MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 463204 | Name: E 2078

Description:

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

E 2078 is a stabilized dynorphin A(1-8) analog.

Chemical Structure

E 2078
E 2078
CAS#103613-84-9

Theoretical Analysis

MedKoo Cat#: 463204

Name: E 2078

CAS#: 103613-84-9

Chemical Formula: C50H81N15O9

Exact Mass: 1035.6342

Molecular Weight: 1036.29

Elemental Analysis: C, 57.95; H, 7.88; N, 20.27; O, 13.89

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.
Bulk Inquiry
Related CAS #
No Data
Synonym
E 2078; E2078; E-2078;
IUPAC/Chemical Name
(S)-N-((R)-1-amino-4-methyl-1-oxopentan-2-yl)-2-((3S,12S,15S,18S)-12-benzyl-18-(3-guanidinopropyl)-3-(4-hydroxybenzyl)-15-isobutyl-N-methyl-4,7,10,13,16-pentaoxo-2,5,8,11,14,17-hexaazanonadecan-19-amido)-N-ethyl-5-guanidinopentanamide
InChi Key
UPIUIXNIRHGCEK-BYAJYZPISA-N
InChi Code
InChI=1S/C50H81N15O9/c1-8-65(40(43(51)69)25-31(4)5)48(74)39(17-13-23-58-50(54)55)64(7)47(73)35(16-12-22-57-49(52)53)62-45(71)37(24-30(2)3)63-46(72)38(27-32-14-10-9-11-15-32)61-42(68)29-59-41(67)28-60-44(70)36(56-6)26-33-18-20-34(66)21-19-33/h9-11,14-15,18-21,30-31,35-40,56,66H,8,12-13,16-17,22-29H2,1-7H3,(H2,51,69)(H,59,67)(H,60,70)(H,61,68)(H,62,71)(H,63,72)(H4,52,53,57)(H4,54,55,58)/t35-,36-,37-,38-,39-,40+/m0/s1
SMILES Code
CC(C)C[C@H](C(N)=O)N(C([C@H](CCCNC(N)=N)N(C([C@H](CCCNC(N)=N)NC([C@H](CC(C)C)NC([C@H](CC1=CC=CC=C1)NC(CNC(CNC([C@H](CC2=CC=C(O)C=C2)NC)=O)=O)=O)=O)=O)=O)C)=O)CC
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 1,036.29 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: Mori T, Nomura M, Yoshizawa K, Nagase H, Narita M, Suzuki T. Differential properties between TRK-820 and U-50,488H on the discriminative stimulus effects in rats. Life Sci. 2004 Oct 1;75(20):2473-82. doi: 10.1016/j.lfs.2004.05.017. PMID: 15350822. 2: Butelman ER, Ball JW, Kreek MJ. Peripheral selectivity and apparent efficacy of dynorphins: comparison to non-peptidic kappa-opioid agonists in rhesus monkeys. Psychoneuroendocrinology. 2004 Apr;29(3):307-26. doi: 10.1016/s0306-4530(03)00030-1. PMID: 14644063. 3: Butelman ER, Ball JW, Harris TJ, Kreek MJ. Topical capsaicin-induced allodynia in unanesthetized primates: pharmacological modulation. J Pharmacol Exp Ther. 2003 Sep;306(3):1106-14. doi: 10.1124/jpet.103.052381. Epub 2003 Jun 26. PMID: 12829725. 4: Hiramatsu M, Inoue K, Ambo A, Sasaki Y, Kameyama T. Long-lasting antinociceptive effects of a novel dynorphin analogue, Tyr-D-Ala-Phe-Leu-Arg psi (CH(2)NH) Arg-NH(2), in mice. Br J Pharmacol. 2001 Apr;132(8):1948-56. doi: 10.1038/sj.bjp.0703982. PMID: 11309268; PMCID: PMC1572722. 5: Butelman ER, Harris TJ, Kreek MJ. Effects of E-2078, a stable dynorphin A(1-8) analog, on sedation and serum prolactin levels in rhesus monkeys. Psychopharmacology (Berl). 1999 Nov;147(1):73-80. doi: 10.1007/s002130051144. PMID: 10591871. 6: Asai Y, Watanabe S. Effect of a Dynorphin A analog, E2078, on phospholipid membrane properties. Biol Pharm Bull. 1999 May;22(5):543-5. doi: 10.1248/bpb.22.543. PMID: 10375180. 