[1]. Pathophysiology . 2003 Sep;9(4):249-256.

[2]. J Pharmacol Exp Ther . 1994 Jul;270(1):228-35.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H31N5O7S
Molecular Weight
569.63
Exact Mass
569.19
CAS #
157212-55-0
Appearance
Powder
SMILES
CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=C(C(=NC(=N2)C3=NC=CC=N3)OCCO)OC4=CC=CC=C4OC.O
InChi Key
SXTRWVVIEPWAKM-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H29N5O6S.H2O/c1-27(2,3)18-10-12-19(13-11-18)39(34,35)32-23-22(38-21-9-6-5-8-20(21)36-4)26(37-17-16-33)31-25(30-23)24-28-14-7-15-29-24;/h5-15,33H,16-17H2,1-4H3,(H,30,31,32);1H2
Chemical Name
4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]benzenesulfonamide;hydrate
Synonyms
Ro-47-0203; Tracleer; Ro 47-0203; Ro47-0203; bosentan monohydrate; Ro47 0203; Ro-47 0203
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~100 mg/mL (~175.6 mM)
Water: <1 mg/mL
Ethanol: 2~50 mg/mL (3.5~87.8 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7555 mL 8.7776 mL 17.5553 mL
5 mM 0.3511 mL 1.7555 mL 3.5111 mL
10 mM 0.1756 mL 0.8778 mL 1.7555 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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