CAS 2381089-83-2 | Retatrutide
Name: Retatrutide
CAS number: 2381089-83-2
Molecular formula:
Molecular weight:
EINECS number: 200-001-8
MDL No.：
Application:
| Application Category | Detailed Uses & Mechanisms | Clinical/Industrial Significance |
|---|---|---|
| Type 2 Diabetes Mellitus (T2D) Treatment | Triple agonist of GLP-1R, GIPR, GCGR; glucose‑dependent insulin secretion; suppresses glucagon; delays gastric emptying; lowers fasting/postprandial glucose; reduces HbA1c | First‑line candidate for T2D; superior glycemic control vs. single agonists |
| Obesity & Weight Management | Reduces appetite (GLP‑1R/GIPR); increases energy expenditure (GCGR); promotes fat breakdown | Phase II: up to 24.2% weight loss in 52 weeks (12 mg weekly) |
| Metabolic Syndrome & NAFLD | Improves insulin sensitivity; reduces liver fat; lowers cardiovascular risk factors | Emerging indication for non‑alcoholic fatty liver disease |
| Pharmaceutical R&D Tool | In vitro/in vivo model for triple receptor agonism; drug discovery for metabolic disorders | Standard reference compound for preclinical studies |
| API & Formulation Intermediate | Active pharmaceutical ingredient for injectable formulations; bulk peptide for drug product manufacturing | High‑purity (≥98–99%) material for clinical trials & commercial production |
Intermediates:
| Intermediate Name | CAS No. | Role in Retatrutide Production |
|---|---|---|
| Fmoc‑L‑Lys[C20‑OtBu‑Glu(OtBu)‑AEEA]‑OH (Side Chain) | 2612237‑97‑3 | lipidated side chain for prolonged half‑life; core building block |
|
Peptide Fragment 1 (7–14 aa): Fmoc‑Phe‑Thr‑Ser‑ Asp‑Tyr‑Ser‑Ile‑αMeLeu‑Leu‑NH₂ |
N/A | N‑terminal fragment for solid‑phase peptide synthesis (SPPS) |
|
Peptide Fragment 2 (15–29 aa): Fmoc‑Gln‑Gly‑Thr‑Phe‑Thr‑Ser‑Asp‑Tyr‑Ser‑Ile‑ αMeLeu‑Leu‑Gln‑Aib‑Tyr‑Leu‑NH₂ |
N/A | Mid‑chain fragment assembled via fragment condensation |
| Peptide Fragment 3 (30–39 aa): Fmoc‑Asp‑Lys‑Gln‑Ala‑Aib‑Glu‑Phe‑Ile‑Ala‑Trp‑NH₂ | N/A | C‑terminal fragment coupled to full‑length peptide backbone |
| Fmoc‑α‑Aminoisobutyric Acid (Fmoc‑Aib‑OH) | 37478‑74‑5 | Stabilizes peptide conformation; critical for receptor agonism |
| Fmoc‑L‑Glutamic Acid γ‑tert‑Butyl Ester (Fmoc‑Glu(OtBu)‑OH) | 147292‑62‑5 | Side‑chain protecting group for Glu residues; enables selective deprotection |
| Fmoc‑L‑Lysine ε‑tert‑Butyl Ester (Fmoc‑Lys(OtBu)‑OH) | 71989‑26‑9 | Protects Lys side chain during SPPS; essential for side‑chain conjugation |
| 2‑Chlorotrityl Chloride Resin (2‑CTC Resin) | 65428‑43‑9 | Solid support for SPPS; allows mild cleavage of peptide‑resin bonds |
| Coupling Reagents: Oxyma, DIC, TPTU, DIEA | N/A | Activate amino acids for amide bond formation; minimize racemization |
| Cleavage Reagents: TFA, TIS, H₂O | N/A | Remove protecting groups and cleave peptide from resin |
Synonyms:
L-tyrosyl-2-methylalanyl-L-glutaminylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-alpha -aspartyl-L-tyrosyl-L-seryl-L-isoleucyl-2-methyl-L-leucyl-Lleucyl-L-alpha -aspartyl-L-lysyl-N6-(N-(19-carboxy-1-oxononadecyl)-L-gamma-glutamyl-2-(2-(2-aminoethoxy)ethoxy)acetyl)-L-lysyl-L-alanyl-L-glutaminyl-2-methylalanyl-L-alanyl-Lphenylalanyl-L-isoleucyl-L-alpha -glutamyl-L-tyrosyl-L-leucyl-L-leucyl-L-alpha -glutamylglycylglycyl-L-prolyl-L-seryl-L-serylglycyl-L-alanyl-L-prolyl-L-prolyl-L-prolyl-L-serinamide
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