7: Butelman ER, Vivian JA, Yu J, Kreek MJ, Woods JH. Systemic effects of E-2078, a stabilized dynorphin A(1-8) analog, in rhesus monkeys. Psychopharmacology (Berl). 1999 Apr;143(2):190-6. doi: 10.1007/s002130050935. PMID: 10326782. 8: Sai Y, Kajita M, Tamai I, Wakama J, Wakamiya T, Tsuji A. Adsorptive-mediated endocytosis of a basic peptide in enterocyte-like Caco-2 cells. Am J Physiol. 1998 Sep;275(3):G514-20. doi: 10.1152/ajpgi.1998.275.3.G514. PMID: 9724263. 9: Fujibayashi K, Kubota K, Saito K. Effects of R-84760, a selective kappa- opioid receptor agonist, on nociceptive reflex in isolated neonatal rat spinal cord. Eur J Pharmacol. 1998 Feb 19;343(2-3):171-7. doi: 10.1016/s0014-2999(97)01550-1. PMID: 9570465. 10: Yu J, Butelman ER, Woods JH, Chait BT, Kreek MJ. Dynorphin A (1-8) analog, E-2078, crosses the blood-brain barrier in rhesus monkeys. J Pharmacol Exp Ther. 1997 Aug;282(2):633-8. PMID: 9262324. 11: Yu J, Butelman ER, Woods JH, Chait BT, Kreek MJ. Dynorphin A (1-8) analog, E-2078, is stable in human and rhesus monkey blood. J Pharmacol Exp Ther. 1997 Mar;280(3):1147-51. PMID: 9067297. 12: Tsuda M, Suzuki T, Misawa M, Nagase H. Involvement of the opioid system in the anxiolytic effect of diazepam in mice. Eur J Pharmacol. 1996 Jun 20;307(1):7-14. doi: 10.1016/0014-2999(96)00219-1. PMID: 8831097. 13: Fujimoto K, Momose T. [Analgesic efficacy of E2078 (dynorphin analog) in patients following abdominal surgery]. Masui. 1995 Sep;44(9):1233-7. Japanese. PMID: 8523656. 14: Ohnishi A, Mihara M, Yasuda S, Tomono Y, Hasegawa J, Tanaka T. Aquaretic effect of the stable dynorphin-A analog E2078 in the human. J Pharmacol Exp Ther. 1994 Jul;270(1):342-7. PMID: 7913498. 15: Chen SZ, Han JS. [Cholecystokinin octapeptide antagonized the effect of NDAP on CaM in rat dorsal spinal synaptosome]. Sheng Li Xue Bao. 1994 Apr;46(2):120-5. Chinese. PMID: 7973792. 16: Funada M, Suzuki T, Narita M, Misawa M, Nagase H. Blockade of morphine reward through the activation of kappa-opioid receptors in mice. Neuropharmacology. 1993 Dec;32(12):1315-23. doi: 10.1016/0028-3908(93)90026-y. PMID: 7908722. 17: Bals-Kubik R, Ableitner A, Herz A, Shippenberg TS. Neuroanatomical sites mediating the motivational effects of opioids as mapped by the conditioned place preference paradigm in rats. J Pharmacol Exp Ther. 1993 Jan;264(1):489-95. PMID: 8093731. 18: Salas SP, Roblero JS, López LF, Tachibana S, Huidobro-Toro JP. [N-methyl- Tyr1,N-methyl-Arg7-D-Leu8]-dynorphin-A-(1-8)ethylamide, a stable dynorphin analog, produces diuresis by kappa-opiate receptor activation in the rat. J Pharmacol Exp Ther. 1992 Sep;262(3):979-86. PMID: 1356155. 19: Ohno M, Yamamoto T, Ueki S. Analgesic and discriminative stimulus properties of U-62,066E, the selective kappa-opioid receptor agonist, in the rat. Psychopharmacology (Berl). 1992;106(1):31-8. doi: 10.1007/BF02253585. PMID: 1346721. 20: Valenzuela R, Tachibana S, Huidobro-Toro JP. E-2078, a potent, selective and stable dynorphin analog with preferential activity for the kappa-opioid receptor subtype on the mouse vas deferens neuroeffector junction. Peptides. 1991 Nov- Dec;12(6):1211-4. doi: 10.1016/0196-9781(91)90196-v. PMID: 1687708.

View History

U 43795

U 43795