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Ghrelin, Obestatin & Nesfatin

G
rowth hormone releasing peptide 6 (GHRP-6) was Feeding Regulatory
the first synthetic peptide that was shown to re- Peptides Series
lease growth hormone (GH) and stimulate weight
gain by binding to growth hormone secretagogue Peptides International offers obestatin, truncated obestatin,
receptor type 1a (GSR1a).1-2 Ghrelin, the endogenous ligand full length acyl and des-acyl ghrelin and ghrelin fragments,
for GSR1a, was later isolated.3 This orexigenic and GH releas- and several ghrelin antagonists to complete your research
ing peptide is derived from ghrelin preproprotein. It is ex- needs. Our acyl and des-acyl ghrelin fragments consist-
pressed primarily in the stomach and has been shown to de- ing of the first 5, 10, 14 or 18 amino acids and contain the
crease insulin levels and increase appetite, body weight gain, core amino acids required for proper binding and activa-
fat accumulation, and glucose and GH levels, suggesting this tion of GHSR1a.13 [Dap3]-Ghrelin (Rat) (PGH-3680-PI) and
peptide plays a highly important physiological role in metab- [Dap3]-Ghrelin (Human, Rat, 1-5) (PGH-3681-PI) analogs
olism.3,4-7 In addition, it may also modulate cell proliferation are replaced with 2,3-diaminopropionic acid (Dap) at Ser3.
of cancer cells and cardiomyocytes. 8-9 This substitution should make the analogs more stable and
less susceptible to esterases and acyl migration.13 Ghrelin
Two forms of ghrelin can be found in circulation: an acyl- analogs with the Dap substitution have been shown to acti-
ated form and a non-acylated form. The acylated form of vate growth hormone secretagogues receptor 1a (GHSR1a)
ghrelin contains an n-octanoic acid at the Ser3 residue that is just as efficiently as the parent peptide.13 The variety
required for activation of GSR1a. Therefore, it was originally of research tools we are able to offer at Peptides
believed that des-acyl ghrelin, which lacks this esterification International may help scientists elucidate the complex regu-
at Ser3, is an inactive form though it is the predominant one lation of appetite and weight gain.
found in circulation. Accumulating evidence, however, in-
dicates that des-acyl ghrelin can counteract some metabolic Nesfatin-1 was discovered in 2006 by Oh-I and colleagues.14
responses of acylated ghrelin in humans, and mice injected The peptide is secreted from hypothalamic nuclei, which
with or over expressed with the des-acyl form were found to are responsible for controlling appetite. In this same report,
decrease food intake and gastric emptying.4, 5, 10 Other studies nesfatin-1 suppressed food intake in obese mice with a
showed both forms of ghrelin mediate cell proliferation and leptin gene knockout. This finding implies that the peptide
fat accumulation.8, 9, 11 Collectively, these studies suggest an may function as an appetite suppressant independent of the
alternative receptor exists for ghrelin that is not dependent leptin pathway.15
on n-octanoylation of Ser3 for activation. Studying des-acyl Peptides International is pleased to offer our Nesfatin-1
ghrelin may offer new insight into the regulation of homeo- (Human), Nesfatin-1 (Rat), Nesfatin-1 Like Peptide
stasis and energy balance. (Mouse)and Nesfatin-1 (30-59) (Human), along with all of
O = C - (CH ) - CH our Ghelin and Obestatin products for your research activi-
26 3
O Ghrelin (Human) ties.
1. A.D. Howard et al., Science, 273, 974 (1996).
2. C.Y. Bowers, et al., Endocrinology, 114, 1537 (1984).
3. M. Kojima, et al., Nature, 402, 656 (1999).
4. F. Broglio, et al., J. Clin. Endoc. and Metabolism, 89, 3062 (2004).
Currently, in addition to ghrelin, a number of gastrointesti- 5. C. Gauna et al., J. Clin. Endoc. and Metabolism, 89, 5035 (2004).
6. M. Tschop, et al., Nature, 407, 908 (2000).
nal hormones have been identified that control appetite by 7. A. Asakawa, et al., Gastroenterology, 120, 337 (2001).
either stimulating food intake and gastric emptying or inhib- 8. P. Cassoni, et al., Eur. J. Endoc., 150, 173 (2004).
9. G. Baldanzi, et al., J. Cell Biol., 159, 1029 (2002).
iting these responses. Zhang et al. has recently identified one 10. A. Asakawa, et al., Gut, 54, 18 (2005).
of the newest members of this family by using bioinformatic 11. N.M. Thompson, et al., Endoc., 145, 234 (2004).
12 J.V. Zhang, et al., Science, 310, 996 (2005).
predictions about enzyme cleavage of the prepropeptide of 13. M.A. Bednarek, et al., J. Med. Chem., 43, 4370 (2000).
ghrelin.12 The newly identified 23 amino acid, ghrelin-asso- 14. I.S. Oh, et al., Nature, 443, 709 (2006).
ciated peptide was named obestatin (PGH-3890-PI and PGH- 15. M.A. Cowley and K.L. Grove, Cell Metab., 4, 421 (2006).

