PD-156707 | CAS#162412-70-6 | Endothelin A Receptor Antagonist

PD-156707
featured

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

MedKoo CAT#: 532448

CAS#: 162412-70-6

Description: PD-156707 is an endothelin A receptor-selective antagonist.

Chemical Structure

PD-156707

CAS# 162412-70-6

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 532448
Name: PD-156707
CAS#: 162412-70-6
Chemical Formula: C28H25NaO9
Exact Mass: 528.14
Molecular Weight: 528.489
Elemental Analysis: C, 63.64; H, 4.77; Na, 4.35; O, 27.25

Price and Availability

Size	Price	Availability
5mg	USD 265	2 Weeks
25mg	USD 730	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: PD-156707; PD 156707; PD156707.

IUPAC/Chemical Name: sodium (Z)-2-(1,3-benzodioxol-5-yl)-4-(4-methoxyphenyl)-4-oxo-3-[(3,4,5-trimethoxyphenyl)methyl]but-2-enoate

InChi Key: ZLHQEGFYBMZQGM-RKVLWQGQSA-M

InChi Code: InChI=1S/C28H26O9.Na/c1-32-19-8-5-17(6-9-19)26(29)20(11-16-12-23(33-2)27(35-4)24(13-16)34-3)25(28(30)31)18-7-10-21-22(14-18)37-15-36-21;/h5-10,12-14H,11,15H2,1-4H3,(H,30,31);/q;+1/p-1/b25-20-;

SMILES Code: O=C([O-])/C(C1=CC=C(OCO2)C2=C1)=C(CC3=CC(OC)=C(OC)C(OC)=C3)\C(C4=CC=C(OC)C=C4)=O.[Na+]

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

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

Certificate of Analysis:

View CoA: current batch, Lot# S8G10M18

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:	PD-156707 is an endothelin A receptor-selective antagonist.
In vitro activity:	PD156707 (Parke-Davis) is one of a series of novel, orally-active butenolide endothelin antagonists and is highly selective for the ETA receptor. PD156707 exhibits subnanomolar affinity and greater than 1000-fold selectivity for human ETA receptors and potently inhibits ET-1-mediated vasoconstriction in human isolated blood vessels. Reference: Expert Opin Investig Drugs. 1999 Jan;8(1):71-8. https://pubmed.ncbi.nlm.nih.gov/15992060/
In vivo activity:	Newborn rats were exposed to anoxia twice daily from postnatal day 1 to 3, and hearts were isolated and studied at postnatal day 4 (P4), 7 (P7), and 14 (P14). Newborn administration of PD156707, an ETA-receptor antagonist, significantly increased cardiomyocyte proliferation at P4 and cell size at P7, resulting in an increase in the heart to body weight ratio in P7 neonates. In addition, PD156707 abrogated the anoxia-mediated effects. Reference: PLoS One. 2015 Feb 18;10(2):e0116600. https://pubmed.ncbi.nlm.nih.gov/25692855/

Preparing Stock Solutions

The following data is based on the product molecular weight 528.49 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.

