Cyclosporin H [83602-39-5]
Référence T21493-1mg
Conditionnement : 1mg
Marque : TargetMol
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Cyclosporin H
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Cyclosporin H (CsH), a specific inhibitor of FPR1, inhibited lung inflammation in the ALI models. CsH significantly attenuated MTDs or NFP-induced inflammatory lung injury and activation of MAPK and AKT pathways. Cyclosporin H is a viral transduction enhancer which increases lentiviral transduction up to 10-fold in human cord blood-derived hematopoietic stem and progenitor cells (HSPCs). When combined with Rapamycin or Prostaglandin E2 Cyclosporin H displays an additive effect. Cyclosporin H lacks immunosuppressant activity of Cyclosporin A.
Cas No. 83602-39-5
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.94%
Appearance:Solid
Color:White
COA HNMR LCMS
Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Cyclosporin H (CsH), a specific inhibitor of FPR1, inhibited lung inflammation in the ALI models. CsH significantly attenuated MTDs or NFP-induced inflammatory lung injury and activation of MAPK and AKT pathways. Cyclosporin H is a viral transduction enhancer which increases lentiviral transduction up to 10-fold in human cord blood-derived hematopoietic stem and progenitor cells (HSPCs). When combined with Rapamycin or Prostaglandin E2 Cyclosporin H displays an additive effect. Cyclosporin H lacks immunosuppressant activity of Cyclosporin A. |
| Targets & IC50 | FMLP:0.1 μM (ki) |
| In vitro | Cyclosporin H is a potent inhibitor of FMLP-induced superoxide anion (O2-) formation in human neutrophils. Cyclosporin H inhibited FMLP binding in HL-60 membranes with a Ki (inhibition constant) of 0.10 μM. Cyclosporin H inhibited activation by FMLP of high affinity GTPase (the enzymatic activity of alpha-subunits of heterotrimeric regulatory guanine nucleotide-binding proteins) in HL-60 membranes with a Ki of 0.79 μM. Cyclosporin H inhibited the stimulatory effects of FMLP on cytosolic Ca2+ concentration ([Ca2+]i), O2- formation, and beta-glucuronidase release with Ki values of 0.08, 0.24, and 0.45 μM, respectively. |
| In vivo | Cyclosporin H, administered intraperitoneally (i.p.) at a dosage of 5 mg/kg prior to challenge with LPS or HCl, mitigates lung injury caused by LPS or HCl in a lung injury model. |
| Molecular Weight | 1202.61 |
| Formula | C62H111N11O12 |
| Cas No. | 83602-39-5 |
| Smiles | [C@H]([C@@H](C/C=C/C)C)(O)[C@@]1(N(C)C(=O)[C@@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H]([C@@H](C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C(=O)[C@H](CC)NC1=O)20 |
| Relative Density. | 1.015 g/cm3 |
| Sequence | Cyclo[{Abu}-{Sar}-{N(Me)Leu}-Val-{N(Me)Leu}-Ala-{D-Ala}-{N(Me)Leu}-{N(Me)Leu}-{D-N(Me)Val}-{N(Me)Bmt(E)}] |
| Sequence Short | XXLVLAALLV |
| Storage | Keep away from moisture,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 99 mg/mL (82.32 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 3.3 mg/mL (2.74 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||