3891-PI). Though both peptides originate from the same


precursor prepropeptide, they have opposing physiological
roles.

Peptides International, Inc. P.O. Box 99703 Phone: 502-266-8787 1-800-777-4779


Louisville, KY 40269-0703 USA Fax: 502-267-1329 E-mail: peptides@pepnet.com
CODE FULL-LENGTH GHRELIN and DES GHRELIN PEPTDES QTY
PGH-4372-s Ghrelin (Human) 0.1 mg vial
PGH-3741-PI (Trifluoroacetate Form) 1 mg
Gly-Ser-Ser(n-Octanoyl)-Phe-Leu-Ser-Pro-Glu-His-Gln-Arg-Val-Gln-Gln-Arg-Lys-Glu- 5 mg
Ser-Lys-Lys-Pro-Pro-Ala-Lys-Leu-Gln-Pro-Arg
(M.W. 3370.90 ) C149H249N47O42 [258279-04-8]
Appetite Stimulating Peptide with Energy Homeostasis Regulation
M. Kojima, et al., 402, 656 (1999). (Original) G. Wang, et al., Regul. Pept., 105, 75 (2002). (Review)
C. Dieguez and F.F. Casanueva, Eur. J. Endocrinol., 440, 235 (2002). (Review)

PGH-4373-s Ghrelin (Rat) 0.1 mg vial


(Trifluoroacetate Form)
Gly-Ser-Ser(n-Octanoyl)-Phe-Leu-Ser-Pro-Glu-His-Gln-Lys-Ala-Gln-Gln-Arg-Lys-Glu-
Ser-Lys-Lys-Pro-Pro-Ala-Lys-Leu-Gln-Pro-Arg
(M.W. 3314.80 ) C147H245O45N42
Appetite Stimulating Peptide with Energy Homeostasis Regulation
M. Kojima, et al., Nature, 402, 656 (1999). (Original) G. Muccioli, et al., Eur. J. Pharmacol., 440, 235 (2002).
G. Wang, et al., Regul. Pept., 105, 75 (2002). (Review) C. Dieguez and F.F. Casanueva, Eur. J. Endocrinol., 440, 235 (2002). (Review)

PGH-3653-PI Des-n-Octanoyl-[Ser3]-Ghrelin (Human) 0.5 mg


Non-Acylated Ghrelin (Human)
Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln-Arg-Val-Gln-Gln-Arg-Lys-Glu-Ser-Lys-Lys-
Pro-Pro-Ala-Lys-Leu-Gln-Pro-Arg
(M.W. 3244.74) C141H235N47O41
Counteracts metabolic effects of acylated ghrelin
F. Broglio, et al., J. Clin. Endoc. and Metabolism, 89, 3062 (2004). A. Asakawa, et al., Gut, 54, 18 (2005).
C. Gauna, et al.,, J. Clin. Endoc. and Metabolism, 89, 5035 (2004).

PGH-3654-PI Des-n-Octanoyl-[Ser3]-Ghrelin (Rat) 0.5 mg


Non-Acylated Ghrelin (Rat)
Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln-Lys-Ala-Gln-Gln-Arg-Lys-Glu-Ser-Lys-Lys-Pro-Pro-Ala-Lys-Leu-Gln-Pro-Arg
(M.W. 3188.67) C139H231N45O41
Counteracts metabolic effects of acylated ghrelin
F. Broglio, et al., J. Clin. Endoc. and Metabolism, 89, 3062 (2004). C. Gauna, et al., J. Clin. Endoc. and Metabolism, 89, 5035 (2004).
A. Asakawa, et al., Gut, 54, 18 (2005). H. Hosoda, et al., Biochem. Biophys. Res. Commun., 279, 909 (2000).

