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Research Exemption (Generic) Peptides O ver the past two decades, there have been many pep-
Research Exemption (Generic) Peptides O ver the past two decades, there have been many pep-
Research Exemption (Generic) Peptides O ver the past two decades, there have been many pep-

Research Exemption (Generic) Peptides

O ver the past two decades,

there have been many pep-

tide drugs approved for

treating a variety of diseases.

Please Note: These are FDA-regulated products. It is the responsibility of the customer to ensure that they are complying with Federal rules. Peptides International cannot be liable for infringement of rights made by the user.

The peptide is a GLP-1 (glucagon like peptide) agonist and is an insulin secre- tagogue with glucoregulatory effects. It has been used extensively in treating type II diabetes in combination with met- formin and pioglitazone.

Linaclotide, LIN-3796-PI: This disulfide-rich peptide is an agonist of gaunylate cyclase 2c. It is currently approved as an orally delivered treatment for chronic constipation.

Liraglutide, PGL-3781-PI: This peptide is a long acting GLP-1 agonist and is an acylated variant of human GLP-1 (7-37). The selective fatty acylation of the peptide increases the half life to 11-15 hours following a sub-cutaneous injection allowing for once daily injection. This peptide drug has been widely used to treat type II diabetes.

Lixisenatide - Lyxumia, LIX-3799-PI: This peptide is a GLP-1 receptor agonist. Originally discovered by Zealand Pharma, it was licensed and developed by Sanofi for its use in the treatment of Type 2 diabetes. GLP-1 is a natually occuring peptide, released shortly after a meal has been consumed.

Semaglutide, GLP-3875-PI: We are proud to introduce research-grade semaglutide. Semaglutide is a glucagon-like peptide (GLP-1) analogue and a GLP-1 receptor agonist. Not only does it have a half-life of up to one week, it has been used in type 2 diabetes research for its ability to stimulate insulin production while suppressing glucagon secretion in a glucose-dependent manner. Semaglutide has an increased albumin affinity and exhibits a three-fold decrease in GLP-1 receptor affinity when compared to liraglutide. 1 Recent stud- ies in patients with Type II Diabetes suggest that semaglu- tide may also have an improved cardiovascular outcome in those patients who are at risk for a cardiac event. 2

Teduglutide TED-3880-PI: This is a 33 amino acid, glucagon- like peptide-2 (GLP-2) analog, used for the treatment of short bowel syndrome. It does this by promoting mucosal growth and possibly restoring gastric emptying and secre- tion. Idiffers from the natural GLP-2 by an alanine that has been replaced with a glycine.

Tetracosactide - ACTH (Human,1-24) PAC-4109-v: This pep- tide drug is derived from the N-terminal 24 amino acids from the naturally occurring peptide hormone ACTH (adre- nocorticotropin hormone). This peptide hormone induces an increase in the levels of circulating glucocorticoids and is primarily used as a diagnostic for proper function of the adrenal glands. It has also been classified as a doping agent or performance enhancing drug (PED) in cycling.

Once the product has achieved regula- tory approval by having completed and

passed clinical trials determining it to be safe and effective, it becomes a marketed Brand drug. Manufacturers of generic peptide drugs are able to utilize the original manufacturer’s approval provided that they can show that the generic peptide drug is bioequivalent to the approved Brand drug. The generic producer is able to run their clinical trials, tests and studies on their generic peptide without infringing upon the original manufacturer’s pat- ented drug before the patent has expired by way of the Bolar exemption in Europe and the UK (including Canada) and Merck vs. Integra for the USA.

Some of the most important of these peptide drugs are avail- able from Peptides International and include:

Bivalirudin, BIV-3767-PI: This peptide drug is a direct and reversible thrombin inhibitor. Originally derived from hiruidin, the salivary anticlot protein found in leeches, this 20 residue peptide congener inhibits both circulating and clot bound thrombin as well as inhibiting platelet activation and aggregation in a highly specific and reversible man- ner. Bivalirudin clinical studies demonstrated consistent positive outcomes in patients with stable angina, unstable angina (UA), non-ST segment elevation myocardial infarc- tion (NSTEMI).

