Somatostatin
H01C - Hypothalamic hormones
ATC H01CB01
Protein
Natural product
JFDA label: Somatostatin-UCB Vial
Mechanism of Action
Agonist of Somatostatin receptor — Somatostatin receptor agonist
| Target | Action | Gene / class |
|---|---|---|
| Somatostatin receptor efficacy | AGONIST |
Indications
Off-label
- Carcinoid Tumor
- Carcinoma, Hepatocellular
- Diabetes Mellitus, Type 1
- Digestive System Diseases
- Gallbladder Neoplasms
- Hypertension, Portal
- Liver Failure
- Neuroendocrine Tumors
- Pancreatitis
- Peptic Ulcer
- Polycystic Kidney, Autosomal Dominant
Chemistry & Properties
| Formula | C76H104N18O19S2 |
|---|---|
| Molecular weight | 1637.91 g/mol |
| IUPAC name | (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-37-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid |
| CAS | 38916-34-6 |
| PubChem CID | 16129706 |
| InChIKey | NHXLMOGPVYXJNR-ATOGVRKGSA-N |
SMILES
C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=OBiology & Pharmacokinetics
Pharmacokinetics predicted
| Bioavailability | 70.0% |
|---|---|
| Half-life | 3.281 h |
| Volume of distribution | 0.285 L/kg |
| Protein binding | 2.2% |
| BBB penetrant | No |
Receptor binding (top 5)
| Target | Action | Affinity |
|---|---|---|
| SOMATOSTATIN SST2 (SSTR2) | Binding | pKi 10.0 |
| SOMATOSTATIN SST3 (SSTR3) | Binding | pKi 9.4 |
| SOMATOSTATIN SST5 (SSTR5) | Binding | pKi 9.4 |
| SOMATOSTATIN SST1 (SSTR1) | Binding | pKi 9.2 |
| SOMATOSTATIN SST4 (SSTR4) | Binding | pKi 8.9 |
Transporters
BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)
Registered Products (2)
| Brand | Form / strength | Pack | Agent | Citizen (JOD) |
|---|---|---|---|---|
| Somatostatin-UCB Vial | Vial 0.25 mg | 1 amp | ORIENT DRUG STORE CO | 11.780 |
| Somatostatin-UCB Vial | Vial 3 mg | 1 amp | ORIENT DRUG STORE CO | 105.440 |