| Description | Gamma-Methylleucine (2-Amino-3-tert-butylpropionic acid) is an auxiliary for copper-catalyzed asymmetric Michael reactions. |
| In vivo | gamma-Methylleucine 提高了肽对Y2R的结合亲和力，同时也增强了其在瘦小鼠中的厌食活性[1]。此外，gamma-Methylleucine 导致ET-1的生物活性丧失或显著降低，而对ETA（IC50=0.42-0.70 nM）和ETB（IC50=0.17-0.43 nM）受体的高亲和力得以保留[2]。研究表明，gamma-Methylleucine 在抵抗由Sarafotoxin S6c引起的兔子肺动脉血管收缩（ET-1: pA2 8.4）方面具有高拮抗活性，并且在任意一种受体亚型上均无激动剂活性，表现出理想的特性[2]。 |
| Synonyms | L-Neopentylglycine, gamma-Methyl-L-leucine, 3-叔丁基-L-丙氨酸, 2-Amino-3-tert-butylpropionic acid |
| molecular weight | 145.2 |
| Molecular formula | C7H15NO2 |
| CAS | 57224-50-7 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: < 1.45 mg/mL (10 mM, insoluble or slightly soluble) |
| References | 1. Naoki Nishizawa, et al. Highly potent antiobesity effect of a short-length peptide YY analog in mice. Bioorg Med Chem. 2017 Oct 15;25(20):5718-5725. 2. Kawato HC, Nakayama K, Inagaki H, Nakajima R, Kitamura A, Someya K, Ohta T. Synthesis and antifungal activity of rhodopeptin analogues. 1. Modification of the east and south amino acid moieties. Org Lett. 2000 Apr 6;2(7):973-6. PubMed PMID: 10768200. 3. Kikuchi T, Kubo K, Ohtaki T, Suzuki N, Asami T, Shimamoto N, Wakimasu M, Fujino M. Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB. J Med Chem. 1993 Dec 10;36(25):4087-93. PubMed PMID: 8258832. 4. Fauchère JL, Petermann C. Synthesis of gamma-methyl-L-leucine (neopentylglycine, Neo) and derivatives suitable for peptide synthesis. Int J Pept Protein Res. 1981 Sep;18(3):249-55. PubMed PMID: 7341518. |