Cyclosporin A (Synonyms: Cyclosporine A; Ciclosporin A; CsA)

Name: Cyclosporin A
Brand: MedChemExpress
SKU: HY-B0579
Rating: 5.0 (133 reviews)

Cat. No.: HY-B0579 Purity: 99.90%: FAQs
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Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM. Cyclosporin A also inhibits CD11a/CD18 adhesion.

For research use only. We do not sell to patients.

Cyclosporin A Chemical Structure

CAS No. : 59865-13-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
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Based on 133 publication(s) in Google Scholar

Other Forms of Cyclosporin A:

119 Publications Citing Use of MCE Cyclosporin A

Proliferation Assay

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142. [Abstract]; Representative western blotting images of NLRP3, ASC, pro-CASP-1, cleaved CASP-1, GSDMD, and cleaved GSDMD in the (CsA; 10 μM; for 24 h)- or DMSO-treated NP cells.

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142. [Abstract]; Representative western blotting images of cGAS and STING in the Cyclosporine (CsA; 10 μM; for 24 h)- or DMSO-treated NP cells.

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142. [Abstract]; Representative immunofluorescence images of STING with different degrees of polymerization in the Cyclosporine (CsA; 10 μM; for 24 h)- or DMSO-treated NP cells.

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Redox Biol. 2022 Aug;54:102355.; Cells are treated with or without Cyclosporine A (CsA; 2 μM) for 4 h in presence of NRC-03 (45 μg/mL). Cell viability determined by CCK-8.

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Redox Biol. 2022 Aug;54:102355.; Cells are treated with or without Cyclosporine A (CsA; 2 μM) for 4 h in presence of NRC-03 (45 μg/mL). TUNEL immunofluorescence staining and quantification of TUNEL positive cells.

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Aging Dis. 2022 Oct 1;13(5):1546-1561. [Abstract]; Additionally, similar to P-gp siRNA silence, pharmacological inhibition of P-gp with Cyclosporine A (CsA; 22 mg/kg) significantly attenuates P-gp expression levels in ischemic brain as compared to vehicle treatment.

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 May 18;12(1):2915. [Abstract]; Immunoblot analysis of Cytochrome c from cytosolic extracts and mitochondria from indicated cells pre-treated with DMSO or Cyclosporine A (50 μM) for 1 h, followed with PFOS treatment (150 μM, 6 h).

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Apr 20;12(5):413. [Abstract]; Inhibition of NR-induced increase of co-localized puncta (LC3 and TOM20) after 1 μMCyclosporin A (CsA) pretreatment.

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Apr 1;12(4):336. [Abstract]; Immunofluorescence staining of subcellular localization of NFATC1 in RANK overexpression and control cells with or without treatment of 10 μg/mL Cyclosporin A (CsA).

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Rep. 2021 Nov 30;37(9):110069. [Abstract]; Colony formation of CRC cells treated with Cyclosporine A (CsA; 2.5-5 μM) in combination with 5-FU or OXA for 48 h.

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Rep. 2021 Nov 30;37(9):110069. [Abstract]; Immunoblotting analysis of indicated apoptotic markers expression in CRC cells treated with Cyclosporine A (CsA; 2.5-5 μM) in combination with 5-FU or OXA.

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2021 Jan 12;118(2):e2009539118. [Abstract]; Calcineurin activities of the PCE after FK506 or Cyclosporine A (CsA; 4 µM) treatment Zebrafish.

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2021 Jun;178(11):2305-2323. [Abstract]; Smooth muscle cells are treated cyclosporin A (CsA, 1 μM) or PDTC (10 μM) for 24 h before measuring the activity of PPARγ2 promoter.

: Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):598. [Abstract]; A549 cells are pretreated with 5 µM Cyclosporin A (CSA) for 2 h, followed by treatment with 80 μM Hirsutine for 24 h. equal amount of lysates are subjected to immunoprecipitation using anti-ANT1 antibody, the associated CypD is determined using immunoblotting.

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Biological Activity
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Description

Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM^[3]. Cyclosporin A also inhibits CD11a/CD18 adhesion^[8].

