Cyclosporin A (Synonyms: 環(huán)bao素; Cyclosporine A; Ciclosporin A; CsA)
Cyclosporin A (Cyclosporine A) 是一種免疫抑制劑,能與親環(huán)素結(jié)合,抑制 calcineurin 活性的IC50 值為 7 nM。Cyclosporin A 也抑制 CD11a/CD18 粘附分子。
生物活性
Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM[3]. Cyclosporin A also inhibits CD11a/CD18 adhesion[8].
IC50 & Target
IC50: 7 nM (calcineurin)
體外研究(In Vitro)
Cyclosporin A is able to bind with the cyclophilin in T cells[1]. Cyclosporin A works by forming a Cyclophilin-Cyclosporin A complex to inhibit calcineurin[2]. Cyclosporin A inhibits calcineurin in stimulated cells with an IC50 value of 7 nM[3]. Cyclosporin A suppresses the nuclear translocation of NF-AT[4]. Cyclosporin A shows an effect on mitochondria via preventing the MTP from opening with an IC50 of 39 nM[5].
體內(nèi)研究(In Vivo)
Cyclosporin A has immunosuppressive activity, and is active via parenteral and p.o. administration in mice, rat and guinea pigs[6]. Cyclosporin A can be used in organ transplantation to prevent rejection[7].
分子量:1202.61
性狀:Solid
Formula:C62H111N11O12
CAS 號:59865-13-3
中文名稱:huan孢霉素A;環(huán)孢suA;環(huán)bao多肽A;環(huán)孢靈;賽斯平;環(huán)bao素
來源:the fungus Beauveria nivea.
運輸條件
Room temperature in continental US; may vary elsewhere.
儲存方式
4°C, protect from light
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性數(shù)據(jù)
DMSO : 62.5 mg/mL (51.97 mM; Need ultrasonic)
Ethanol : 50 mg/mL (41.58 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 0.8315 mL | 4.1576 mL | 8.3152 mL |
5 mM | 0.1663 mL | 0.8315 mL | 1.6630 mL |
10 mM | 0.0832 mL | 0.4158 mL | 0.8315 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時,請在 6 個月內(nèi)使用,-20°C 儲存時,請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑: corn oil
Solubility: 20 mg/mL (16.63 mM); Clear solution; Need ultrasonic
- 2.
請依序添加每種溶劑: 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: 2.62 mg/mL (2.18 mM); Suspended solution; Need ultrasonic
- 3.
請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (1.73 mM); Suspended solution; Need ultrasonic
- 4.
請依序添加每種溶劑: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (1.73 mM); Suspended solution; Need ultrasonic
- 5.
請依序添加每種溶劑: 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (1.73 mM); Clear solution
參考文獻
[1]. Handschumacher RE, et al. Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science. 1984 Nov 2;226(4674):544-7. [Content Brief]
[2]. Liu J, et al. Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15. [Content Brief]
[3]. Fruman DA, et al. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc Natl Acad Sci U S A. 1992 May 1;89(9):3686-90. [Content Brief]
[4]. Flanagan WM, et al. Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A. Nature. 1991 Aug 29;352(6338):803-7. [Content Brief]
[5]. Nicolli A, et al. Interactions of cyclophilin with the mitochondrial inner membrane and regulation of the permeability transition pore, and cyclosporin A-sensitive channel. J Biol Chem. 1996 Jan 26;271(4):2185-92. [Content Brief]
[6]. Borel JF, et al. Effects of the new anti-lymphocytic peptide cyclosporin A in animals. Immunology. 1977 Jun;32(6):1017-25. [Content Brief]
[7]. Williams, R, et al. Randomised trial comparing FK506 and cyclosporin in prevention of liver allograft rejection. European FK506 Multicentre Liver Study Group. Lancet, 1994, 344(8920), 423-428. [Content Brief]
[8]. Dalmarco EM, et al. Cyclosporin A inhibits CD11a/CD18 adhesion molecules due to inhibition of TNFalpha and IL-1 beta levels in the mouse model of pleurisy induced by carrageenan. Cell Adh Migr. 2008 Oct-Dec;2(4):231-5. [Content Brief]
注:產(chǎn)品僅用于科研