Anamorelin | CAS 249921-19-5 | Ghrelin Receptor Agonist (Research Use Only) | Knowlux

Product Description

Anamorelin, CAS 249921-19-5, is a synthetic, orally active ghrelin receptor (GHSR-1a) agonist supplied by Knowlux for laboratory research use. It is also known by the development codes RC-1291, ONO-7643, and ST-1291. The molecular formula is C31H42N6O3 and the molecular weight is 546.70 g/mol. Each lot is released with a lot-specific COA, MSDS and full analytical traceability.

Regulatory and form clarification: Anamorelin is not approved by the FDA or EMA for any indication. It was approved in Japan in 2021 for cancer cachexia associated with non-small cell lung cancer, making it the first pharmacological treatment approved for this condition globally. The EMA issued a negative opinion, and the FDA rejected the original NDA, primarily due to the failure of handgrip strength to improve as a co-primary endpoint in the ROMANA trials. Ozmosi lists approval status as Not Approved for the US, with approvals noted for Japan and the EMA (negative opinion). Knowlux supplies the free base form explicitly; the hydrochloride salt (CAS 861998-00-7) is a distinct entity. Commercial listings describe anamorelin as a cachexia treatment or appetite stimulant; those designations attach to the approved Japanese pharmaceutical product and do not apply to, and are not represented by, this research-grade lot.

Product Parameters

Product Details

1. Overview

Anamorelin is a synthetic small-molecule ghrelin receptor agonist developed for the management of cancer cachexia and anorexia. Unlike native ghrelin, anamorelin does not require octanoylation for activity and has a longer half-life of approximately 7 hours, supporting once-daily oral dosing. It was investigated in the ROMANA 1 and ROMANA 2 Phase 3 trials in patients with unresectable non-small cell lung cancer and cachexia. Both trials met the lean body mass endpoint (gains of approximately 1.46 kg and 1.63 kg over placebo at 12 weeks), but failed to show statistically significant improvement in handgrip strength, the co-primary endpoint. Japan approved anamorelin in 2021 based on the lean body mass data, while the EMA and FDA did not. Knowlux supplies anamorelin as a research-grade material for laboratory and analytical use; this supply is not intended for human administration and does not constitute a finished drug product.

2. Mechanism of Action (Research Context)

Published research describes anamorelin as a high-affinity, selective ghrelin receptor (GHSR-1a) agonist with an EC50 of 0.74 nM in HEK293/GRLN FLIPR assays. Activation of GHSR-1a mimics the action of endogenous ghrelin, stimulating growth hormone release and increasing serum IGF-1 levels. In cachexia models, this anabolic signalling is thought to counteract the catabolic effects of inflammatory cytokines, promoting appetite and lean body mass preservation. In vitro studies indicate that anamorelin has weak binding affinity for L-type calcium channels, the serotonin transporter, and sodium channels, suggesting high selectivity for the ghrelin receptor. These descriptions are derived from published preclinical and clinical research and are provided for scientific reference only. Knowlux makes no claims regarding the efficacy, safety, or suitability of this product for any human application. Promotion of anamorelin for appetite stimulation, weight gain, cachexia treatment, or any therapeutic indication is not supported by Knowlux and is inconsistent with research-use-only supply.

3. Quality Control

4. Applications

• Reference standard for anamorelin analytical method development

• In vitro GHSR-1a binding and functional assay development

• Ghrelin signalling and growth hormone release research models

• Cancer cachexia and anorexia research models (investigational)

• LC-MS and biochemical assay calibrators

5. Packaging, Storage & Shipping

Powder: amber glass vial or high-barrier foil bag under nitrogen headspace, sealed with tamper-evident closure. Secondary packing: light-protected carton with desiccant. Cold-chain shipping with validated gel packs and temperature logger; dry ice for -20 C shipments. COA, MSDS, packing list and certificate of origin issued with each shipment.

6. Documentation Support

Per lot: COA, MSDS, certificate of origin, residual solvent statement, heavy metal statement, enantiomeric purity report. Specification summaries and audit support available on a project basis.

About Knowlux

Knowlux Biotechnology is a GMP-oriented manufacturer and supplier of peptides, APIs and fine-chemical research compounds, operating from Hubei, China. We serve research groups, CDMOs and distributors in more than 40 countries, and support contract synthesis, custom packaging and technical documentation requests.

Compliance Statement

This product is supplied for laboratory research use only. It is not for human or animal administration, not for diagnostic or therapeutic use, not for retail sale, and not for personal use. Anamorelin is approved in Japan (2021) for cancer cachexia associated with non-small cell lung cancer; it is not approved by the FDA or EMA. That regulatory status is specific to the approved Japanese pharmaceutical product and does not extend to this research-grade supply as sold by Knowlux. Anamorelin carries a GHS classification of H301 (toxic if swallowed); appropriate handling precautions should be observed. Research context statements are for scientific reference only and do not constitute medical advice, promotional claims, or dosing guidance.