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Research Exemption (Generic) Peptides

O
ver the past two decades, The peptide is a GLP-1 (glucagon like
Please Note: These are FDA-regulated
there have been many pep- products. It is the responsibility of the peptide) agonist and is an insulin secre-
tide drugs approved for customer to ensure that they are complying tagogue with glucoregulatory effects. It
treating a variety of diseases. with Federal rules. Peptides International has been used extensively in treating
Once the product has achieved regula- cannot be liable for infringement of rights type II diabetes in combination with met-
tory approval by having completed and made by the user. formin and pioglitazone.
passed clinical trials determining it to Linaclotide, LIN-3796-PI: This disulfide-rich peptide is an
be safe and effective, it becomes a marketed Brand drug. agonist of gaunylate cyclase 2c. It is currently approved as an
Manufacturers of generic peptide drugs are able to utilize orally delivered treatment for chronic constipation.
the original manufacturers approval provided that they can
show that the generic peptide drug is bioequivalent to the Liraglutide, PGL-3781-PI: This peptide is a long acting GLP-1
approved Brand drug. The generic producer is able to run agonist and is an acylated variant of human GLP-1 (7-37).
their clinical trials, tests and studies on their generic peptide The selective fatty acylation of the peptide increases the
without infringing upon the original manufacturers pat- half life to 11-15 hours following a sub-cutaneous injection
ented drug before the patent has expired by way of the Bolar allowing for once daily injection. This peptide drug has been
exemption in Europe and the UK (including Canada) and widely used to treat type II diabetes.
Merck vs. Integra for the USA. Lixisenatide - Lyxumia, LIX-3799-PI: This peptide is a GLP-1
Some of the most important of these peptide drugs are avail- receptor agonist. Originally discovered by Zealand Pharma,
able from Peptides International and include: it was licensed and developed by Sanofi for its use in the
treatment of Type 2 diabetes. GLP-1 is a natually occuring
Bivalirudin, BIV-3767-PI: This peptide drug is a direct and peptide, released shortly after a meal has been consumed.
reversible thrombin inhibitor. Originally derived from
hiruidin, the salivary anticlot protein found in leeches, this Semaglutide, GLP-3875-PI: We are proud to introduce
20 residue peptide congener inhibits both circulating and research-grade semaglutide. Semaglutide is a glucagon-like
clot bound thrombin as well as inhibiting platelet activation peptide (GLP-1) analogue and a GLP-1 receptor agonist. Not
and aggregation in a highly specific and reversible man- only does it have a half-life of up to one week, it has been
ner. Bivalirudin clinical studies demonstrated consistent used in type 2 diabetes research for its ability to stimulate
positive outcomes in patients with stable angina, unstable insulin production while suppressing glucagon secretion in
angina (UA), non-ST segment elevation myocardial infarc- a glucose-dependent manner. Semaglutide has an increased
tion (NSTEMI). albumin affinity and exhibits a three-fold decrease in GLP-1
receptor affinity when compared to liraglutide.1 Recent stud-
Enfuvirtide, ENF-3787-PI: This 36 residue peptide blocks the ies in patients with Type II Diabetes suggest that semaglu-
entry of the HIV virus by binding to the virus gp41 protein. tide may also have an improved cardiovascular outcome in
This prevents a conformational change in gp41 which is nec- those patients who are at risk for a cardiac event.2
essary for the virus to fuse and form the entry pore for the
capsid of the virus into the CD4+ T-cell, and keeps it from Teduglutide TED-3880-PI: This is a 33 amino acid, glucagon-
entering the cell. This peptide drug has been used success- like peptide-2 (GLP-2) analog, used for the treatment of
fully in HIV patients as part of a combination therapy with short bowel syndrome. It does this by promoting mucosal
protease and reverse transcriptase inhibitors. growth and possibly restoring gastric emptying and secre-
tion. Idiffers from the natural GLP-2 by an alanine that has
Eptifibatide, EPT-3786-PI: Originally derived from a pro- been replaced with a glycine.
tein obtained from the venom of Southeastern Pygmy
Rattlesnake, this cyclic heptapeptide is an anti-platelet drug Tetracosactide - ACTH (Human,1-24) PAC-4109-v: This pep-
which binds to the glycoprotein IIb-IIIa. The drug has a tide drug is derived from the N-terminal 24 amino acids
very short half life and is used to reduce the risk of acute from the naturally occurring peptide hormone ACTH (adre-
cardiac ischemic events in patients with unstable angina nocorticotropin hormone). This peptide hormone induces
or in patients with non-ST-segment elevation myocardial an increase in the levels of circulating glucocorticoids and
infarction. is primarily used as a diagnostic for proper function of the
adrenal glands. It has also been classified as a doping agent
Exenatide - Exendin-4, PEX-3784-PI: This 39 residue peptide or performance enhancing drug (PED) in cycling.
was originally isolated from the saliva of the Gila Monster.

