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Adipotide (FTPP) Pen

10 mg of the prohibitin-targeted proapoptotic peptidomimetic in 3 mL of bacteriostatic water (0.33% w/v). Filled from a peptide lot tested in the manufacturer’s own laboratory, with a certificate.

CompoundAdipotide FTPP; prohibitin-targeting proapoptotic peptide CKGGRAKDC-GG-D(KLAKLAK)₂
CAS number859216-15-2
Molecular formulaC111H204N36O28S2
Theoretical mass2555.2 Da
Sequence / structureH-CKGGRAKDC-GG-klaklakklaklak-OH (25 residues; Cys1–Cys9 disulfide; lower case = D-amino acids; free N- and C-termini)
ContentsAdipotide: 10 mg per 3 mL pen (0.33% w/v)
FormSterile aqueous solution in bacteriostatic water (0.9% benzyl alcohol), supplied in a 3 mL glass cartridge inside a preloaded autoinjector pen fitted with a needle
Storage, sealedStore at 2–8 °C in the original carton, protected from light
FormatSolution in a 3 mL pre-filled pen

Sizes and lots

  • 10 mg · 1 pen — $99.99
  • 10 mg · Kit of 10 — $993.99

Adipotide (FTPP) is an experimental peptidomimetic that joins a prohibitin-homing motif to a proapoptotic domain made of D-amino acids. Here it is supplied in a preloaded pen: 3 mL of sterile solution in bacteriostatic water carrying 10 mg of peptide, with nothing to reconstitute. Everything published on adipotide comes from cell and animal work on targeting the blood vessels of white fat, including a study in obese monkeys.

What is in the pen

The pen holds a 3 mL glass cartridge of sterile aqueous solution with adipotide at 0.33% w/v, 10 mg in total. That is about 3.3 mg/mL, or roughly 1.3 µmol/mL (1.3 mM) at the theoretical mass of 2555.2 Da. The solvent is bacteriostatic water with 0.9% benzyl alcohol as an antimicrobial preservative. The safety data sheet does not classify adipotide as hazardous; benzyl alcohol carries statements for harm if swallowed or inhaled, serious eye irritation and possible skin sensitisation.

Store the pen at 2 to 8 °C in its original carton, away from light, with the cap on between uses. It must not be frozen, and a pen whose solution has frozen, discoloured or turned cloudy should be thrown away. The Adipotide 5mg vial supplies the same peptide as dry powder, and peptide pen vs vial weighs the two formats against each other.

What the research covers

Adipotide combines two ideas. One is the targeted proapoptotic peptide: a homing domain that carries the molecule to chosen cells, joined to a domain designed to be harmless outside cells but to disrupt mitochondrial membranes once internalised1. Ellerby's original prototypes were aimed at tumour blood vessels and showed anti-cancer activity in mice1. The other is a vascular address for white fat. Kolonin and colleagues found CKGGRAKDC by in vivo phage display, showed that it associates with prohibitin and reported that aiming a proapoptotic peptide at prohibitin in fat vasculature ablated white fat in their model2.

The fullest study is in primates. In obese Old World monkeys, Barnhart and colleagues found targeted apoptosis in white fat blood vessels, lower body weight, improved insulin resistance and less white adipose tissue on imaging, together with predictable and reversible changes in kidney proximal tubule function across three species3. None of these papers reports a human study or used a pre-dissolved solution, and the abstracts give no data on how long adipotide stays intact in bacteriostatic water.

The Adipotide 5mg page carries the full research summary, from the antimicrobial origins of the KLAKLAK sequence to the review literature on targeting fat vasculature.

Frequently asked questions

How is the pen different from the adipotide vial?

The pen arrives ready in solution: 10 mg of adipotide in 3 mL of bacteriostatic water, kept at 2 to 8 °C and never frozen. The vial is 5 mg of dry powder held at −20 °C until the lab dissolves it at a concentration of its own choosing.

What is the concentration?

0.33% w/v, which is 10 mg in 3 mL or about 3.3 mg/mL. With adipotide's theoretical mass of 2555.2 Da, that comes to roughly 1.3 mM, or about 3.9 µmol in the whole pen.

References

  1. Ellerby HM, Arap W, Ellerby LM, et al. Anti-cancer activity of targeted pro-apoptotic peptides. Nat Med. 1999;5(9):1032-8. DOI · PubMed
  2. Kolonin MG, Saha PK, Chan L, et al. Reversal of obesity by targeted ablation of adipose tissue. Nat Med. 2004;10(6):625-32. DOI · PubMed
  3. Barnhart KF, Christianson DR, Hanley PW, et al. A peptidomimetic targeting white fat causes weight loss and improved insulin resistance in obese monkeys. Sci Transl Med. 2011;3(108):108ra112. DOI · PubMed

For laboratory research use only. Not for human or veterinary consumption. Products have not been evaluated by the U.S. Food and Drug Administration and are not intended to diagnose, treat, cure or prevent any disease.