MedKoo Cat#: 535169 | Name: PD 151242

Description:

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

PD 151242 is an endothelin receptor antagonist.

Chemical Structure

PD 151242
PD 151242
CAS#155561-67-4

Theoretical Analysis

MedKoo Cat#: 535169

Name: PD 151242

CAS#: 155561-67-4

Chemical Formula: C34H45N5O6

Exact Mass: 619.3370

Molecular Weight: 619.76

Elemental Analysis: C, 65.89; H, 7.32; N, 11.30; O, 15.49

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
PD 151242; PD-151242; PD151242
IUPAC/Chemical Name
D-Tyrosine, N-(N-(N-((hexahydro-1H-azepin-1-yl)carbonyl)-L-leucyl)-1-methyl-D-tryptophyl)-
InChi Key
JVILFANCFWZBFU-ZGIBFIJWSA-N
InChi Code
InChI=1S/C34H45N5O6/c1-22(2)18-27(37-34(45)39-16-8-4-5-9-17-39)31(41)35-28(20-24-21-38(3)30-11-7-6-10-26(24)30)32(42)36-29(33(43)44)19-23-12-14-25(40)15-13-23/h6-7,10-15,21-22,27-29,40H,4-5,8-9,16-20H2,1-3H3,(H,35,41)(H,36,42)(H,37,45)(H,43,44)/t27-,28+,29+/m0/s1
SMILES Code
OC1=CC=C(C=C1)C[C@H](C(O)=O)NC([C@@H](CC2=CN(C)C3=C2C=CC=C3)NC([C@H](CC(C)C)NC(N4CCCCCC4)=O)=O)=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
Shelf Life
>3 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

Preparing Stock Solutions

The following data is based on the product molecular weight 619.76 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
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Naunyn Schmiedebergs Arch Pharmacol. 1999 Jun;359(6):471-6. doi: 10.1007/pl00005378. PMID: 10431758. 5: Dashwood MR, Timm M, Kaski JC. Regional variations in ETA/ETB binding sites in human coronary vasculature. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S351-4. PMID: 8587412. 6: Kohnen G, Campbell S, Irvine GA, Church HJ, MacLachlan F, Titterington M, Cameron IT. Endothelin receptor expression in human decidua. Mol Hum Reprod. 1998 Feb;4(2):185-93. doi: 10.1093/molehr/4.2.185. PMID: 9542978. 7: Collett GP, Kohnen G, Campbell S, Davenport AP, Jeffers MD, Cameron IT. Localization of endothelin receptors in human uterus throughout the menstrual cycle. Mol Hum Reprod. 1996 Jun;2(6):439-44. doi: 10.1093/molehr/2.6.439. PMID: 9238714. 8: D'Amico M, Dashwood MR, Warner TD. Endothelin-1 and the periaqueductal gray area of the rat: an autoradiographic and functional pharmacological study. Br J Pharmacol. 1996 May;118(1):21-6. doi: 10.1111/j.1476-5381.1996.tb15361.x. PMID: 8733571; PMCID: PMC1909490. 9: Di Filippo C, Filippelli A, Rinaldi B, Piegari E, Esposito F, Rossi F, D'Amico M. Chronic peripheral ouabain treatment affects the brain endothelin system of rats. J Hypertens. 2003 Apr;21(4):747-53. doi: 10.1097/00004872-200304000-00018. PMID: 12658021. 10: Nava P, Carbó R, Guarner V. Coronary and femoral arterial contraction with high glucose, insulin, and glucose-insulin-potassium solution: effects of hypoxia. Heart Vessels. 2002 Jan;16(2):57-63. doi: 10.1007/s380-002-8318-5. PMID: 11833843. 11: Kuc R, Davenport AP. Comparison of endothelin-A and endothelin-B receptor distribution visualized by radioligand binding versus immunocytochemical localization using subtype selective antisera. J Cardiovasc Pharmacol. 2004 Nov;44 Suppl 1:S224-6. doi: 10.1097/01.fjc.0000166260.35099.d5. PMID: 15838285. 12: Docherty CC, Kalmar-Nagy J, Engelen M, Koenen SV, Nijland M, Kuc RE, Davenport AP, Nathanielsz PW. Effect of in vivo fetal infusion of dexamethasone at 0.75 GA on fetal ovine resistance artery responses to ET-1. Am J Physiol Regul Integr Comp Physiol. 2001 Jul;281(1):R261-8. doi: 10.1152/ajpregu.2001.281.1.R261. PMID: 11404302. 13: Maguire JJ, Davenport AP. Endothelin receptor expression and pharmacology in human saphenous vein graft. Br J Pharmacol. 1999 Jan;126(2):443-50. doi: 10.1038/sj.bjp.0702326. PMID: 10077237; PMCID: PMC1565828. 14: Harada N, Himeno A, Shigematsu K, Sumikawa K, Niwa M. Endothelin-1 binding to endothelin receptors in the rat anterior pituitary gland: possible formation of an ETA-ETB receptor heterodimer. Cell Mol Neurobiol. 2002 Apr;22(2):207-26. doi: 10.1023/a:1019822107048. PMID: 12363203. 15: Harland SP, Kuc RE, Pickard JD, Davenport AP. Characterization of endothelin receptors in human brain cortex, gliomas, and meningiomas. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S408-11. PMID: 8587429. 16: Peter MG, Davenport AP. Selectivity of [125I]-PD151242 for human, rat and porcine endothelin ETA receptors in the heart. Br J Pharmacol. 1995 Jan;114(2):297-302. doi: 10.1111/j.1476-5381.1995.tb13226.x. PMID: 7881728; PMCID: PMC1510233. 17: Khan MA, Dashwood MR, Mumtaz FH, Thompson CS, Mikhailidis DP, Morgan RJ. Upregulation of endothelin A receptor sites in the rabbit diabetic kidney: potential relevance to the early pathogenesis of diabetic nephropathy. Nephron. 1999;83(3):261-7. doi: 10.1159/000045519. PMID: 10529633. 18: Pierre LN, Davenport AP. Relative contribution of endothelin A and endothelin B receptors to vasoconstriction in small arteries from human heart and brain. J Cardiovasc Pharmacol. 1998;31 Suppl 1:S74-6. doi: 10.1097/00005344-199800001-00024. PMID: 9595405. 19: Yu JC, Pickard JD, Davenport AP. Endothelin ETA receptor expression in human cerebrovascular smooth muscle cells. Br J Pharmacol. 1995 Nov;116(5):2441-6. doi: 10.1111/j.1476-5381.1995.tb15093.x. PMID: 8581282; PMCID: PMC1909054. 20: Bacon CR, Davenport AP. Endothelin receptors in human coronary artery and aorta. Br J Pharmacol. 1996 Mar;117(5):986-92. doi: 10.1111/j.1476-5381.1996.tb15292.x. PMID: 8851522; PMCID: PMC1909397.