| Description | α-Galactosylceramide (KRN7000) is a synthetic glycolipid with antitumorial and immunostimulatory and is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide and CD1d can bind to the T cell antigen receptor of NKT cells. |
| In vitro | 使用α-Galactosylceramide脉冲的单核来源树突细胞(Mo-DC)刺激活化的Vα24+ NKT细胞培养可以对抗黑素瘤细胞的增殖。通过可溶性介质刺激的Vα24+ NKT细胞对人类黑素瘤表现出抗肿瘤活性，这种效应主要是由于释放IFN-γ，以及在较小程度上，释放IL-12。虽然还会释放包括IL-4和IL-10在内的其他细胞因子，但这些细胞因子对抗增殖的效果较弱。 |
| In vivo | α-Galactosylceramide处理能预防小鼠中自发的、癌基因或癌基因诱导的原发性肿瘤形成。与NKT细胞介导的肿瘤反应中IFN-γ的主要作用一致，优先刺激IFN-γ产生的α-Galactosylceramide的C-糖苷类似物比α-半乳糖更有效地防止了B16黑色素瘤的转移。Ceramides的效果更佳[1]。α-Galactosylceramide展示了强大的抗肿瘤活性，并在小鼠同种异体混合淋巴细胞反应(MLR)[4]中刺激了淋巴细胞增殖(LP)。 |
| Synonyms | KRN7000, α-GalCer |
| molecular weight | 858.32 |
| Molecular formula | C50H99NO9 |
| CAS | 158021-47-7 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 1 mg/mL (1.17 mM), Sonication and heating to 80℃ are recommended. |
| References | 1. Godfrey DI, et al. Going both ways: immune regulation via CD1d-dependent NKT cells. J Clin Invest. 2004 Nov;114(10):1379-88. 2. Morita M, et al. Practical Total Synthesis of (2S,3S,4R)-1-O-(α-D-Galactopyranosyl)-N-hexacosanoyl-2-amino-1,3,4-octadecanetriol, the Antitumorial and Immunostimulatory α-Galactosylcer-amide, KRN7000. Biosci Biotechnol Biochem. 1996 Jan;60(2):288-92. 3. Kikuchi A, et al. In vitro anti-tumour activity of alpha-galactosylceramide-stimulated human invariant Valpha24+NKT cells against melanoma. Br J Cancer. 2001 Sep 1;85(5):741-6. 4. Masahiro Morita, et al. Structure-Activity Relationship of .alpha.-Galactosylceramides against B16-Bearing Mice. J. Med. Chem. 1995, 38, 12, 2176-2187. |