WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H463204
CAS#: 103613-84-9
Description: E 2078 is a stabilized dynorphin A(1-8) analog.
Hodoodo Cat#: H463204
Name: E 2078
CAS#: 103613-84-9
Chemical Formula: C50H81N15O9
Exact Mass: 1,035.63
Molecular Weight: 1,036.294
Elemental Analysis: C, 57.95; H, 7.88; N, 20.27; O, 13.89
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.
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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
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.
| 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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
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.
