FR 139317 - CAS 142375-60-8
Catalog number:
142375-60-8
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C33H44N6O5
Molecular Weight:
604.75
COA:
Inquire
Targets:
Endothelin Receptor
Description:
FR 139317 is a selective Endothelin A receptor antagonist originated by Fujisawa. (Ki values are 1 nM and 7.3 μM at ETA and ETB subtypes respectively). No development was reported for the treatment of Cerebrovascular disorders, Coronary disorders, Diabetic nephropathies, Heart failure, Hypertension, Ischaemic heart disorders, Myocardial infarction and Renal failure.
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Purity:
98 %
Appearance:
White solid
Synonyms:
PD 147953;2-((1-(Hexahydro-1H-azepinyl)carbonyl)amino-4-methylpentanoyl)-3-(-(1-methyl-1H-indolyl)propionyl)amino-3-(2-pyridyl)propionic acid
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Cerebrovascular disorders; Coronary disorders; Diabetic nephropathies; Heart failure; Hypertension; Ischaemic heart disorders; Myocardial infarction; Renal failure
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Density:
1.27 g/cm3
InChIKey:
LIOKMIQQPDDTNO-UPRLRBBYSA-N
InChI:
1S/C33H44N6O5/c1-22(2)18-26(37-33(44)39-16-10-4-5-11-17-39)30(40)35-27(19-23-21-38(3)29-14-7-6-13-25(23)29)31(41)36-28(32(42)43)20-24-12-8-9-15-34-24/h6-9,12-15,21-22,26-28H,4-5,10-11,16-20H2,1-3H3,(H,35,40)(H,36,41)(H,37,44)(H,42,43)/t26-,27+,28+/m0/s1
Canonical SMILES:
c12c(c(C[C@@H](NC([C@@H](NC(=O)N3CCCCCC3)CC(C)C)=O)C(=O)N[C@@H](C(O)=O)Cc3ncccc3)cn2C)cccc1
Current Developer:
Originator Fujisawa
1.Investigation into the potential anti-inflammatory effects of endothelin antagonists in a murine model of experimental monosodium urate peritonitis.
Getting SJ1, Di Filippo C, Lam CW, Rossi F, D'Amico M. J Pharmacol Exp Ther. 2004 Jul;310(1):90-7. Epub 2004 Mar 2.
Endothelin (ET)-1 has been detected in many inflammatory pathologies, including rheumatoid arthritic patients, asthma, and ischemic-reperfusion injury. In this study, we have investigated the effect of a panel of different ET-1 antagonists displaying different selectivities for the receptors in a murine model of experimental inflammatory peritonitis. Systemic treatment of mice with the ETA antagonist C33H44N6O5, N-[N-[-N(hexahydro-1H-azepin-1-yl)carbonyl]-L-leucyl]-1-methyl-D-tryptophyl]-3-(2-pyridinyl)-D-alanine (FR139317) inhibited neutrophil accumulation. However, a greater degree of inhibition was observed with the ETB antagonist C34H51N5O7, N-cis-2,6-dimethylpiperidinocarbonyl-b-tBu-Ala-D-Trp(1-methoxycarbonyl)-D-Nle-OH (BQ-788) and the ET(A and B) antagonist C52H65N7O10, N-acetyl-alpha-[10,11-dihydro-5H-dibenzo-[a,d]cycloheptadien-5-yl]-D-Gly-Leu-Asp-lle-lle-Trp (PD145065); all these effects occurred without altering peripheral blood cell counts.
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CAS 142375-60-8 FR 139317

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