GHRELIN RELATED PEPTIDES


PGH-3652-PI [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P 1 mg
D-Arg-Pro-Lys-Pro-D-Phe-Gln-D-Trp-Phe-D-Trp-Leu-Leu-NH2
(M.W. 1516.87) C79H109N14O12
Ghrelin Antagonist / Potent Ghrelin Inverse Agonist / Bombesin Antagonist
P.J. Woll and E. Rozengurt, Proc. Natl. Acad. Sci. USA, 85, 1859 (1988). (Original: Bombesin Antagonist)
B. Holst, et al., Mol. Endocrin., 17, 2201 (2003). (Original: Ghrelin Antagonist)

PGH-3656-PI H-His-D-Trp-D-Lys-Trp-D-Phe-Lys-NH2 1 mg
[D-Lys3]-Growth Hormone Releasing Peptide-6 (GHRP-6) 5 mg
(M.W. 930.13) C49H63N13O6
Ghrelin Antagonist
K. Fujino, et al., J. Physiol., 550, 227 (2003).

PGH-3694-PI H-His-D-Trp-Ala-Trp-D-Phe-Lys-NH2 1 mg
[His1,Lys6]-Growth Hormone Releasing Peptide (GHRP-6) 5 mg
(M.W. 873.04) C46H56N12O6
Growth Hormone Releasing Peptide
C.Y. Bowers, et al., Endocrinol., 114, 1537 (1984).

PGH-3902-PI [Trp3, Arg5]-Ghrelin (1-5) 1 mg


H-Gly-Ser-Trp-Phe-Arg-OH 5 mg
(M.W. 651.73) C31H41N9O7
Growth-Hormone Secretogue (GHS) Receptor Agonist / Stimulates Food-Intake
K. Ohinata, et al., Peptides, 27, 1632 (2006).

PGH-3908-PI H-Lys-d-Trp-Phe-d-Trp-Leu-Leu-NH2
Potent Full Inverse Agonist for Ghrelin Receptor
B. Holst, et al., Mol. Pharmacol., 70, 936 (2006).

PGH-3911-PI H-d-Ala-d-Nal(2)-Ala-Trp-d-Phe-Lys-NH2
GHRP-2 or KP102
Ghrelin agonist growth hormone releasing peptide 2

Peptides International, Inc. P.O. Box 99703 Phone: 502-266-8787 1-800-777-4779


Louisville, KY 40269-0703 USA Fax: 502-267-1329 E-mail: peptides@pepnet.com
CODE GHRELIN ACTIVE FRAGMENTS M.A. Bednarek, et al., J. Med. Chem., 43, 4370 (2000). QTY
PGH-3625-PI Ghrelin (Human, 1-18) 1 mg
H-Gly-Ser-Ser(n-Octanoyl)-Phe-Leu-Ser-Pro-Glu-His-Gln-Arg-Val-Gln-Gln-Arg-Lys-Glu-Ser-NH2 5 mg
(M.W. 225.51) C96H157N31O30
Ghrelin Active Fragment
PGH-3626-PI Ghrelin (Human, 1-14) 1 mg
H-Gly-Ser-Ser(n-Octanoyl)-Phe-Leu-Ser-Pro-Glu-His-Gln-Arg-Val-Gln-Gln-OH 5 mg
(M.W. 1725.94) C76H120N22O24
Ghrelin Active Fragment
PGH-3627-PI Ghrelin (Human, Rat 1-10) 1 mg
H-Gly-Ser-Ser(n-Octanoyl)-Phe-Leu-Ser-Pro-Glu-His-Gln-NH2 5 mg
(M.W. 1213.37) C55H84N14O17
Ghrelin Active Fragment
PGH-3628-PI Ghrelin (Human, Rat, 1-5) 1 mg
H-Gly-Ser-Ser(n-Octanoyl)-Phe-Leu-NH2 5 mg
(M.W. 634.78) C31H50N6O8
Ghrelin Active Fragment