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. Maguire JJ, Davenport AP. The therapeutic potential of PD156707 and related butenolide endothelin antagonists. Expert Opin Investig Drugs. 1999 Jan;8(1):71-8. doi: 10.1517/13543784.8.1.71. PMID: 15992060. 2. Harland SP, Kuc RE, Pickard JD, Davenport AP. Expression of endothelin(A) receptors in human gliomas and meningiomas, with high affinity for the selective antagonist PD156707. Neurosurgery. 1998 Oct;43(4):890-8; discussion 898-9. doi: 10.1097/00006123-199810000-00097. PMID: 9766317. 3. Paradis AN, Gay MS, Wilson CG, Zhang L. Newborn hypoxia/anoxia inhibits cardiomyocyte proliferation and decreases cardiomyocyte endowment in the developing heart: role of endothelin-1. PLoS One. 2015 Feb 18;10(2):e0116600. doi: 10.1371/journal.pone.0116600. PMID: 25692855; PMCID: PMC4334650. 4. Wedgwood S, McMullan DM, Bekker JM, Fineman JR, Black SM. Role for endothelin-1-induced superoxide and peroxynitrite production in rebound pulmonary hypertension associated with inhaled nitric oxide therapy. Circ Res. 2001 Aug 17;89(4):357-64. doi: 10.1161/hh1601.094983. PMID: 11509453.
In vitro protocol:	1. Maguire JJ, Davenport AP. The therapeutic potential of PD156707 and related butenolide endothelin antagonists. Expert Opin Investig Drugs. 1999 Jan;8(1):71-8. doi: 10.1517/13543784.8.1.71. PMID: 15992060. 2. Harland SP, Kuc RE, Pickard JD, Davenport AP. Expression of endothelin(A) receptors in human gliomas and meningiomas, with high affinity for the selective antagonist PD156707. Neurosurgery. 1998 Oct;43(4):890-8; discussion 898-9. doi: 10.1097/00006123-199810000-00097. PMID: 9766317.
In vivo protocol:	1. Paradis AN, Gay MS, Wilson CG, Zhang L. Newborn hypoxia/anoxia inhibits cardiomyocyte proliferation and decreases cardiomyocyte endowment in the developing heart: role of endothelin-1. PLoS One. 2015 Feb 18;10(2):e0116600. doi: 10.1371/journal.pone.0116600. PMID: 25692855; PMCID: PMC4334650. 2. Wedgwood S, McMullan DM, Bekker JM, Fineman JR, Black SM. Role for endothelin-1-induced superoxide and peroxynitrite production in rebound pulmonary hypertension associated with inhaled nitric oxide therapy. Circ Res. 2001 Aug 17;89(4):357-64. doi: 10.1161/hh1601.094983. PMID: 11509453.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

1: Höltke C, Law MP, Wagner S, Breyholz HJ, Kopka K, Bremer C, Levkau B, Schober O, Schäfers M. Synthesis, in vitro pharmacology and biodistribution studies of new PD 156707-derived ET(A) receptor radioligands. Bioorg Med Chem. 2006 Mar 15;14(6):1910-7. Epub 2005 Nov 10. PubMed PMID: 16289856.

2: Coe Y, Haleen SJ, Welch KM, Liu YA, Coceani F. The endothelin A receptor antagonists PD 156707 (CI-1020) and PD 180988 (CI-1034) reverse the hypoxic pulmonary vasoconstriction in the perinatal lamb. J Pharmacol Exp Ther. 2002 Aug;302(2):672-80. PubMed PMID: 12130731.

3: Doherty AM, Uprichard AC. Discovery and development of an endothelin A receptor-selective antagonist PD 156707. Pharm Biotechnol. 1998;11:81-112. Review. PubMed PMID: 9760677.

4: Ignasiak DP, McClanahan TB, Saganek LJ, Potoczak RE, Hallak H, Gallagher KP. Effects of endothelin ETA receptor antagonism with PD 156707 on hemodynamics and renal vascular resistance in rabbits. Eur J Pharmacol. 1997 Mar 5;321(3):295-300. PubMed PMID: 9085040.

5: Mertz TE, McClanahan TB, Flynn MA, Juneau P, Reynolds EE, Hallak H, Bradford L, Gallagher KP. Endothelin A receptor antagonism by PD 156707 does not reduce infarct size after coronary artery occlusion/reperfusion in pigs. J Pharmacol Exp Ther. 1996 Jul;278(1):42-9. PubMed PMID: 8764334.

6: Rossi DT, Hallak H, Bradford L. Liquid chromatographic assay for a butenolide endothelin antagonist (PD 156707) in plasma. J Chromatogr B Biomed Appl. 1996 Mar 3;677(2):299-304. PubMed PMID: 8704933.

7: Reynolds EE, Keiser JA, Haleen SJ, Walker DM, Olszewski B, Schroeder RL, Taylor DG, Hwang O, Welch KM, Flynn MA, et al. Pharmacological characterization of PD 156707, an orally active ETA receptor antagonist. J Pharmacol Exp Ther. 1995 Jun;273(3):1410-7. PubMed PMID: 7791115.

Your view history

PD-156707 featured