IC₅₀ & Target

Cyclophilin D

Cellular Effect

Cell Line	Type	Value	Description	References
2008	IC₅₀	2.7 μM Compound: Cyclosporine A	Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay	[PMID: 24184213]
2008	IC₅₀	2.81 μM Compound: CsA	Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay	[PMID: 23851114]
A2780	GI₅₀	8.94 μM Compound: Cyclosporine A	Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27100033]
A2780 ADR	IC₅₀	0.919 μM Compound: CsA	Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay	[PMID: 25855895]
A2780 ADR	IC₅₀	0.92 μM Compound: Cyclosporine A	Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay	[PMID: 24184213]
A2780 ADR	IC₅₀	0.99 μM Compound: CsA	Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay	[PMID: 23851114]
A2780 ADR	IC₅₀	1.21 μM Compound: Cyclosporine A	Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay	[PMID: 27676469]
A2780 ADR	IC₅₀	1.4 μM Compound: Cyclosporin A	Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay	[PMID: 19250834]
A2780 ADR	IC₅₀	1.41 μM Compound: Cyclosporine A	Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay	[PMID: 27100033]
A2780 ADR	GI₅₀	8.63 μM Compound: Cyclosporine A	Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27100033]
B-cell	IC₅₀	0.07 μg/mL Compound: cyclosporin A	Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay	[PMID: 14738397]
B-cell	IC₅₀	0.74 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in LPS-induced mouse B-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in LPS-induced mouse B-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay	[PMID: 35678710]
Breast cancer cell line	EC₅₀	0.5 μM Compound: Cyclosporin A	Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%. Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%.	[PMID: 11784143]
Breast cancer cell line	EC₅₀	0.6 μM Compound: Cyclosporin A	Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50% Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%	[PMID: 11784143]
CCRF-CEM	IC₅₀	3.4 μM Compound: 1	Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells	[PMID: 12361387]
HEK293	IC₅₀	0.7 μM Compound: Cyclosporine A	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate	[PMID: 22587986]
HEK293	IC₅₀	0.7 μM Compound: Cyclosporine A	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate	[PMID: 22587986]
HEK293	IC₅₀	1.2 μM Compound: Cyclosporine A	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate	[PMID: 22587986]
HEK293	IC₅₀	1.3 μM Compound: Cyclosporin A	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	1.4 μM Compound: Cyclosporin A	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	37 μM Compound: Cyclosporin A	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
HeLa	IC₅₀	6.6 μM Compound: Cs	Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 3 days Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 3 days	[PMID: 18212100]
HFF	IC₅₀	> 10000 nM Compound: CSA	Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting	[PMID: 14593182]
Huh-5-2	EC₅₀	0.3 μM Compound: Cyclosporine A	Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay	[PMID: 18625766]
Huh-5-2	EC₅₀	306 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 1b I389luc-ubi-neo/NS3-3'/5.1 subgenomic replicon infected in human Huh5-2 cells after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b I389luc-ubi-neo/NS3-3'/5.1 subgenomic replicon infected in human Huh5-2 cells after 4 days by luciferase assay	10.1039/C1MD00227A
Huh-5-2	CC₅₀	4.4 μM Compound: CsA	Cytostatic activity against human Huh5-2 cells assessed as decrease in cell proliferation after 3 days by MTS method Cytostatic activity against human Huh5-2 cells assessed as decrease in cell proliferation after 3 days by MTS method	10.1039/C1MD00227A
Huh-5-2	CC₅₀	6 μM Compound: Cyclosporine A	Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay	[PMID: 18625766]
Huh-7	EC₅₀	> 10 μM Compound: CsA	Antiviral activity against cyclosporine A/NIM-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against cyclosporine A/NIM-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	EC₅₀	0.21 μM Compound: CsA	Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	EC₅₀	137 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Huh-7	EC₅₀	198 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 1a H77 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1a H77 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Huh-7	EC₅₀	3.39 μM Compound: CsA	Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	EC₅₀	455 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 2a JFH-1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 2a JFH-1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Huh-7	CC₅₀	5.62 μM Compound: CsA	Antiviral activity against Hepatitis C virus infected in human Huh7ET cells assessed as inhibition of viral replication after 72 hrs by luciferase reporter gene assay Antiviral activity against Hepatitis C virus infected in human Huh7ET cells assessed as inhibition of viral replication after 72 hrs by luciferase reporter gene assay	[PMID: 19933795]