DES GHRELIN FRAGMENTS


PGH-3645-PI Des-n-Octanoyl-[Ser3]-Ghrelin (Human, 1-18) 1 mg
H-Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln-Arg-Val-Gln-Gln-Arg-Lys-Glu-Ser-NH2 5 mg
(M.W. 2099.31) C88H143N31O29
Nonacylated Ghrelin Fragment (Human, 1-18)
PGH-3646-PI Des-n-Octanoyl-[Ser3]-Ghrelin (Human, 1-14) 1 mg
H-Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln-Arg-Val-Gln-Gln-OH 5 mg
(M.W. 1599.74) C68H106N22O23
Nonacylated Ghrelin Fragment (Human, 1-14)
PGH-3647-PI Des-n-Octanoyl-[Ser3]-Ghrelin (Human, Rat, 1-10) 1 mg
H-Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln-NH2 5 mg
(M.W. 1087.172) C47H70N14O16
Nonacylated Ghrelin Fragment (Human, Rat, 1-10)
PGH-3648-PI Des-n-Octanoyl-[Ser3]-Ghrelin (Human, Rat, 1-5) 1 mg
H-Gly-Ser-Ser-Phe-Leu-NH2 5 mg
(M.W. 508.58) C23H36N6O7
Nonacylated Ghrelin Fragment (Human, Rat, 1-5)
CODE (DAP3) GHRELIN ANALOGS M.A. Bednarek, et al., J. Med. Chem., 43, 4370-4376 (2000). QTY
PGH-3681-PI [Dap ]-Ghrelin (Human, Rat, 1-5)
3
1 mg
H-Gly-Ser-Dap(n-Octanoyl)-Phe-Leu-NH2 5 mg
Dap = 2,3-diaminopropionic acid
(M.W. 633.79) C31H51N7O7
Growth-Hormone Releasing Peptide / Ghrelin Analog Active Fragment
PGH-3680-PI [Dap3]-Ghrelin (Rat) 0.5 mg
H-Gly-Ser-Dap(n-Octanoyl)-Phe-Leu-Ser-Pro-Glu-His-Gln-Lys-Ala-Gln-Gln-Arg-Lys-
Glu-Ser-Lys-Lys-Pro-Pro-Ala-Lys-Leu-Gln-Pro-Arg-OH
Dap = 2,3-diaminopropionic acid
(M.W. 3313.88) C147H246N46O41
Growth-Hormone Releasing Peptide / Ghrelin Analog

OBESTATIN J.V. Zhang, et al., Science, 310, 996 (2005).


PGH-3890-PI Obestatin (Human) 1 mg
Human, Monkey 5 mg
H-Phe-Asn-Ala-Pro-Phe-Asp-Val-Gly-Ile-Lys-Leu-Ser-Gly-Val-Gln-Tyr-Gln-Gln-His-Ser-Gln-Ala-Leu-NH2
FNAPFDVGIKLSGVQYQQHSQAL-NH2
(M.W. 2546.89) C116H176N32O33
Suppressor of Food Intake and Gastric Emptying
PGH-4429-s Obestatin (Human) 0.1 mg
Phe-Asn-Ala-Pro-Phe-Asp-Val-Gly-Ile-Lys-Leu-Ser-Gly-Val-Gln-Tyr-Gln-Gln-His-Ser-Gln-Ala-Leu-NH2
(M.W. 2546.8) C116H176N32O33
Food Intake Suppressor / Ligand for GPR39

Peptides International, Inc. P.O. Box 99703 Phone: 502-266-8787 1-800-777-4779


Louisville, KY 40269-0703 USA Fax: 502-267-1329 E-mail: peptides@pepnet.com
OBESTATIN J.V. Zhang, et al., Science, 310, 996 (2005).
PGH-3891-PI Obestatin (Rat, Mouse) 1 mg
H-Phe-Asn-Ala-Pro-Phe-Asp-Val-Gly-Ile-Lys-Leu-Ser-Gly-Ala-Gln-Tyr-Gln-Gln-His- 5 mg
Gly-Arg-Ala-Leu-NH2
FNAPFDVGIKLSGAQYQQHGRAL-NH2
(M.W. 2516.87) C114H174N34O31
Suppressor of Food Intake and Gastric Emptying

PGH-4430-s Obestatin (Rat, Mouse) 0.1 mg


Phe-Asn-Ala-Pro-Phe-Asp-Val-Gly-Ile-Lys-Leu-Ser-Gly-Ala-Gln-Tyr-Gln-Gln-His-
Gly-Arg-Ala-Leu-NH2
(M.W. 2516.8) C114H174N34O31
Food Intake Suppressor / Ligand for GPR39
PGH-3892-PI Des 1-10 Obestatin (Human) 1 mg
Obestatin (Human, 11-23) 5 mg
H-Leu-Ser-Gly-Val-Gln-Tyr-Gln-Gln-His-Ser-Gln-Ala-Leu-NH2
H-LSGVQYQQHSQAL-NH2
(M.W. 1457.62) C63H100N20O20
Truncated Analog of Obestatin
PGH-3893-PI Des 1-10 Obestatin (Rat, Mouse) 1 mg
Obestatin (Rat, Mouse, 11-23) 5 mg
H-Leu-Ser-Gly-Ala-Gln-Tyr-Gln-Gln-His-Gly-Arg-Ala-Leu-NH2
H-LSGAQYQQHGRAL-NH2
(M.W. 1427.60) C61H98N22O18
Truncated Analog of Obestatin
Nesfatins
NES-3863-PI Nesfatin-1 (Human) 0.5 mg
NEFA Encoded Satiety and Fat-influencing Protein 1; Nucleobindin-2 (25-106) (Human); 1 mg
NUCB2 (25-106) (Human); DNA-Binding Protein NEFA (25-106) (Human); Gastric Cancer Antigen Zg4 (25-106) (Human)
H-Val-Pro-Ile-Asp-Ile-Asp-Lys-Thr-Lys-Val-Gln-Asn-Ile-His-Pro-Val-Glu-Ser-Ala-Lys-Ile-Glu-Pro-Pro-Asp-Thr-Gly-Leu-Tyr-
Tyr-Asp-Glu-Tyr-Leu-Lys-Gln-Val-Ile-Asp-Val-Leu-Glu-Thr-Asp-Lys-His-Phe-Arg-Glu-Lys-Leu-Gln-Lys-Ala-Asp-Ile-Glu-Glu-
Ile-Lys-Ser-Gly-Arg-Leu-Ser-Lys-Glu-Leu-Asp-Leu-Val-Ser-His-His-Val-Arg-Thr-Lys-Leu-Asp-Glu-Leu-OH
(M.W. 9551.95) C427H691N113O134
NEFA Encoded Satiety and Fat-Influencing Protein
I.S. Oh, et al., Nature, 443, 709 (2006). M.G.Myers, Jr., Nat Med, 12, 1248 (2006).

