环孢菌素 D

环孢菌素 D用途

Cyclosporin D 是 Cyclosporin A 的代谢产物,是一种弱免疫抑制剂。Cyclosporin D 作为 Cyclosporin A 定量的内标,Cyclosporin A 是一种免疫抑制药物,通过抑制钙调磷酸酶和钙调磷酸酶依赖性转录因子激活的T细胞核因子 (NFAc) 来抑制 T 细胞活化。

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环孢菌素 D名称

[ CAS 号 ]:
63775-96-2

[ 中文名 ]:
环孢菌素 D

[ 英文名 ]:
Val2-Cyclosporine

[中文别名 ]:

环孢霉素D

[英文别名 ]:

CyclosporinD
cyclosporine D
Val2-Cyclosporine
7-L-Valinecyclosporin A
Cyclosporin Impurity 4

环孢菌素 D生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 炎症/免疫

[体外研究]

环孢素D体外抑制钙/钙调素依赖的EF-2磷酸化[1]。

[体内研究]

环孢素D是佛波酯TPA诱导小鼠皮肤生物效应的体内有效抑制剂[1]。

[参考文献]

[1]. Gschwendt M, et al. The weak immunosuppressant cyclosporine D as well as the immunologically inactive cyclosporine H are potent inhibitors in vivo of phorbol ester TPA-induced biological effects in mouse skin and of Ca2+/calmodulin dependent EF-2 phosphorylation in vitro. Biochem Biophys Res Commun. 1988 Jan 29;150(2):545-51.

[2]. Kaiser P, et al. A new approach for the determination of immunosuppressive drugs using HPLC-MS/MS and Cs+ adducts. Ger Med Sci. 2006 Jan 18;4:Doc01.

[3]. Minguillón J, et al. Concentrations of cyclosporin A and FK506 that inhibit IL-2 induction in human T cells do not affect TGF-beta1 biosynthesis, whereas higher doses of cyclosporin A trigger apoptosis and release of preformed TGF-beta1. J Leukoc Biol. 2005 May;77(5):748-58. Epub 2005 Feb 16.

环孢菌素 D物理化学性质

[ 密度 ]:
1.0±0.1 g/cm3

[ 沸点 ]:
1294.7±65.0 °C at 760 mmHg

[ 熔点 ]:
148-151ºC

[ 分子式 ]:
C₆₃H₁₁₃N₁₁O₁₂

[ 分子量 ]:
1216.638

[ 闪点 ]:
736.8±34.3 °C

[ 精确质量 ]:
1215.857056

[ PSA ]:
275.64000

[ LogP ]:
3.70

[ 外观性状 ]:
无色至灰白色结晶固体

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.468

[ 储存条件 ]:
20°C

环孢菌素 D安全信息

[ 符号 ]:

GHS02, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H302 + H312 + H332-H319

[ 警示性声明 ]:
P210-P280-P305 + P351 + P338

[ 危害码 (欧洲) ]:
F,Xn,T

[ 风险声明 (欧洲) ]:
11-20/21/22-36-39/23/24/25-23/24/25

[ 安全声明 (欧洲) ]:
16-36/37-45-7

[ 危险品运输编码 ]:
UN 1648 3 / PGII

[ 海关编码 ]:
29419090

环孢菌素 D文献

Antimalarial activity of cyclosporins A, C and D.

Afr. J. Med. Med. Sci. 23(1) , 47-51, (1994)

Cyclosporin A (CsA) is an immunosuppressive drug widely used in organ transplants. It is also accumulated by the erythrocyte, a site that accommodates one of the stages of malaria parasite. We observe...

Enzymatic synthesis of cyclosporin A.

J. Biol. Chem. 262(36) , 17258-9, (1987)

An enzyme fraction, isolated from crude extracts of the fungus Tolypocladium inflatum, strain 7939/F, is able to synthesize the undecapeptide cyclosporin A. The formation of cyclosporin A was monitore...

In vitro and in vivo comparative studies on immunosuppressive properties of cyclosporines A, C, D and metabolites M1, M17 and M21.

Immunopharmacol. Immunotoxicol. 15(2-3) , 163-77, (1993)

Cyclosporine A (CsA) and its major metabolites: M1, M17 and M21 and two analogues: cyclosporines C (CsC) and D (CsD), were studied for their capacity to interfere with different in vitro activation pa...

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