Jurkat	IC₅₀	> 10 μM Compound: CsA	Cytotoxicity against human Jurkat cells after 4 days by MTT assay Cytotoxicity against human Jurkat cells after 4 days by MTT assay	[PMID: 22984987]
Jurkat	EC₅₀	0.005 μM Compound: CsA	Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay	[PMID: 19933795]
Jurkat	IC₅₀	1.4 nM Compound: 1	Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay	[PMID: 23964991]
Jurkat	IC₅₀	1.9 μM Compound: CsA	Immunosuppressive activity in human Jurkat cells assessed as reduction in PHA + PMA-induced IL-2 production after 48 hrs by ELISA Immunosuppressive activity in human Jurkat cells assessed as reduction in PHA + PMA-induced IL-2 production after 48 hrs by ELISA	[PMID: 30579802]
Jurkat	IC₅₀	11 nM Compound: 1; CyA	Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA	[PMID: 27647370]
Jurkat	IC₅₀	12 nM Compound: CsA	The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells. The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells.	[PMID: 7473543]
Jurkat	IC₅₀	2 nM Compound: CsA	Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells. Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells.	[PMID: 14643337]
K562/R7	IC₅₀	0.7 μM Compound: cyclosporin A	Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay	[PMID: 25634041]
KB	IC₅₀	0.6 μM Compound: CSA (cyclosporin A)	Inhibitory activity against KB cell line after 72 h of drug exposure Inhibitory activity against KB cell line after 72 h of drug exposure	[PMID: 15481991]
KB 3-1	IC₅₀	1.5 μM Compound: CSA (cyclosporin A)	Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure	[PMID: 15481991]
L929	IC₅₀	29.9 μM Compound: Cyclosporin A	Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 34597896]
L929	IC₅₀	30 μM Compound: cyclosporin A	Cytotoxicity against mouse L929 cells after 3 days by MTS assay Cytotoxicity against mouse L929 cells after 3 days by MTS assay	[PMID: 25985195]
L929	IC₅₀	33.9 μM Compound: cyclosporine A	Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay	[PMID: 24171478]
L929	IC₅₀	33.9 μM Compound: 2	Cytotoxicity against mouse L929 cells after 72 hrs Cytotoxicity against mouse L929 cells after 72 hrs	[PMID: 22320402]
LLC-PK1	IC₅₀	0.7 μM Compound: Cyclosporin a	Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	0.8 μM Compound: Cyclosporin a	Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	4.8 μM Compound: Cyclosporin a	Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
Lymphocyte	IC₅₀	0.054 μM Compound: CsA	Immunosuppressive activity in peripheral blood lymphocytes isolated from two individuals assessed as proliferation using [methyl-3H]thymidine by mixed lymphocyte reaction assay Immunosuppressive activity in peripheral blood lymphocytes isolated from two individuals assessed as proliferation using [methyl-3H]thymidine by mixed lymphocyte reaction assay	[PMID: 21171614]
Lymphocyte	IC₅₀	0.054 μM Compound: CsA	Immunosuppressive activity in lymphocytes by mixed lymphocyte reaction assay Immunosuppressive activity in lymphocytes by mixed lymphocyte reaction assay	[PMID: 20064721]
Lymphocyte	IC₅₀	0.2 μg/mL Compound: Cyclosporin A	Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay	[PMID: 3373220]
Lymphocyte	EC₅₀	60 nM Compound: 1, CSA	Immunosuppressive activity in lymphocytes (unknown origin) by mixed lymphocyte reaction assay Immunosuppressive activity in lymphocytes (unknown origin) by mixed lymphocyte reaction assay	[PMID: 24831536]
Lymphocyte	IC₅₀	89 nM Compound: CsA	Immunosuppressive activity in lymphocytes by MLR assay Immunosuppressive activity in lymphocytes by MLR assay	[PMID: 24900866]
MDCK-II	IC₅₀	25.6 μM Compound: Cyclosporine A	Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry	[PMID: 27393949]
MT4	IC₅₀	> 0.83 μM Compound: Cs	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay	[PMID: 18212100]
MT4	EC₅₀	450 nM Compound: 1, CsA	Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 23849880]
MT4	CC₅₀	5608 nM Compound: CSA	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay	[PMID: 30074795]
PBMC	EC₅₀	0.0031 μM Compound: CsA	Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay	[PMID: 19933795]
PBMC	IC₅₀	0.056 μM Compound: Cs	Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs	[PMID: 18212100]
PBMC	IC₅₀	3 nM Compound: CsA	Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay	10.1039/C1MD00227A
RD	CC₅₀	> 10 μM Compound: CsA	Cytotoxicity against human RD cells after 24 hrs by WST-1 assay Cytotoxicity against human RD cells after 24 hrs by WST-1 assay	[PMID: 26564266]
RD	EC₅₀	3.66 μM Compound: CsA	Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay	[PMID: 26564266]
