Need Assistance?

US & Canada:
+
UK: +

Our Highlights

GMP Grade Efficient workshop for GMP production.
Optimal Prices Buying products on this site guarantees the best price!
Commercial Batches Independent GMP manufacturing suites that handle commercial batches
Prompt Delivery Warehouses in multiple cities to ensure timely delivery
Flexible Quantity Quantities available from milligrams to ton

E-76

* Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients.

E-76, a potent anticoagulant, is an inhibitor of coagulation factor VIIa. It acts by binding to an exosite on the VIIa protease domain and non-competitively inhibits the activation of factor X and amide hydrolytic activity.

Category

Peptide Inhibitors

Catalog number

BAT-014458

CAS number

1926163-13-4

Molecular Formula

C97H139N27O29S2

Molecular Weight

2211.47

Specification
Reference Reading

IUPAC Name

(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(3S,6S,9S,14R,17S,20S,23S,26S,29S,32S,35S)-9-[[(2S)-2-[[(2S)-2-acetamidopropanoyl]amino]-4-methylpentanoyl]amino]-23,32-bis(3-carbamimidamidopropyl)-3,6,26-tris(carboxymethyl)-17-[(4-hydroxyphenyl)methyl]-20-(1H-indol-3-ylmethyl)-2,5,8,16,19,22,25,28,31,34-decaoxo-29-propan-2-yl-11,12-dithia-1,4,7,15,18,21,24,27,30,33-decazabicyclo[33.3.0]octatriacontane-14-carbonyl]amino]-5-amino-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]-3-methylbutanoyl]amino]-5-[(2-amino-2-oxoethyl)amino]-5-oxopentanoic acid

Synonyms

E-76; Acetyl-ALCDDPRVDRWYCQFVEG-amide; Ac-Ala-Leu-D-Cys-Asp-Asp-Pro-Arg-Val-Asp-Arg-Trp-Tyr-Cys-Gln-Phe-Val-Glu-Gly-NH2 (Disulfide bridge: Cys3-Cys13); N-acetyl-L-alanyl-L-leucyl-D-cysteinyl-L-alpha-aspartyl-L-alpha-aspartyl-L-prolyl-L-arginyl-L-valyl-L-alpha-aspartyl-L-arginyl-L-tryptophyl-L-tyrosyl-L-cysteinyl-L-glutaminyl-L-phenylalanyl-L-valyl-L-alpha-glutamyl-glycinamide (3->13)-disulfide

Appearance

White Powder

Purity

≥95% by HPLC

Density

1.5±0.1 g/cm3

Sequence

Ac-ALCDDPRVDRWYCQFVEG-NH2 (Disulfide bridge: Cys3-Cys13)

Storage

Store at -20°C

Solubility

Soluble in Methanol

InChI

InChI=1S/C97H139N27O29S2/c1-46(2)35-61(113-79(137)49(7)108-50(8)125)84(142)120-69-45-155-154-44-68(90(148)110-60(28-30-71(98)127)82(140)114-63(36-51-17-10-9-11-18-51)89(147)123-77(47(3)4)93(151)112-59(29-31-73(129)130)80(138)107-43-72(99)128)121-85(143)62(37-52-24-26-54(126)27-25-52)115-86(144)64(38-53-42-106-56-20-13-12-19-55(53)56)116-81(139)57(21-14-32-104-96(100)101)109-87(145)66(40-75(133)134)118-94(152)78(48(5)6)122-83(141)58(22-15-33-105-97(102)103)111-92(150)70-23-16-34-124(70)95(153)67(41-76(135)136)119-88(146)65(39-74(131)132)117-91(69)149/h9-13,17-20,24-27,42,46-49,57-70,77-78,106,126H,14-16,21-23,28-41,43-45H2,1-8H3,(H2,98,127)(H2,99,128)(H,107,138)(H,108,125)(H,109,145)(H,110,148)(H,111,150)(H,112,151)(H,113,137)(H,114,140)(H,115,144)(H,116,139)(H,117,149)(H,118,152)(H,119,146)(H,120,142)(H,121,143)(H,122,141)(H,123,147)(H,129,130)(H,131,132)(H,133,134)(H,135,136)(H4,100,101,104)(H4,102,103,105)/t49-,57-,58-,59-,60-,61-,62-,63-,64-,65-,66-,67-,68-,69+,70-,77-,78-/m0/s1

InChI Key

IIZLCMCPDOZBBI-YMLAWGCDSA-N

Canonical SMILES

CC(C)CC(C(=O)NC1CSSCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2CCCN2C(=O)C(NC(=O)C(NC1=O)CC(=O)O)CC(=O)O)CCCNC(=N)N)C(C)C)CC(=O)O)CCCNC(=N)N)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O)C(=O)NC(CCC(=O)N)C(=O)NC(CC6=CC=CC=C6)C(=O)NC(C(C)C)C(=O)NC(CCC(=O)O)C(=O)NCC(=O)N)NC(=O)C(C)NC(=O)C

1. [No title available]

C Schmidt, C Camus, H Caudiu, C Her, E Soudant, R Bazin Int J Cosmet Sci. 1987 Feb;9(1):21-8. doi: 10.1111/j.1467-2494.1987.tb00457.x.

