中文名 | 环孢菌素 H |
英文名 | Cyclosporin H |
别名 | 环孢素H 环孢菌素H 环胞霉素B 环孢霉素H 环孢菌素 H 环孢素杂质8 环孢菌素杂质H 环孢素H, 来源于小单孢菌 环[L-丙氨酰-D-丙氨酰-N-甲基-L-亮氨酰-N-甲基-L-亮氨酰-N-甲基-L-缬氨酰-3-羟基-N,4-二甲基-L-2-氨基-6-辛烯酰-L-2-氨基丁酰-N-甲基甘氨酰-N-甲基-L-亮氨酰-L-缬氨酰-N-甲基-L-亮氨酰] |
英文别名 | CS-1741 CS-1030 CYCLOSPORIN H Sandoz 37-839 Cyclosporin H 5-(N-Methyl-D-valine)cyclosporin A Cyclo[L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-D-valyl-3-hydroxy-N,4-dimethyl-L-2-amino-6-octenoyl-L-2-aminobutanoyl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl] Cyclo[L-alanyl-D-alanyl-N-Methyl-L-leucyl-N-Methyl-L-leucyl-N-Methyl-D-valyl-(3R,4R,6E)-6,7-didehydro-3-hydroxy-N,4-diMethyl-L-2-aMinooctanoyl-L-2-aMinobutanoyl-N-Methylglycyl-N-Methyl-L-leucyl-L-valyl-N-Methyl-L-leucyl] (3S,6S,9R,12R,15S,18S,21R,24S,30S)-30-ethyl-33-[(1R,2R,4E)-1-hydroxy-2-methylhex-4-en-1-yl]-1,4,7,10,12,15,19,22,25,28-decamethyl-3,21-bis(1-methylethyl)-6,9,18,24-tetrakis(2-methylpropyl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone |
CAS | 83602-39-5 |
化学式 | C62H111N11O12 |
分子量 | 1202.61 |
InChI | InChI=1/C63H113N11O12/c1-26-28-29-41(15)53(76)52-56(79)66-44(27-2)58(81)67(18)34-49(75)68(19)46(31-36(5)6)60(83)72(23)50(39(11)12)62(85)69(20)45(30-35(3)4)55(78)64-42(16)54(77)65-43(17)57(80)70(21)47(32-37(7)8)59(82)71(22)48(33-38(9)10)61(84)73(24)51(40(13)14)63(86)74(52)25/h26,28,35-48,50-53,76H,27,29-34H2,1-25H3,(H,64,78)(H,65,77)(H,66,79)/b28-26+/t41-,42+,43-,44+,45+,46+,47-,48+,50-,51+,52?,53-/m1/s1 |
密度 | 1.016±0.06 g/cm3(Predicted) |
熔点 | 148-151°C |
沸点 | 1293.8±65.0 °C(Predicted) |
闪点 | 729.1°C |
蒸汽压 | 0mmHg at 25°C |
溶解度 | 氯仿 (微溶),甲醇 (微溶,加热,超声处理) |
折射率 | 1.468 |
酸度系数 | 13.32±0.70(Predicted) |
存储条件 | -20°C |
外观 | 粉末 |
颜色 | white to beige |
体外研究 | The cyclic undecapeptide, cyclosporin H, is a potent inhibitor of formyl-Met-Leu-Phe (FMLP)-induced superoxide anion (O2-) formation in human neutrophils. Cyclosporin H inhibits FMLP binding in HL-60 membranes with a K i of 0.1 μM. Cyclosporin H inhibits 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 K i of 0.79 μM. Cyclosporin H inhibits the stimulatory effects of FMLP on cytosolic Ca 2+ concentration ([Ca 2+ ]i), O2- formation, and beta-glucuronidase release with K i values of 0.08, 0.24, and 0.45 μM, respectively. |
体内研究 | Cyclosporin H (5 mg/kg; i.p.; before LPS or HCl challenge) attenuats lung injury induced by LPS or HCl (a lung injurymodel). |
海关编号 | 29420000 |
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