Splenocyte	CC₅₀	> 2.5 μM Compound: CsA	Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 35104138]
Splenocyte	IC₅₀	0.01 μg/mL Compound: Cyclosporine A	Antiproliferative activity against concanavalin A-stimulated BALB/c mouse splenocytes after 72 hrs by AlamarBlue assay Antiproliferative activity against concanavalin A-stimulated BALB/c mouse splenocytes after 72 hrs by AlamarBlue assay	[PMID: 23167554]
Splenocyte	IC₅₀	0.01 μM Compound: CsA	Immunosuppressive activity in splenocytes assessed as inhibition of concanavalin A-induced proliferation after 48 hrs by [3H]thymidine incorporation assay Immunosuppressive activity in splenocytes assessed as inhibition of concanavalin A-induced proliferation after 48 hrs by [3H]thymidine incorporation assay	[PMID: 19481938]
Splenocyte	EC₅₀	0.03 μM Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocyte assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 48 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenocyte assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 48 hrs by MTT assay	[PMID: 36596229]
Splenocyte	IC₅₀	0.03 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of concanavalin A induced T-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of concanavalin A induced T-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis	[PMID: 35104138]
Splenocyte	IC₅₀	0.04 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated before concanavalin A stimulation for 48 hrs followed by [3H]-thymidine additio Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated before concanavalin A stimulation for 48 hrs followed by [3H]-thymidine additio	[PMID: 31253536]
Splenocyte	IC₅₀	0.04 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by concanavalin A stimulation and [3H]-thymidine addition f Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by concanavalin A stimulation and [3H]-thymidine addition f	[PMID: 30500185]
Splenocyte	IC₅₀	0.07 μM Compound: CsA	Immunosuppressive activity in splenocytes assessed as inhibition of LPS-induced proliferation after 48 hrs by [3H]thymidine incorporation assay Immunosuppressive activity in splenocytes assessed as inhibition of LPS-induced proliferation after 48 hrs by [3H]thymidine incorporation assay	[PMID: 19481938]
Splenocyte	IC₅₀	0.1 μM Compound: Cyclosporin A	Immunosupressive activity in OVA323-339 peptide-stimulated OT-2 T cell receptor transgenic mouse splenocytes assessed as inhibition of T cell proliferation after 3 days by MTT assay Immunosupressive activity in OVA323-339 peptide-stimulated OT-2 T cell receptor transgenic mouse splenocytes assessed as inhibition of T cell proliferation after 3 days by MTT assay	[PMID: 25537268]
Splenocyte	IC₅₀	0.3 μM Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation incubated for 48 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33544615]
Splenocyte	IC₅₀	0.32 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of LPS induced B-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of LPS induced B-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis	[PMID: 35104138]
Splenocyte	IC₅₀	0.4 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated before LPS stimulation for 48 hrs followed by [3H]-thymidine addition for 8 hrs by beta-sc Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated before LPS stimulation for 48 hrs followed by [3H]-thymidine addition for 8 hrs by beta-sc	[PMID: 31253536]
Splenocyte	IC₅₀	0.4 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by LPS stimulation and [3H]-thymidine addition for 8 hrs measured afte Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by LPS stimulation and [3H]-thymidine addition for 8 hrs measured afte	[PMID: 30500185]
Splenocyte	CC₅₀	0.88 μM Compound: CsA	Cytotoxicity against splenocytes after 48 hrs by MTT assay Cytotoxicity against splenocytes after 48 hrs by MTT assay	[PMID: 19481938]
Splenocyte	CC₅₀	1.2 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocytes assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay Cytotoxicity against BALB/c mouse splenocytes assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay	[PMID: 31253536]
Splenocyte	CC₅₀	1.2 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocytes after 48 hrs by CCK-8 assay Cytotoxicity against BALB/c mouse splenocytes after 48 hrs by CCK-8 assay	[PMID: 30500185]
Splenocyte	IC₅₀	10 nM Compound: Cyclosporine A	Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay	[PMID: 19827831]
Splenocyte	IC₅₀	10.15 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocyte assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay Cytotoxicity against BALB/c mouse splenocyte assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay	[PMID: 33973788]
Splenocyte	IC₅₀	17 nM Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay	[PMID: 19827831]
