α-Galactosylceramide(Synonyms: α-GalCer; KRN7000)

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α-Galactosylceramide (Synonyms: α-GalCer; KRN7000) 纯度: 95.51%

α-Galactosylceramide (α-GalCer) 是一种合成的糖脂,具有抗肿瘤和免疫刺激作用。α-Galactosylceramide 是一种非常有效的 NKT 细胞激动剂,可与 CD1d 有效结合。α-Galactosylceramide 与 CD1d 的复合物可与 NKT 细胞的 T 细胞抗原受体结合。

α-Galactosylceramide(Synonyms: α-GalCer;  KRN7000)

α-Galactosylceramide Chemical Structure

CAS No. : 158021-47-7

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生物活性

α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor)[1][2][3][4].

IC50 & Target

NKT cell[3]

体外研究
(In Vitro)

Culture supernatants of activated Vα24+NKT-cell cultures stimulated with α-Galactosylceramide pulsed monocyte-derived dendritic cells (Mo-DCs) exhibits antiproliferative activities against melanoma cells. This effect is predominantly due to release of IFN-γ, and to a lesser extent IL-12. Other cytokines, including IL-4 and IL-10, are released but these cytokines have less antiproliferative effects. Vα24+NKT-cells stimulated by α-Galactosylceramide-pulsed Mo-DCs have anti-tumour activities against human melanoma through antiproliferative effects exerted by soluble mediators[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

α-Galactosylceramide treatment can protect against spontaneous, carcinogen-, or oncogene-induced primary tumor formation in mice. Consistent with a prime role for IFN-γ in NKT cell-mediated tumor responses, a C-glycoside analog of α-Galactosylceramide that preferentially stimulated IFN-γ production is even more effective than α-Galactosylceramide at preventing metastases of the B16 melanoma[1].
Since α-Galactosylceramide shows a potent antitumor activity and stimulates the lymphocyte proliferation (LP) on allogeneic mixed lymphocyte reaction (MLR) in the mouse, α-Galactosylceramide is considered to be a nonspecific immunostimulating agent which is a biological response modifier[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

858.34

Formula

C15H29NO9

CAS 号

158021-47-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 0.5 mg/mL (0.58 mM; ultrasonic and warming and heat to 60°C)

参考文献
  • [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.

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