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
continuedfrom front page

Teriparatide - Parathyroid Hormone (Human, 1-34) PTH- stimulating cyclic guanosine monophosphate, leading to
4068-s: This 34 residue parathyroid hormone (PTH 1-34) has smooth muscle cell relaxation.
been used to treat osteoporosis. This peptide is derived from Ziconotide - -Conotoxin MVII-A, PCN-4289-v: This 25
PTH-1-84. PTH 1-34 is the primary regulator of calcium and residue 3 disulfide peptide is a non-opioid, non-NSAID
phosphate metabolism in bone and kidney. PTH increases drug used to treat patients with chronic intractable pain.
calcium levels by stimulating bone resorption. When used Originally derived from the cone snail, Conus magus, this
intermittently, the effect stimulates osteoblasts more than peptide is a potent blocker of N-type Ca+2 channels.
osteoclasts, thereby resulting in new bone formation.
Nesiritide - BNP-32 (Human), PBN-4212-v: This drug is a 32
residue B-type natriuretic peptide. This peptide is normally 1. J. Lau, et al., J. Med. Chem., 58, 7370 (2015).
Retrieved from http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b00726
produced by the ventricular myocardium. Nesiritide works
to facilitate cardiovascular fluid homeostasis through coun- 2. S.P. Marso, et al., N. Engl. J. Med., 375, 1834 (2016).
Retrieved from http://www.nejm.org/doi/full/10.1056/NEJMoa1607141#t=article
ter-regulation of the renin-angiotensin-aldoesterone system,

CODE PRODUCT QTY USD


PAC-4109-v ACTH (Human,1-24) (Tetracosactide) 0.5 mg 275
Adrenocorticotropic Hormone (Human, 1-24) vial
H-SYSMEHFRWGKPVGKKRRPVKVYP-OH
Increases the Circulating Level of Glucocorticoids
BIV-3767-PI Bivalirudin 1 mg 44
H-f PRPGGGGNGDFEEIPEEYL-OH 5 mg 200
Specific, Reversible, Direct Thrombin Inhibitor
C. Michael and G. Mckendall, Am. J. Health-System Pharma., 60, 18 (2003).
TE. Warkentin, Thromb. Haemost., 99, 830, 18 (2010).

PBN-4212-v BNP-32 (Human) 0.5 mg 490


(Nesiritide) vial
B-Type (Brain) Natriuretic Peptide-32 (Human)
H-SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH-OH
(Disulfide bridged)
Cardiac Hormone
PCN-4289-v -Conotoxin MVIIA (Ziconotide) 0.5 mg 375
(Marine Snail, Conus magus) vial
H-CKGKGAKCSRLMYDCCTGSCRSGKC-NH2
(Reported disulfide bonds between Cys1-Cys16, Cys8-Cys20, and Cys15-Cys25)
Reversible N-type Ca2+ Channel Blocker
ENF-3787-PI Enfurirtide 1 mg 110
Ac-YTSLIHSLIEESQNQQEKNEQELLELDK WASLWNWF-NH2 5 mg 450
H.B. Fung and Y.Guo, Clin. Ther., 26, 352 (2004).
R. Manfredi and S. Sabbatani, Curr. Med. Chem., 13, 2369 (2006).

EPT-3786-PI Eptifibatide 1 mg 48
[Mpa-Har-GDWP-C]-NH2 5 mg 150
(Disulfide bridged)
Platelet Aggregation Inhibitor
J.F. Granada and N.S. Kleiman, Am. J. Cardiovasc. Drugs, 4, 31 (2004).
M.P. Curran and G.M. Keating, Biodrugs, 20, 63 (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
Research Exemption (Generic) Peptides
CODE PRODUCT QTY USD
PEX-3784-PI Exendin-4 (Exenatide) 1 mg 450
H-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 5 mg 1800
Glucagon-Like-Peptide-1 (GLP-1) Receptor Agonist
R. Gke, et al., J Biol Chem., 268, 19650 (1993).
B. Thorens, et al., Diabetes, 42, 1678 (1993).
A. Alcntara, et al., Arch. Biochem Biophys, 341, 1, (1997).