Splenocyte	IC₅₀	30 nM Compound: 1, CsA	Immunosuppressant activity in mouse splenocytes by mixed-leukocyte reaction assay Immunosuppressant activity in mouse splenocytes by mixed-leukocyte reaction assay	[PMID: 23017885]
Splenocyte	CC₅₀	7.33 μM Compound: CsA	Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 35678710]
T cell line	IC₅₀	26 nM Compound: CsA	Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay	[PMID: 32822186]
T cell line	CC₅₀	9.8 μM Compound: CsA	Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 32822186]
T-cell	IC₅₀	> 10000 nM Compound: CSA	Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting	[PMID: 14593182]
T-cell	IC₅₀	0.011 μM Compound: CsA	Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay	[PMID: 22984987]
T-cell	IC₅₀	0.03 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay	[PMID: 35678710]
T-cell	IC₅₀	0.04 μg/mL Compound: cyclosporin A	Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay	[PMID: 14738397]
T-cell	IC₅₀	0.06 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay	[PMID: 21131104]
T-cell	IC₅₀	0.07 μM Compound: CsA	Immunosuppressive activity in lymph node T cell assessed as inhibition of ConA-stimulated cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in lymph node T cell assessed as inhibition of ConA-stimulated cell proliferation after 72 hrs by MTT assay	[PMID: 22300886]
T-cell	IC₅₀	0.08 μM Compound: Cyclosporin A	Inhibition of ConA-induced cell proliferation of BALB/c mouse T-lymphocytes assessed as reduction in [3H]thymidine incorporation incubated for 48 hrs by beta scintillation counting method Inhibition of ConA-induced cell proliferation of BALB/c mouse T-lymphocytes assessed as reduction in [3H]thymidine incorporation incubated for 48 hrs by beta scintillation counting method	[PMID: 28294615]
T-cell	IC₅₀	0.2 μM Compound: CsA	Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis	[PMID: 31181920]
T-cell	IC₅₀	0.34 μM Compound: cyclosporin A	Inhibition of PHA-induced human T cell proliferation after 24 hrs by MTT assay Inhibition of PHA-induced human T cell proliferation after 24 hrs by MTT assay	[PMID: 11678649]
T-cell	CC₅₀	13.78 μM Compound: CsA	Cytotoxicity against lymph node T cell after 24 hrs by MTT assay Cytotoxicity against lymph node T cell after 24 hrs by MTT assay	[PMID: 22300886]
T-cell	IC₅₀	14 nM Compound: cyclosporin A	Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay	[PMID: 21456524]
T-cell	CC₅₀	15.82 μM Compound: CsA	Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay	[PMID: 21131104]
T-cell	IC₅₀	2.12 μM Compound: csa	Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay	[PMID: 22727369]
T-cell	IC₅₀	32 nM Compound: CSA	Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method	[PMID: 14593182]
T-cell	CC₅₀	4.5 μM Compound: Cyclosporin A	Cytotoxic activity against BALB/c mouse T-lymphocytes assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxic activity against BALB/c mouse T-lymphocytes assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 28294615]
T-cell	IC₅₀	550 nM Compound: CsA	Immunosuppressive activity in concanavalin A-activated T cell assessed as inhibition of lymphoproliferation after 3 days by beta-scintillation counting Immunosuppressive activity in concanavalin A-activated T cell assessed as inhibition of lymphoproliferation after 3 days by beta-scintillation counting	[PMID: 19502058]
T-cell	EC₅₀	6.4 nM Compound: CsA	Immunosuppressive activity in human PBMC assessed as inhibition of anti-human CD3-induced T-cell proliferation after 4 days by CellTrace violet cell proliferation dye based FACS analysis Immunosuppressive activity in human PBMC assessed as inhibition of anti-human CD3-induced T-cell proliferation after 4 days by CellTrace violet cell proliferation dye based FACS analysis	[PMID: 28075591]
T-cell	IC₅₀	74 nM Compound: CSA	Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method	[PMID: 14593182]
Ventricular myocyte	IC₅₀	2 μM Compound: Cyclosporin A	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]
Vero	CC₅₀	> 50 μM Compound: Cyclosporine	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	≤ 0.5 μM Compound: Cs	Antiviral activity against Dengue virus 1 infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay Antiviral activity against Dengue virus 1 infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay	[PMID: 19451286]
Vero	IC₅₀	5.82 μM Compound: Cyclosporine	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730
Vero	IC₅₀	8 μM Compound: Cs	Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay	[PMID: 19451286]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Cyclosporin A can be used to construct uremia models. In male Wistar rats (weighing 140-200 g, aged 5-6 weeks), the pharmacokinetic parameters following intravenous administration of Cyclosporin A (10 mg/kg) show an area under the curve of 27.3 μg·h/mL, a half-life of 6.9 hours, and a volume of distribution of 3.7 L/kg^[9].