Synopsis Several methods exist for measuring cutaneous relief. Profilometry allows the measurement of the profile of a skin-positive araldite replica. Image analysis detects and measures shadows behind the crests created by glazing lighting on a negative silicone skin replica. We have studied the correlation between both methods for twenty-nine crow's feet replicas. The area explored by image analysis is a circle of fifteen millimeters diameter. The areas explored by profilometry are, on one hand, ten scans 9500 mum long at intervals of 60 mum, i.e., 5.13 mm(2) (D 60 mum), and on the other hand ten scans of the same length at intervals of 900 mum, i.e., 76.95 mm(2) (D 900 mum). All parameters of peak height and surface were correlated. The best correlations were obtained between image analysis and profilometry for D 900 mum. In this case the P parameter (wrinkles depth measured by image analysis) was influenced for 46% by surface S under the peaks and for 33.5% by the peak height H measured by profilometry. In the same way the coefficient of developed skin surface CDSS was influenced for 45% by H and for 44% by S. The field of analysis common to both methods was found to be middle wrinkles with depth between 45 and 100 mum.

2. Anomalous fluctuation properties

H Touchette, E G D Cohen Phys Rev E Stat Nonlin Soft Matter Phys. 2009 Jul;80(1 Pt 1):011114. doi: 10.1103/PhysRevE.80.011114. Epub 2009 Jul 10.

We complement and extend our work on fluctuations arising in nonequilibrium systems in steady states driven by Lévy noise [H. Touchette and E. G. D. Cohen, Phys. Rev. E 76, 020101(R) (2007)]. As a concrete example, we consider a particle subjected to a drag force and a Lévy white noise with tail index mu epsilon (0,2), and calculate the probability distribution of the work done on the particle by the drag force, as well as the probability distribution of the work dissipated by the dragged particle in a nonequilibrium steady state. For 0

3. Therapeutic value of H2-receptor stimulation in congestive heart failure. Hemodynamic effects of BU-E-76, BU-E-75 and arpromidine (BU-E-50) in comparison to impromidine

S B Felix, A Buschauer, G Baumann Agents Actions Suppl. 1991;33:257-69. doi: 10.1007/978-3-0348-7309-3_16.

Previous studies from our department revealed that congestive heart failure (CHF) is paralleled by a decrease in number of sarcolemmal beta-receptors due to excessive levels of circulating endogenous catecholamines. In contrast, the myocardial H2-receptor system proved to be not affected (Am. Heart J. 101; 569, 1981). The first clinically tested specific H2-receptor agonist impromidine (IMP) turned out to be a potent stimulator in patients with CHF which were insensitive to catecholamine stimulation (Pharmacol. Ther. 24; 165, 1984). Though the overall results of such an H2-receptor stimulation were salutary with favourable hemodynamic effects, the narrow therapeutic range, high costs of synthesis and the arrhythmogenic potential of IMP limited its broad clinical application in large scale trials. - Recently developed phenylpyridylalkylguanidines (J. Med. Chem. 32, 1963, 1989) were investigated under in vitro and in vivo conditions in the guinea-pig under physiologic and pathophysiologic conditions using IMP as reference. - Compounds tested were arpromidine (INN) (BU-E-50) and the difluorinated analogues BU-E-75 and BU-E-76, all guanidine-type H2-agonists with additional H1-antagonistic properties due to a pheniramine like moiety. In the isolated perfused heart all three new compounds were more potent in increasing cardiac contractile force and coronary flow but less effective on heart rate and less arrhythmogenic. The same could be established under in vivo conditions where BU-E-76 was more potent than BU-E-75, arpromidine and IMP, respectively, in augmenting LVdp/dt, LVP, cardiac output and systemic blood pressure, but all compounds revealed to have less chronotropic and arrhythmogenic potentials. In the vasopressin-induced acute heart failure model BU-E-76 and BU-E-75 normalized all contractile parameters in contrast to arpromidine and IMP. Within minutes it is concluded that the new H2-receptor agonists may represent a promising therapeutic improvement for treatment of CHF patients with a cardiovascular profile superior to IMP and conventional catecholamines.