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MedKoo Cat#: 597999 | Name: PD 145065

Description:

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

PD 145065 is a non-selective endothelin(A)/endothelin(B) antagonist.

Chemical Structure

PD 145065
PD 145065
CAS#153049-49-1

Theoretical Analysis

MedKoo Cat#: 597999

Name: PD 145065

CAS#: 153049-49-1

Chemical Formula: C52H67N7O10

Exact Mass: 949.4949

Molecular Weight: 950.14

Elemental Analysis: C, 65.73; H, 7.11; N, 10.32; O, 16.84

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 #
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Synonym
PD 145065; PD-145065; PD145065;
IUPAC/Chemical Name
(2S,5S,8S,11S,14S,17R)-2-((1H-indol-3-yl)methyl)-5,8-di((S)-sec-butyl)-11-(carboxymethyl)-17-(10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl)-14-isobutyl-4,7,10,13,16,19-hexaoxo-3,6,9,12,15,18-hexaazaicosanoic acid
InChi Key
HRAQSWKGRRUBDJ-OMUAVVNCSA-N
InChi Code
1S/C52H67N7O10/c1-8-29(5)44(49(65)57-41(52(68)69)25-34-27-53-38-21-15-14-18-35(34)38)59-50(66)45(30(6)9-2)58-48(64)40(26-42(61)62)55-47(63)39(24-28(3)4)56-51(67)46(54-31(7)60)43-36-19-12-10-16-32(36)22-23-33-17-11-13-20-37(33)43/h10-21,27-30,39-41,43-46,53H,8-9,22-26H2,1-7H3,(H,54,60)(H,55,63)(H,56,67)(H,57,65)(H,58,64)(H,59,66)(H,61,62)(H,68,69)/t29-,30-,39-,40-,41-,44-,45-,46+/m0/s1
SMILES Code
O=C(O)[C@H](Cc1c2ccccc2[nH]c1)NC([C@H]([C@@H](C)CC)NC([C@H]([C@@H](C)CC)NC([C@H](CC(O)=O)NC([C@H](CC(C)C)NC([C@H](NC(C)=O)C3c4ccccc4CCc5ccccc53)=O)=O)=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
2934.99.03.00
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 950.14 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
1: Wellings RP, Warner TD, Thiemermann C, Cristol JP, Corder R, Vane JR. Vasoconstriction in the rat kidney induced by endothelin-1 is blocked by PD 145065. J Cardiovasc Pharmacol. 1993;22 Suppl 8:S103-6. PubMed PMID: 7509915. 2: Dobrowolski L, Endlich K, Sadowski J, Steinhausen M. Cardiovascular and renal effects of endothelin receptor blockade with PD 145065 and interaction with urodilatin. Acta Physiol Scand. 1997 Jan;159(1):7-13. PubMed PMID: 9124073. 3: Norota I, Endoh M. Pharmacological characteristics of endothelin receptors in the rabbit ventricular myocardium: the nonselective endothelin receptor antagonist PD 145065 antagonizes the positive inotropic effect of endothelin-3 but not of endothelin-1. Mol Cell Biochem. 1996 Jul-Aug;160-161:67-74. PubMed PMID: 8901457. 4: Wellings RP, Corder R, Doherty AM, Vane JR. Antagonism of renal and systemic responses to endothelin-1 infusion with PD 145065. Eur J Pharmacol. 1994 Apr 21;256(2):201-4. PubMed PMID: 8050471. 5: Warner TD, Allcock GH, Vane JR. Reversal of established responses to endothelin-1 in vivo and in vitro by the endothelin receptor antagonists, BQ-123 and PD 145065. Br J Pharmacol. 1994 May;112(1):207-13. PubMed PMID: 8032643; PubMed Central PMCID: PMC1910322. 6: Battistini B, Warner TD, Fournier A, Vane JR. Comparison of PD 145065 and Ro 46-2005 as antagonists of contractions of guinea-pig airways induced by endothelin-1 or IRL 1620. Eur J Pharmacol. 1994 Feb 11;252(3):341-5. PubMed PMID: 8162956. 7: Battistini B, Warner TD, Fournier A, Vane JR. Characterization of ETB receptors mediating contractions induced by endothelin-1 or IRL 1620 in guinea-pig isolated airways: effects of BQ-123, FR139317 or PD 145065. Br J Pharmacol. 