Induction of uraemia^[10]^[11]

Background

Cyclosporin A administration induces interstitial deposition of collagen type III and fibrosis via stimulation of the Transforming Growth Factor beta (TGF-β)-signalling pathway, while inhibiting extracellular matrix (ECM) degradation via modulation of matrix metallopeptidase 9, thus leading to an imbalance in ECM turn over^[2].

Specific Mmodeling Methods

Mice: Six-to-eight weeks old C57BL/6 mice
Administration: 30 mg/kg • SC • daily for 16 weeks

Note

Modeling Indicators

Molecular changes: Upregulated mRNA expression of both LOX, LOXL2, TNFα, MCP-1, (NOX)4; significantly downregulated SOD2 mRNA expression; increased the urea nitrogen (BUN) level, increased tubular injury, interstitial inflammation and fibrosis scores, PAS scores, increased the level the deposition of collagen type I (COL1) and type III (COL3) in the renal ECM,increased the expression of alpha-smooth-muscle actin (α-SMA), fibronectin (FN), COL1A, MCP-1^[10]^[11].

Correlated Product(s): /

Opposite Product(s): Lipoxygenase, general (HY-P2976); Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11) (HY-P990107)

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

1202.61

Formula

C₆₂H₁₁₁N₁₁O₁₂

CAS No.

59865-13-3

Appearance

Solid

Color

White to off-white

SMILES

C/C=C/C[C@H]([C@@H](O)[C@@]1(N(C)C([C@]([H])(C(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@]([H])(CC(C)C)N(C)C([C@@H](C)NC([C@H](C)NC([C@@H](N(C([C@@]([H])(NC([C@@H](N(C(CN(C([C@@H](NC1=O)CC)=O)C)=O)C)CC(C)C)=O)C(C)C)=O)C)CC(C)C)=O)=O)=O)=O)=O)=O)[H])C

Structure Classification

Others

Initial Source

Microorganisms

the fungus Beauveria nivea.

