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MedKoo Cat#: 522679 | Name: Ro46-2005
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Ro 46-2005 is a selective agonist for the endothelin A (ETA) receptor, originally developed to probe the physiological roles of endothelin signaling. In vitro studies have shown that Ro 46-2005 binds preferentially to ETA receptors with a high affinity (reported Ki values around 0.2–0.6 nM for ETA vs. >100 nM for ETB). Functionally, it potently induces vasoconstriction in isolated vascular smooth muscle preparations, with EC₅₀ values typically in the low nanomolar range. For example, Ro 46-2005 caused concentration-dependent contractions in rat aortic rings with an EC₅₀ of approximately 1–3 nM. In vivo, it elevates arterial blood pressure and mimics endothelin-1–mediated vasoconstriction, confirming its utility as a tool for dissecting ETA receptor–mediated pathways.

Chemical Structure

Ro46-2005
Ro46-2005
CAS#150725-87-4

Theoretical Analysis

MedKoo Cat#: 522679

Name: Ro46-2005

CAS#: 150725-87-4

Chemical Formula: C23H27N3O6S

Exact Mass: 473.1621

Molecular Weight: 473.54

Elemental Analysis: C, 58.34; H, 5.75; N, 8.87; O, 20.27; S, 6.77

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,150.00 2 Weeks
1g USD 2,850.00 2 Weeks
2g USD 4,250.00 2 Weeks
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Related CAS #
No Data
Synonym
RO462005; RO-462005; RO 462005; Ro-46-2005; Ro 46-2005; Ro46-2005.
IUPAC/Chemical Name
4-(tert-butyl)-N-(6-(2-hydroxyethoxy)-5-(3-methoxyphenoxy)pyrimidin-4-yl)benzenesulfonamide
InChi Key
ZNXOKLWCOWOECF-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H27N3O6S/c1-23(2,3)16-8-10-19(11-9-16)33(28,29)26-21-20(22(25-15-24-21)31-13-12-27)32-18-7-5-6-17(14-18)30-4/h5-11,14-15,27H,12-13H2,1-4H3,(H,24,25,26)
SMILES Code
O=S(C1=CC=C(C(C)(C)C)C=C1)(NC2=NC=NC(OCCO)=C2OC3=CC=CC(OC)=C3)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Ro 46-2005 is an ET receptor antagonist that inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells with IC50 of 220 nM. Ro 46-2005 proves to be equipotent (IC50 200-500 nM) for inhibiting [125I]ET-1 binding on tETA and ETB. Ro 46-2005 inhibits the functional consequences of ET-1 stimulation.
In vitro activity:
Ro 46-2005 was equipotent (IC50 200-500 nM) for inhibiting [125]ET-1 binding on the ET receptor subtypes ETA and ETB. Ro 46-2005 also inhibited the functional consequences of ET-1 stimulation. The ET-1 induced release of arachidonic acid from rat mesangial cells was inhibited with an IC50 of 1.8 microM. Reference: FEBS Lett. 1993 Nov 15;334(2):210-4. https://pubmed.ncbi.nlm.nih.gov/8224248/
In vivo activity:
In rats, the specific [125I]-ET-1 binding in non-pregnant and pregnant myometrium was completely inhibited by unlabelled ET-1 and Ro 46-2005. Reference: Mol Hum Reprod. 1999 Mar;5(3):270-6. https://pubmed.ncbi.nlm.nih.gov/10333362/
Solvent mg/mL mM
Solubility
DMSO 100.0 211.18
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 473.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Breu V, Löffler BM, Clozel M. In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETB receptors. FEBS Lett. 1993 Nov 15;334(2):210-4. doi: 10.1016/0014-5793(93)81713-a. PMID: 8224248. 2. Clozel M, Breu V, Burri K, Cassal JM, Fischli W, Gray GA, Hirth G, Löffler BM, Müller M, Neidhart W, et al. Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature. 1993 Oct 21;365(6448):759-61. doi: 10.1038/365759a0. PMID: 8413655. 3. Sakamoto S, Aso T, Masuda H, Goto M, Tamaoki S, Azuma H. Gestational changes in endothelin-1-induced receptors and myometrial contractions in rat. Mol Hum Reprod. 1999 Mar;5(3):270-6. doi: 10.1093/molehr/5.3.270. PMID: 10333362.
In vitro protocol:
1. Breu V, Löffler BM, Clozel M. In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETB receptors. FEBS Lett. 1993 Nov 15;334(2):210-4. doi: 10.1016/0014-5793(93)81713-a. PMID: 8224248. 2. Clozel M, Breu V, Burri K, Cassal JM, Fischli W, Gray GA, Hirth G, Löffler BM, Müller M, Neidhart W, et al. Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature. 1993 Oct 21;365(6448):759-61. doi: 10.1038/365759a0. PMID: 8413655.
In vivo protocol:
1. Sakamoto S, Aso T, Masuda H, Goto M, Tamaoki S, Azuma H. Gestational changes in endothelin-1-induced receptors and myometrial contractions in rat. Mol Hum Reprod. 1999 Mar;5(3):270-6. doi: 10.1093/molehr/5.3.270. PMID: 10333362.
1: Nabokov AV, Amann K, Wessels S, Münter K, Wagner J, Ritz E. Endothelin receptor antagonists influence cardiovascular morphology in uremic rats. Kidney Int. 1999 Feb;55(2):512-9. doi: 10.1046/j.1523-1755.1999.00290.x. PMID: 9987075. 2: Chiou WJ, Magnuson SR, Dixon D, Sundy S, Opgenorth TJ, Wu-Wong JR. Dissociation characteristics of endothelin receptor agonists and antagonists in cloned human type-B endothelin receptor. Endothelium. 1997;5(3):179-89. doi: 10.3109/10623329709053397. PMID: 9272381. 3: Wu-Wong JR, Chiou W, Magnuson SR, Bianchi BR, Lin CW. Human astrocytoma U138MG cells express predominantly type-A endothelin receptor. Biochim Biophys Acta. 1996 May 28;1311(3):155-63. doi: 10.1016/0167-4889(95)00202-2. PMID: 8664342. 4: Wu-Wong JR, Chiou WJ, Magnuson SR, Opgenorth TJ. Endothelin receptor in human astrocytoma U373MG cells: binding, dissociation, receptor internalization. J Pharmacol Exp Ther. 1995 Jul;274(1):499-507. PMID: 7616437. 5: Wu-Wong JR, Chiou WJ, Dixon DB, Opgenorth TJ. Dissociation characteristics of endothelin ETA receptor agonists and antagonists. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S380-4. PMID: 8587421. 6: Wu-Wong JR, Chiou WJ, Magnuson SR, Opgenorth TJ. Endothelin receptor agonists and antagonists exhibit different dissociation characteristics. Biochim Biophys Acta. 1994 Nov 10;1224(2):288-94. doi: 10.1016/0167-4889(94)90202-x. PMID: 7981244. 7: Wu-Wong JR, Chiou WJ, Naugles KE Jr, Opgenorth TJ. Endothelin receptor antagonists exhibit diminishing potency following incubation with agonist. Life Sci. 1994;54(22):1727-34. doi: 10.1016/0024-3205(94)00613-x. PMID: 8177014.