Enfuvirtide, ENF-3787-PI: This 36 residue peptide blocks the entry of the HIV virus by binding to the virus gp41 protein. This prevents a conformational change in gp41 which is nec- 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 entering the cell. This peptide drug has been used success- fully in HIV patients as part of a combination therapy with protease and reverse transcriptase inhibitors.

Eptifibatide, EPT-3786-PI: Originally derived from a pro- tein obtained from the venom of Southeastern Pygmy Rattlesnake, this cyclic heptapeptide is an anti-platelet drug which binds to the glycoprotein IIb-IIIa. The drug has a very short half life and is used to reduce the risk of acute cardiac ischemic events in patients with unstable angina or in patients with non-ST-segment elevation myocardial infarction.

Exenatide - Exendin-4, PEX-3784-PI: This 39 residue peptide was originally isolated from the saliva of the Gila Monster.

Peptides International, Inc. P.O. Box 99703 Louisville, KY 40269-0703 USA Phone: 502-266-8787 1-800-777-4779 Fax:
Peptides International, Inc.
P.O. Box 99703
Louisville, KY 40269-0703 USA
Phone: 502-266-8787
1-800-777-4779
Fax: 502-267-1329
E-mail: peptides@pepnet.com
continuedfrom front page Teriparatide - Parathyroid Hormone (Human, 1-34) PTH- 4068-s : This 34 residue

continuedfrom front page

Teriparatide - Parathyroid Hormone (Human, 1-34) PTH- 4068-s: This 34 residue parathyroid hormone (PTH 1-34) has been used to treat osteoporosis. This peptide is derived from PTH-1-84. PTH 1-34 is the primary regulator of calcium and phosphate metabolism in bone and kidney. PTH increases calcium levels by stimulating bone resorption. When used intermittently, the effect stimulates osteoblasts more than 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 produced by the ventricular myocardium. Nesiritide works to facilitate cardiovascular fluid homeostasis through coun- ter-regulation of the renin-angiotensin-aldoesterone system,

stimulating cyclic guanosine monophosphate, leading to smooth muscle cell relaxation.

Ziconotide - ω-Conotoxin MVII-A, PCN-4289-v: This 25 residue 3 disulfide peptide is a non-opioid, non-NSAID drug used to treat patients with chronic intractable pain. Originally derived from the cone snail, Conus magus, this peptide is a potent blocker of N-type Ca +2 channels.

1. J. Lau, et al., J. Med. Chem., 58, 7370 (2015). Retrieved from http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b00726

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

CODE

PRODUCT

QTY

USD

PAC-4109-v

ACTH (Human,1-24) (Tetracosactide) Adrenocorticotropic Hormone (Human, 1-24) H-SYSMEHFRWGKPVGKKRRPVKVYP-OH Increases the Circulating Level of Glucocorticoids

0.5

mg

275

vial

BIV-3767-PI

Bivalirudin H-f PRPGGGGNGDFEEIPEEYL-OH Specific, Reversible, Direct Thrombin Inhibitor

C.

Michael and G. Mckendall, Am. J. Health-System Pharma., 60, 18 (2003).

 

1

mg

44

5

mg

200

 

TE. Warkentin, Thromb. Haemost., 99, 830, 18 (2010).

PBN-4212-v

BNP-32 (Human) (Nesiritide) B-Type (Brain) Natriuretic Peptide-32 (Human) H-SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH-OH (Disulfide bridged) Cardiac Hormone

0.5

mg

490

vial

PCN-4289-v

ω-Conotoxin MVIIA (Ziconotide) (Marine Snail, Conus magus) H-CKGKGAKCSRLMYDCCTGSCRSGKC-NH 2 (Reported disulfide bonds between Cys 1 -Cys 16 , Cys 8 -Cys 20 , and Cys 15 -Cys 25 ) Reversible N-type Ca 2+ Channel Blocker

0.5

mg

375

vial

ENF-3787-PI

Enfurirtide Ac-YTSLIHSLIEESQNQQEKNEQELLELDK WASLWNWF-NH 2

1

mg

110

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 [Mpa-Har-GDWP-C]-NH 2 (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).

