Formyl-LHRH (2-10) CAS NO.211376-91-9
<p>Formyl-LHRH (2-10) is a synthetic 9-amino acid peptide fragment, corresponding to residues 2-10 of the Luteinizing Hormone-Releasing Hormone (LHRH or GnRH) sequence, with an N-terminal formyl group modification. This peptide represents a truncated analog of the native decapeptide, lacking the N-terminal pyroglutamate (pGlu1) residue and featuring a formyl group on the new N-terminal histidine. Its structure is: <…
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TECHNICAL SPECIFICATIONS
| Item | Specification |
|---|---|
| Product Name | Formyl-LHRH (2-10) |
| CAS NO. | 11376-91-9 |
| Appearance | White to off-white lyophilized powder |
| Molecular Formula | C51H70N16O12 |
| Molecular Weight | 1099.22g/mol |
| Purity (RP-HPLC) | ≥ 95.0% |
| Solubility | Soluble in water, dilute PBS (pH 7.2-7.4), 0.1% TFA aqueous solution and DMSO. |
| Endotoxin | < 1.0 EU/mg |
| Biological Activity | N-formylated truncated fragment of mammalian LH-RH (2-10); a selective research tool for studying LH-RH receptor binding affinity and structural activity relationships (SAR). |
| Storage Conditions | Store at -20°C to -80°C in a sealed, dry and light-protected container; avoid repeated freeze-thaw cycles. |
| Stock Location | Stock in USA |
| MOQ | 1g |
1.MECHANISM OF ACTION
This truncated analog functions as a ligand for the GnRH Receptor (GnRHR) with significantly altered or diminished biological activity compared to the full-length GnRH. The N-terminal pyroglutamate (pGlu1) of native GnRH is crucial for receptor binding and activation. Its removal in the (2-10) fragment drastically reduces receptor affinity and functional potency. The formyl group at the new N-terminus (His2) is a chemical modification that may slightly influence peptide stability or receptor interaction but does not restore the lost binding energy.
2.PRODUCT INDICATIONS
- Structure-Activity Relationship (SAR) Studies: Used to investigate the critical role of the N-terminal pGlu1 residue in GnRH receptor binding and activation. Comparing its activity to native GnRH and other analogs highlights the importance of specific residues.
- Receptor Binding & Pharmacology: Serving as a low-affinity ligand or potential antagonist in competitive binding assays to study the GnRH receptor's binding site characteristics and to characterize the effects of N-terminal truncation.
Peptide Chemistry & Synthesis: Acting as a reference compound or synthetic intermediate in the chemical synthesis of longer or more complex GnRH analogs, exploring the impact of N-terminal modifications.
3.CLINICAL EFFICACY OF PRODUCT
- Foundation for Drug Design: SAR studies using fragments like this one were historically crucial in mapping the pharmacophore of GnRH. This knowledge directly informed the rational design of potent GnRH agonists (e.g., Leuprolide, Buserelin) and antagonists (e.g., Cetrorelix, Ganirelix), which are cornerstone therapies in medicine.
- Therapeutic Analogs: The clinically used superagonists and antagonists are all full-length or near-full-length analogs with specific modifications to enhance stability and receptor affinity. A truncated fragment like (2-10) lacks the necessary structure for clinical utility.
- Clinical Status: This peptide is not and will not be developed as a drug. Its value is entirely confined to basic science and preclinical research, providing fundamental insights that have already been translated into successful therapeutics targeting the GnRH receptor.
4.DELIVERY & SHIPPING
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