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Histrelin / Studies
Synthetic analog · 9 amino acids · 1,323.5 Da

Histrelin studies and research data

PepBank has 57 histrelin studies with results. 55 of them gave histrelin, with 246 results, grouped by what the studies measured. In each group, results from studies in people come first. Data as of 2026-10-30.

Searches 246 results and 88 papers. Newer studies from Europe PMC

Results in people
181
74% of 246 results
Results in animals
63
26% of 246 results
Results in lab cells
2
under 1% of 246 results
From computer models
0
0% of 246 results
The molecule

Histrelin identity

Identifiers, parent molecule, targets and development stage, from curated data.

Histrelin is a synthetic nine-residue GnRH agonist analog. Supprelin LA contains histrelin acetate and treats children with central precocious puberty. Vantas contains histrelin acetate and has a US label for palliative treatment of advanced prostate cancer. These implants have distinct release specifications.

Kind
Synthetic analog · 9 residues
Identifiers
ChEMBLCHEMBL1201255 (opens in a new tab)PubChem CID25077993 (opens in a new tab)UNIIH50H3S3W74 (opens in a new tab)DrugBankDB06788 (opens in a new tab)CAS76712-82-8
Parent
Analog of GonadorelinHistrelin is a synthetic GnRH analog. Compared with mature human gonadorelin, it replaces Gly6 with 1-benzyl-D-His and omits Gly10. Pro9 has an N-ethylamide terminus. UniProt P01148 identifies the human precursor, not histrelin itself. No direct precursor slice represents this modified analog.
Development
Approved in the US and EU (Supprelin LA)Approved histrelin acetate implant products exist. This status does not apply to every formulation or indication. Current commercial availability was not established. Source (opens in a new tab)

Targets

Molecular targets with action and evidence source
TargetActionEvidence
Gonadotropin-releasing hormone receptorGNRHRP30968 (opens in a new tab)AgonistOfficial prescribing information, mechanism of actionSource (opens in a new tab)

Sequence and structure

Residues, differences from the parent, calculated properties and 3D structure. Source values and calculated values are shown separately.

Sequence

9 amino acids · 2 modifications

Residues 1 to 9:
HWSYLRP
  • HydrophobicA V I L M
  • AromaticF W Y
  • PositiveK R H
  • PolarS T N Q
  • SpecialC G P
  • Non-canonicalX
  • Modified residue

Modifications

Residue 1
Other modification
L-pyroglutamate at the N-terminus.
Residue 6
Non-canonical residue
D-histidine with benzyl substitution on the imidazole nitrogen (Nt, also designated 1-benzyl).

Alignment to Gonadorelin

Calculated from the two sequences. Curated notes are shown as given.

7 of 9 aligned residues identical (78%) · 2 non-canonical residues · Gonadorelin 1–9

  • Top row: Gonadorelin (parent)
  • Bottom row: Histrelin
HWSYLRP
  • Same as parent
  • Substituted
  • Non-canonical or D-form
  • Added
  • Gap
  • Modified side chain or end
  • Parent context

Differences from the parent

  1. 1Parent 1 · analog 1Xaa → Xaa · Non-canonical residueL-pyroglutamate at the N-terminus.
  2. 2Parent 6 · analog 6Gly → Xaa · Non-canonical residueD-histidine with benzyl substitution on the imidazole nitrogen (Nt, also designated 1-benzyl).

Basis: Histrelin is a synthetic GnRH analog. Compared with mature human gonadorelin, it replaces Gly6 with 1-benzyl-D-His and omits Gly10. Pro9 has an N-ethylamide terminus. UniProt P01148 identifies the human precursor, not histrelin itself. No direct precursor slice represents this modified analog.

Calculated from the two sequences with @pepdb/chem alignToParent (ungapped unless a gap scores higher). The record’s curated notes are shown as given.

Properties

From identity sources

Formula
C66H86N18O12
Molecular weight
1,323.5 g/mol
Monoisotopic mass
1,322.6673 Da

Calculated from the sequence

Some values cannot be calculated. The sequence has a non-canonical residue (X). Residue tables cover only the 20 standard amino acids.

Average mass
Not calculated
Monoisotopic mass
Not calculated
Isoelectric point (pI)
Not calculated
Net charge at pH 7.4
Not calculated
GRAVY (hydropathy)
Not calculated
Extinction coefficient, 280 nm (Cys reduced)
6,990 M⁻¹ cm⁻¹
5500 x Trp + 1490 x Tyr · Pace et al. 1995 (ExPASy ProtParam)
Instability index
Not calculated
Aliphatic index
Not calculated
Boman index
Not calculated
Hydrophobic moment (μH)
Not calculated
  • 2 non-canonical residues (X) are not included in calculated values.
  • Not included: other modification. Mass, charge and pI are not calculated; use the identity-source values.
  • The N-terminal group is not modeled.
  • The C-terminal group is not modeled.
  • Defined and validated for proteins; use with care for short peptides.
  • Assumes an ideal alpha helix. Many short peptides are not helical.

@pepdb/chem 0.2.0 · EMBOSS pKa set · ExPASy residue masses

Net charge by pH

No charge curve

The sequence has a non-canonical residue (X). Residue tables cover only the 20 standard amino acids.

Composition

  • Hydrophobic11% (1)
  • Aromatic22% (2)
  • Positive22% (2)
  • Polar11% (1)
  • Special11% (1)
  • Non-canonical22% (2)

9 residues. Each residue counts in one class; F and W count as aromatic.

A Ala0 · 0%
I Ile0 · 0%
L Leu1 · 11%
M Met0 · 0%
V Val0 · 0%
F Phe0 · 0%
W Trp1 · 11%
Y Tyr1 · 11%
H His1 · 11%
K Lys0 · 0%
R Arg1 · 11%
D Asp0 · 0%
E Glu0 · 0%
N Asn0 · 0%
Q Gln0 · 0%
S Ser1 · 11%
T Thr0 · 0%
C Cys0 · 0%
G Gly0 · 0%
P Pro1 · 11%
X Xaa2 · 22%

3D structure

PredictedAlphaFold DB · P01148

Loads the 3D viewer (3Dmol.js, about 150 KB) and the model file from AlphaFold DB (EMBL-EBI).

  • Very high (pLDDT > 90)
  • Confident (90 > pLDDT > 70)
  • Low (70 > pLDDT > 50)
  • Very low (pLDDT < 50)

Predicted model of the whole UniProt entry P01148, not an experimental structure of Histrelin.

AlphaFold DB, EMBL-EBI and Google DeepMind · CC BY 4.0

2D structure

Draws the structure in your browser with RDKit (about 2.3 MB, loaded once).

SMILES fromPubChem CID 25077993(opens in a new tab)

CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC2=CN(C=N2)CC3=CC=CC=C3)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CNC6=CC=CC=C65)NC(=O)[C@H](CC7=CN=CN7)NC(=O)[C@@H]8CCC(=O)N8
Results by area

What the studies measured

People first in each area, then animals, then lab cells. Counts are exact and come from studies that gave the peptide.

Trials and papers
Status and safety
Data