1

mg

48

5

mg

150

 
Peptides International, Inc. P.O. Box 99703 Louisville, KY 40269-0703 USA Phone: 502-266-8787 1-800-777-4779 Fax:
Peptides International, Inc.
P.O. Box 99703
Louisville, KY 40269-0703 USA
Phone: 502-266-8787
1-800-777-4779
Fax: 502-267-1329
E-mail: peptides@pepnet.com

Research Exemption (Generic) Peptides

CODE

PRODUCT

QTY

USD

PEX-3784-PI

Exendin-4 (Exenatide) H-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2 Glucagon-Like-Peptide-1 (GLP-1) Receptor Agonist

R.

Göke, et al., J Biol Chem., 268, 19650 (1993).

1

mg

450

5

mg

1800

 

B.

Thorens, et al., Diabetes, 42, 1678 (1993).

A.

Alcántara, et al., Arch. Biochem Biophys, 341, 1, (1997).

 

LIN-3796-PI

Linaclotide H-Cys-Cys-Glu-Tyr-Cys-Cys-Asn-Pro-Ala-Cys-Thr-Gly-Cys-Tyr-OH (Disulfide bonds between Cys 1 -Cys 6 , Cys 2 -Cys 10 , Cys 5 -Cys 13 ) (M.W. 1526.76) C 59 H 79 N 15 O 21 S 6 [851199-59-2] Peptide Agonist of Guanylate Cyclase 2C

W.D. Chey, et al., Am. J. Gastroenterol., 107, 1702 (2012).

1

mg

625

5

mg

2500

 

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 Lys(γ-Glu-palmitoyl) 26 ,Arg 34 -GLP-1 (7-37) H-HAEGTFTSDVSSYLEGQAA-K(γ-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)

1

mg

225

5

mg

900

 

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-NH 2

 

H-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK-NH 2

(M.W. 4858.49) C 215 H 347 N 61 O 65 S

[827033-10-3]

Glucagon-Like-Peptide-1 (GLP-1) Receptor Agonist

 

M.

Christensen, et al., IDrugs, 12, 503 (2009).

PCI-3738-PI

Octreotide Phe-Cys-Phe-Trp-Lys-Thr-Cys-Thr-ol (Disulfide bond between Cys 2 -Cys 7 )

(M.W. 1019.24) C 49 H 66 N 10 O 10 S 2 Somatostatin Analog

[83150-76-9]

 

1

mg

70

5

mg

280

 

PTH-4068-v

Parathyroid Hormone (Human, 1-34) (Teriparatide) H-SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF-OH Stimulates Bone Formation & Increases Bone Mineral Density (BMD)

0.5

mg

370

vial

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-γ-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) C 187 H 291 N 45 O 59

[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) C 164 H 252 N 44 O 55 S

[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 Louisville, KY 40269-0703 USA Phone: 502-266-8787 1-800-777-4779 Fax:
Peptides International, Inc.
P.O. Box 99703
Louisville, KY 40269-0703 USA
Phone: 502-266-8787
1-800-777-4779
Fax: 502-267-1329
E-mail: peptides@pepnet.com

Research Today. Cures Tomorrow.

Peptides International, Inc. P.O. Box 99703 Louisville, KY 40269-0703 USA Phone: 502-266-8787 1-800-777-4779 Fax:
Peptides International, Inc.
P.O. Box 99703
Louisville, KY 40269-0703 USA
Phone: 502-266-8787
1-800-777-4779
Fax: 502-267-1329
E-mail: peptides@pepnet.com

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