Cyclosporin G
Based on 1 Customer Validation
Cyclosporin G is a cyclic peptide analog of Cyclosporin A (HY-B0579) metabolized by CYP3A4, and is an immunosuppressant. Cyclosporin G inhibits interleukin-1β-induced NO synthase expression/nitrite production and inhibits insulin release from isolated human pancreatic islets. Cyclosporin G is cytotoxic to hepatoblastoma cells and induces intracellular calcium elevation and necrosis. Cyclosporin G inhibits P-glycoprotein-mediated dye efflux. Cyclosporin G can be used in research on psoriasis and multiple myeloma.
For research use only. We do not sell to patients.
- Purity : 95.0%
- CAS No.: 74436-00-3
- Formula: C63H113N11O12
- Molecular Weight:1216.64
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[2]|
CYP3A4 |
In Vitro
Cyclosporin G inhibits interleukin-1β-stimulated nitrite production in rat glomerular mesangial cells with an IC50 of 2.0 μM[3].
Cyclosporin G (CsG) (0.01-1.0 mg/mL; 3 h) inhibits Rh123 (HY-D0816) efflux in malignant MM B cells at a concentration of 0.05 μg/mL and inhibits Rh123 efflux in normal B cells at a concentration of 0.08 μg/mL[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A431 human epidermoid carcinoma keratinocytes
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Concentration:0.3, 0.6, 1.25, 2.5, 5, 7.5, 10 μg/mL
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Incubation Time:24, 48, 72, 96 h
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Result:Exerted negligible A431 keratinocyte growth inhibition at 24 h.
Produced dose‑dependent antiproliferative effects starting from 48 h, reaching maximal suppression at 72‑96 h under 7.5 μg/mL and 10 μg/mL conditions.
Exhibited time‑ and dose‑dependent cytostatic activity against A431 keratinocytes without overt cytotoxicity, as validated by MTT assay.
Parmacokinetics
| Species | Dose | Route | CL | T1/2 | Vd |
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| Rat[1] | 15 mg/kg | i.v. | 6.4 mL/min/kg | 11.0 h | 6.2 L/kg |
Chemical Information
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CAS No. 74436-00-3
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Appearance Solid
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Molecular Weight 1216.64
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Formula C63H113N11O12
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Color White to off-white
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (82.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (302 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Burdmann EA, et al. Experimental nephrotoxicity, hepatotoxicity and pharmacokinetics of cyclosporin G versus cyclosporin A. Kidney international. 1994 Mar;45(3):684-91. [Content Brief]
[4]. Teofoli P, et al. Cyclosporin G inhibits proliferation of A431 cells in a dose- and time-dependent manner comparable to cyclosporin A. Skin pharmacology : the official journal of the Skin Pharmacology Society. 1997;10(2):79-84. [Content Brief]
[6]. Nielsen JH, et al. Direct effects of cyclosporin A on human pancreatic β-cells. Diabetes. 1986 Sep 1;35(9):1049-52. [Content Brief]
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.8219 mL | 4.1097 mL | 8.2194 mL | 20.5484 mL |
| 5 mM | 0.1644 mL | 0.8219 mL | 1.6439 mL | 4.1097 mL | |
| 10 mM | 0.0822 mL | 0.4110 mL | 0.8219 mL | 2.0548 mL | |
| 15 mM | 0.0548 mL | 0.2740 mL | 0.5480 mL | 1.3699 mL | |
| 20 mM | 0.0411 mL | 0.2055 mL | 0.4110 mL | 1.0274 mL | |
| 25 mM | 0.0329 mL | 0.1644 mL | 0.3288 mL | 0.8219 mL | |
| 30 mM | 0.0274 mL | 0.1370 mL | 0.2740 mL | 0.6849 mL | |
| 40 mM | 0.0205 mL | 0.1027 mL | 0.2055 mL | 0.5137 mL | |
| 50 mM | 0.0164 mL | 0.0822 mL | 0.1644 mL | 0.4110 mL | |
| 60 mM | 0.0137 mL | 0.0685 mL | 0.1370 mL | 0.3425 mL | |
| 80 mM | 0.0103 mL | 0.0514 mL | 0.1027 mL | 0.2569 mL |
Cyclosporin G Related Classifications
HY-105023 Related Classifications
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Keywords
- Cyclosporin G
- 74436-00-3
- Amino Acid Derivatives
- Cytochrome P450
- NO Synthase
- CYP3A4
- P-glycoprotein 170
- apoptosis
- cyclophilin
- epidermoid carcinoma
- glomerular mesangial cells
- hepatoblastoma
- hepatocyte cytotoxicity
- hypomagnesemia
- iNOS
- insulin release
- interleukin-1β
- intracellular calcium
- keratinocyte proliferation
- magnesium excretion
- multiple myeloma
- necrosis
- nitrite
- pancreatic islets
- psoriasis
- Inhibitor
- inhibitor
- inhibit