1994 Apr;111(4):1009-16. PubMed PMID: 8032583; PubMed Central PMCID: PMC1910170. 8: Allcock GH, Warner TD, Vane JR. Roles of endothelin receptors in the regional and systemic vascular responses to ET-1 in the anaesthetized ganglion-blocked rat: use of selective antagonists. Br J Pharmacol. 1995 Nov;116(5):2482-6. PubMed PMID: 8581288; PubMed Central PMCID: PMC1909069. 9: Doherty AM, Cody WL, He JX, DePue PL, Cheng XM, Welch KM, Flynn MA, Reynolds EE, LaDouceur DM, Davis LS, et al. In vitro and in vivo studies with a series of hexapeptide endothelin antagonists. J Cardiovasc Pharmacol. 1993;22 Suppl 8:S98-102. PubMed PMID: 7510009. 10: Castro-Chaves P, Fontes-Carvalho R, Pintalhao M, Pimentel-Nunes P, Leite-Moreira AF. Angiotensin II-induced increase in myocardial distensibility and its modulation by the endocardial endothelium in the rabbit heart. Exp Physiol. 2009 Jun;94(6):665-74. doi: 10.1113/expphysiol.2008.046458. Epub 2009 Apr 3. PubMed PMID: 19346335. 11: Warner TD, Battistini B, Allcock GH, Vane JR. Endothelin ETA and ETB receptors mediate vasoconstriction and prostanoid release in the isolated kidney of the rat. Eur J Pharmacol. 1993 Dec 21;250(3):447-53. PubMed PMID: 8112405. 12: Seo JW, Jones SM, Hostetter TA, Iliff JJ, West GA. Methamphetamine induces the release of endothelin. J Neurosci Res. 2016 Feb;94(2):170-8. doi: 10.1002/jnr.23697. Epub 2015 Nov 16. PubMed PMID: 26568405. 13: Tanus-Santos JE, Gordo WM, Udelsmann A, Cittadino MH, Moreno H Jr. Nonselective endothelin-receptor antagonism attenuates hemodynamic changes after massive pulmonary air embolism in dogs. Chest. 2000 Jul;118(1):175-9. PubMed PMID: 10893375. 14: Han HK, Stewart BH, Doherty AM, Cody WL, Amidon GL. In vitro stability and intestinal absorption characteristics of hexapeptide endothelin receptor antagonists. Life Sci. 1998;63(18):1599-609. PubMed PMID: 9806213. 15: Stewart BH, Reyner EL, Tse E, Hayes RN, Werness S, He JX, Cody WL, Doherty AM. In vitro assessment of oral delivery for hexapeptide endothelin antagonists. Life Sci. 1996;58(12):971-82. PubMed PMID: 8786709. 16: Wenzel RR, Noll G, Lüscher TF. Endothelin receptor antagonists inhibit endothelin in human skin microcirculation. Hypertension. 1994 May;23(5):581-6. PubMed PMID: 8175165. 17: Kato T, Kassab S, Wilkins FC Jr, Kirchner KA, Keiser J, Granger JP. Endothelin antagonists improve renal function in spontaneously hypertensive rats. Hypertension. 1995 Apr;25(4 Pt 2):883-7. PubMed PMID: 7721448. 18: Wellings RP, Corder R, Warner TD, Cristol JP, Thiemermann C, Vane JR. Evidence from receptor antagonists of an important role for ETB receptor-mediated vasoconstrictor effects of endothelin-1 in the rat kidney. Br J Pharmacol. 1994 Feb;111(2):515-20. PubMed PMID: 8004396; PubMed Central PMCID: PMC1909948. 19: Battistini B, O'Donnell LJ, Warner TD, Fournier A, Farthing MJ, Vane JR. Characterization of endothelin (ET) receptors in the isolated gall bladder of the guinea-pig: evidence for an additional ET receptor subtype. Br J Pharmacol. 1994 Aug;112(4):1244-50. PubMed PMID: 7952887; PubMed Central PMCID: PMC1910268. 20: Banting JD, Friberg P, Adams MA. Acute hypertension after nitric oxide synthase inhibition is mediated primarily by increased endothelin vasoconstriction. J Hypertens. 1996 Aug;14(8):975-81. PubMed PMID: 8884552.

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