NES-3865-PI Nesfatin-1 Like Peptide (Mouse) 0.5 mg


H-Val-Pro-Val-Asp-Arg-Ala-Ala-Pro-Pro-Gln-Glu-Asp-Ser-Gln-Ala-Thr-Glu-Thr-Pro-Asp-Thr-Gly-Leu-Tyr-Tyr- 1 mg
His-Arg-Tyr-Leu-Gln-Glu-Val-Ile-Asn-Val-Leu-Glu-Thr-Asp-Gly-His-Phe-Arg-Glu-Lys-Leu-Gln-Ala-Ala-Asn-Ala-
Glu-Asp-Ile-Lys-Ser-Gly-Lys-Leu-Ser-Gln-Glu-Leu-Asp-Phe-Val-Ser-His-Asn-Val-Arg-Thr-Lys-Leu-Asp-Glu-Leu-OH
(M.W. 8738.67) C382H599N107O128
N. Ramesh, et al., Gen. Comp. Endocrinol., 216, 182 (2015).

NES-3864-PI Nesfatin-1 (Rat) 0.5 mg


NEFA Encoded Satiety and Fat-Influencing Protein 1; Nucleobindin-2 (1-82) (Rat); NUCB2 (1-82) (Rat); 1 mg
DNA-Binding Protein NEFA (1-82) (Rat)
H-Val-Pro-Ile-Asp-Val-Asp-Lys-Thr-Lys-Val-His-Asn-Val-Glu-Pro-Val-Glu-Ser-Ala-Arg-Ile-Glu-Pro-Pro-Asp-Thr-Gly-Leu-Tyr-
Tyr-Asp-Glu-Tyr-Leu-Lys-Gln-Val-Ile-Glu-Val-Leu-Glu-Thr-Asp-Pro-His-Phe-Arg-Glu-Lys-Leu-Gln-Lys-Ala-Asp-Ile-Glu-Glu-
Ile-Arg-Ser-Gly-Arg-Leu-Ser-Gln-Glu-Leu-Asp-Leu-Val-Ser-His-Lys-Val-Arg-Thr-Arg-Leu-Asp-Glu-Leu-OH
(M.W. 9582.88) C424H684N116O136
I.S. Oh, et al., Nature, 443, 709 (2006). M.G.Myers, Jr., Nat Med, 12, 1248 (2006).

NES-3740-PI Nesfatin-1 (30-59) (Human) 1 mg


H-Tyr-Asp-Glu-Tyr-Leu-Lys-Gln-Val-Ile-Asp-Val-Leu-Glu-Thr-Asp- 5 mg
Lys-His-Phe-Arg-Glu-Lys-Leu-Gln-Lys-Ala-Asp-Ile-Glu-Glu-Ile-OH
(M.W. 3709.20) C167H263N41O54
Active Fragment of Nesfatin-1; Anorexigenic Peptide
A.Stengel, et al., Peptides, 35, 143 (2012).
M.Goebel, et al., Peptides, 32, 36 (2011).
M.G.Myers, Jr., Nat. Med., 12, 1248 (2006).
I.S.Oh, et al., Nature, 443, 709 (2006).

Peptides International, Inc. P.O. Box 99703 Phone: 502-266-8787 1-800-777-4779


Louisville, KY 40269-0703 USA Fax: 502-267-1329 E-mail: peptides@pepnet.com

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