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (51.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 50 mg/mL (41.58 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.62 mg/mL (2.18 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (1.73 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (1.73 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (1.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: Corn Oil
Solubility: 20 mg/mL (16.63 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (293 KB) SDS (419 KB)

COA (260 KB) LCMS (193 KB)

Handling Instructions (2659 KB)

References

[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]

[9]. Medeiros M, et al. Increased cyclosporine bioavailability induced by experimental nephrotic syndrome in rats. Can J Physiol Pharmacol. 2007 May;85(5):502-6. [Content Brief]

[10]. Nguyen LT, et al. Lysyl oxidase inhibitors attenuate cyclosporin A-induced nephropathy in mouse. Sci Rep. 2021 Jun 14;11(1):12437. [Content Brief]

[11]. Ling H, et al. Therapeutic role of TGF-beta-neutralizing antibody in mouse cyclosporin A nephropathy: morphologic improvement associated with functional preservation. J Am Soc Nephrol. 2003 Feb;14(2):377-88. [Content Brief]

Cell Assay ^[3]	Immunosuppressive agents are dissolved in ethanol at concentrations 1000-fold more than the concentration desired for cell treatments. Cells (10⁶) are suspended in 1 mL of complete medium in microcentrifuge tubes; 1 μL of ethanol or of the ethanolic solution of Cyclosporin A is added, and the cells are incubated at 37°C for 1 hr. Cells are washed twice with 1 mL of PBS on ice and lysed in 50 μL of hypotonic buffer containing 50 mM Tris (pH 7.5); 0.1 mM EGTA; 1 mM EDTA; 0.5 mM dithiothreitol; and 50 μg of phenylmethylsulfonyl fluoride, 50 μg of soybean trypsin inhibitor, 5 μg of leupeptin, and 5 μg of Kiker 52G per mL. Lysates are subjected to three cycles of freezing in liquid nitrogen followed by thawing at 30°C and then are centrifuged at 4°C for 10 min at 12,000×g. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[6]	Rats are immunized on day 0 i.p. with 0 5 mL and mice i.v. with 0 2 mL of a 10% suspension of washed sheep erythrocytes (SE). To elicit a secondary response, mice are boosted 8-11 weeks after the primary immunization with an i.v. injection of 0-2 mL of 0 25% washed SE (10⁷ cells). For prolonged treatment the animals receive on the average 45 mg/kg cyclosporin A daily in the food during 13 weeks. These rats are immunized 5 days before killing. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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] [9]. Medeiros M, et al. Increased cyclosporine bioavailability induced by experimental nephrotic syndrome in rats. Can J Physiol Pharmacol. 2007 May;85(5):502-6. [Content Brief] [10]. Nguyen LT, et al. Lysyl oxidase inhibitors attenuate cyclosporin A-induced nephropathy in mouse. Sci Rep. 2021 Jun 14;11(1):12437. [Content Brief] [11]. Ling H, et al. Therapeutic role of TGF-beta-neutralizing antibody in mouse cyclosporin A nephropathy: morphologic improvement associated with functional preservation. J Am Soc Nephrol. 2003 Feb;14(2):377-88. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

Ethanol / DMSO	1 mM	0.8315 mL	4.1576 mL	8.3152 mL	20.7881 mL
	5 mM	0.1663 mL	0.8315 mL	1.6630 mL	4.1576 mL
	10 mM	0.0832 mL	0.4158 mL	0.8315 mL	2.0788 mL
	15 mM	0.0554 mL	0.2772 mL	0.5543 mL	1.3859 mL
	20 mM	0.0416 mL	0.2079 mL	0.4158 mL	1.0394 mL
	25 mM	0.0333 mL	0.1663 mL	0.3326 mL	0.8315 mL
	30 mM	0.0277 mL	0.1386 mL	0.2772 mL	0.6929 mL
	40 mM	0.0208 mL	0.1039 mL	0.2079 mL	0.5197 mL
DMSO	50 mM	0.0166 mL	0.0832 mL	0.1663 mL	0.4158 mL

Cyclosporin A Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Cyclosporin A59865-13-3Cyclosporine A Ciclosporin A CsAMolecular GluesComplement SystemAntibioticCyclophilinInhibitorinhibitorinhibit

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Cyclosporin A (Synonyms: Cyclosporine A; Ciclosporin A; CsA)

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