CJC-1295 with DAC

An albumin-binding 30-residue synthetic peptide corresponding to a tetrasubstituted GRF(1-29) sequence, studied in class B GPCR structural pharmacology and albumin-conjugation chemistry.

Molecular Profile

Type
Synthetic peptide (tetrasubstituted GRF(1-29) sequence, 30 residues, with an albumin-binding DAC group)
Molecular formula
C165H269N47O46
Molecular weight
~3,647 g/mol
CAS number
863288-34-0
Amino acids
30
Sequence
H-Tyr-D-Ala-Asp-Ala-Ile-Phe-Thr-Gln-Ser-Tyr-Arg-Lys-Val-Leu-Ala-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Leu-Ser-Arg-Lys-NH2 (Nε-3-maleimidopropionyl on the C-terminal Lys30)
Modification
Four substitutions relative to GRF(1-29) — D-Ala2, Gln8, Ala15, Leu27 — conferring resistance to dipeptidyl peptidase-4 and other plasma proteases; C-terminal amidation; and an Nε-3-maleimidopropionyl-Lys30 (DAC) linker whose maleimide forms a covalent thioether bond with cysteine-34 of serum albumin.

Mechanism & Target Class

A 30-residue synthetic peptide corresponding to a tetrasubstituted GRF(1-29) sequence — an N-terminal fragment analog of a 44-residue hypothalamic peptide. Class B / secretin-family GPCRs of this family comprise an extracellular domain and a seven-transmembrane bundle, and cryo-EM studies of the family resolve the canonical two-domain binding mode in which the peptide N-terminus inserts into the transmembrane bundle while the C-terminal segment is held by the extracellular domain. Two structural features distinguish the molecule: a tetrasubstituted GRF(1-29) backbone (D-Ala2, Gln8, Ala15, Leu27) that resists protease cleavage, and a Drug Affinity Complex — an Nε-maleimidopropionyl-lysine appended at the C-terminus whose maleimide reacts with the free thiol on cysteine-34 of serum albumin, converting the peptide into a long-circulating albumin conjugate.

Storage & Handling

Lyophilized
-20°C; protected from light and moisture; frozen for longer-term storage.
Handling
As a peptide, susceptible to degradation from heat, light, moisture, and repeated freeze-thaw. The DAC maleimide group is thiol-reactive. Research-use-only; not for human or veterinary use.

Primary Database

PubChem CID 91971820 ↗

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