LIN-3796-PI Linaclotide 1 mg 625


H-Cys-Cys-Glu-Tyr-Cys-Cys-Asn-Pro-Ala-Cys-Thr-Gly-Cys-Tyr-OH 5 mg 2500
(Disulfide bonds between Cys1-Cys6, Cys2-Cys10, Cys5-Cys13)
(M.W. 1526.76) C59H79N15O21S6 [851199-59-2]
Peptide Agonist of Guanylate Cyclase 2C
W.D. Chey, et al., Am. J. Gastroenterol., 107, 1702 (2012).
S. Rao, et al., Am. J. Gastroenterol., 107, 1714 ((2012).
J.M. Johnston, et al., The Amer. J. of Gastroent., 104, 125 (2009).
A.J. Lembo, et al., N. Eng. J. Med., 365, 527 (2011).
G.F. Longstreth, et al., Gastroenterology, 130, 1480 (2006).

PGL-3781-PI Liraglutide 1 mg 225


Lys(-Glu-palmitoyl)26,Arg34-GLP-1 (7-37) 5 mg 900
H-HAEGTFTSDVSSYLEGQAA-K(-E-palmitoyl)-EFIAWLVRGRG-OH
Glucagon-Like-Peptide-1 (GLP-1) Receptor Agonist
J.J.Neumiller, J. Am. Pharm. Assoc., 49, S16 (2009)
M.C.Rossi and A.Nicolucci, Acta Biomed., 80, 93 (2009)
C.F.Deacon, Vasc. Health Risk Manag., 5, 199 (2009)

LIX-3799-PI Lixisenatide 1 mg 450


H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe- 5 mg 1800
Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-Lys-Lys-Lys-Lys-Lys-Lys-NH2
H-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK-NH2
(M.W. 4858.49) C215H347N61O65S [827033-10-3]
Glucagon-Like-Peptide-1 (GLP-1) Receptor Agonist
M. Christensen, et al., IDrugs, 12, 503 (2009).

PCI-3738-PI Octreotide 1 mg 70
Phe-Cys-Phe-Trp-Lys-Thr-Cys-Thr-ol 5 mg 280
(Disulfide bond between Cys2-Cys7)
(M.W. 1019.24) C49H66N10O10S2 [83150-76-9]
Somatostatin Analog
PTH-4068-v Parathyroid Hormone (Human, 1-34) (Teriparatide) 0.5 mg 370
H-SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF-OH vial
Stimulates Bone Formation & Increases Bone Mineral Density (BMD)

GLU-3875-PI Semaglutide 0.5 mg 225


H-His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys[(AEEA)2--Glu-N-(17-carboxy-1- 1 mg 325
oxoheptadecyl)]-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH
(M.W. 4113.67) C187H291N45O59 [910463-68-2]
Glucagon-Like-Peptide-1 (GLP-1) Receptor Agonist
J. Lau, et al., J. Med. Chem., 58, 7370 (2015). Retrieved from http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b00726
S.P. Marso, et al., N. Engl. J. Med., 375, 1834 (2016). Retrieved from http://www.nejm.org/doi/full/10.1056/NEJMoa1607141#t=article

TED-3880-PI Teduglutide 1 mg 425


(Trifluoroacetate Form) 5 mg 1675
H-His-Gly-Asp-Gly-Ser-Phe-Ser-Asp-Glu-Met-Asn-Thr-Ile-Leu-Asp-Asn-Leu-Ala-Ala-Arg-Asp-Phe-Ile-Asn-Trp-Leu-Ile-Gln-Thr-
Lys-Ile-Thr-Asp-OH
(M.W. 3752.08) C164H252N44O55S [197922-42-2]
Glucagon-like Peptide 2 Analog Used to Treat Short Bowel Syndrome
P. Jeppesen, et al., Gut, 54, 1224 (2005).
P. Jeppesen, Therap. Adv. Gastroenterol., 5, 159 (2012).

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
Research Today.
Cures Tomorrow.

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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