Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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25mg |
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Other Sizes |
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Purity: = 96.32%
Cyclosporin H is a naturally occuring cyclic undecapeptide, acting as a potent TPA/PMA (tumor promoting phorbol ester) inhibitor and a selective inhibitor of formyl peptide receptors (FPR-1) with Ki of 0.1 uM. Unlike Cyclosporin A, Cyclosporin H does not bind cyclophilin to evoke an immunosuppressant response. Cyclosporin H has been shown to prevent EF-2 phosphorylation that is dependent on calcium/calmodulin in vitro and to inhibit the effects of phorbol ester in mouse skin.
ln Vitro |
Cyclosporin H is a potent marker of formyl-Met-Leu-Phe (FMLP)-induced superoxide label (O2-) formation in human neutrophils. Cyclosporin H inhibits the binding of FMLP on the HL-60 membrane, with a Ki of 0.1. Cyclosporine H inhibits the high-affinity GTPase (heterotrimer regulates the enzymatic activity of the guanine inhibitory binding protein α subunit) on the HL-60 membrane. For activation, Ki is 0.79 μM. Cyclosporine H inhibits the stimulating effect of FMLP on cytoplasmic Ca2+ concentration ([Ca2+]i), O2- formation and β-aldase release, with Ki values of 0.08, 0.24 and 0.45 μM respectively [2].
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ln Vivo |
Cyclosporine H (5 mg/kg; intraperitoneally; before LPS or HCl challenge) reduces LPS or HCl-conducted lung injury (a model of lung injury) [1].
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References |
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Molecular Formula |
C62H111N11O12
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Molecular Weight |
1202.6113
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Exact Mass |
1201.84
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Elemental Analysis |
C, 61.92; H, 9.30; N, 12.81; O, 15.96
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CAS # |
83602-39-5
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Appearance |
White Solid powder
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SMILES |
CC[C@H]1C(=O)N(CC(=O)N([C@H](C(=O)N[C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N([C@@H](C(=O)N([C@H](C(=O)N1)[C@@H]([C@H](C)C/C=C/C)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C
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InChi Key |
PMATZTZNYRCHOR-JLPRAAIDSA-N
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InChi Code |
InChI=1S/C62H111N11O12/c1-25-27-28-40(15)52(75)51-56(79)65-43(26-2)58(81)67(18)33-48(74)68(19)44(29-34(3)4)55(78)66-49(38(11)12)61(84)69(20)45(30-35(5)6)54(77)63-41(16)53(76)64-42(17)57(80)70(21)46(31-36(7)8)59(82)71(22)47(32-37(9)10)60(83)72(23)50(39(13)14)62(85)73(51)24/h25,27,34-47,49-52,75H,26,28-33H2,1-24H3,(H,63,77)(H,64,76)(H,65,79)(H,66,78)/b27-25+/t40-,41+,42-,43+,44+,45+,46+,47+,49+,50-,51+,52-/m1/s1
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Chemical Name |
(3R,6S,9S,12R,15S,18S,21S,24S,30S,33S)-30-ethyl-33-[(E,1R,2R)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone
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Synonyms |
Cyclosporin H; 5-(N-methyl-D-valine)-Cyclosporin A; Sandoz 37-839
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~100 mg/mL (~83.2 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 3 mg/mL (2.49 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 3 mg/mL (2.49 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.