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83602-39-5

中文名稱 環(huán)孢菌素 H
英文名稱 Cyclosporin H
CAS 83602-39-5
分子式 C62H111N11O12
分子量 1202.61
MOL 文件 83602-39-5.mol
更新日期 2024/12/23 09:09:19
83602-39-5 結(jié)構(gòu)式 83602-39-5 結(jié)構(gòu)式

基本信息

中文別名
環(huán)孢素H
環(huán)胞霉素B
環(huán)孢霉素H
環(huán)孢菌素 H
環(huán)孢菌素雜質(zhì)H
環(huán)孢素H, 來源于小單孢菌
環(huán)[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-纈氨酰-3-羥基-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-纈氨酰-N-甲基-L-亮氨酰]
英文別名
Sandoz 37-839
CYCLOSPORIN H
Cyclosporin H, >=95%
Cyclosporine IMpurity-H
5-(N-Methyl-D-valine)cyclosporin A
Cyclosporin H, froM MicroMonospora
5-(N-Methyl-D-valine)cyclosporine 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]
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)148-151°C
沸點(diǎn)1293.8±65.0 °C(Predicted)
密度1.016±0.06 g/cm3(Predicted)
儲存條件-20°C
儲存條件-20°C冷凍
溶解度氯仿(微溶)、甲醇(微溶、加熱、超聲處理)
酸度系數(shù)(pKa)13.32±0.70(Predicted)
形態(tài)粉末
顏色白色至米色
旋光性 (optical activity)[α]/D -100 to -115°, c = 0.5 in methanol

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS07,GHS08
警示詞危險(xiǎn)
危險(xiǎn)性描述H302-H350-H360
海關(guān)編碼29420000

常見問題列表

生物活性
Cyclosporin H 是 FPR-1 (甲酰肽受體 1) 的選擇性強(qiáng)效抑制劑。Cyclosporin H 是一種病毒轉(zhuǎn)導(dǎo) (viral transduction) 增強(qiáng)劑,可使人臍帶血來源的造血干細(xì)胞和祖細(xì)胞 (HSPCs) 中慢病毒轉(zhuǎn)導(dǎo)增強(qiáng) 10 倍。Cyclosporin H 與雷帕霉素 (HY-10219) 或前列腺素 E2 (HY-101952) 聯(lián)合使用時(shí)表現(xiàn)出累加效應(yīng)。Cyclosporin H 缺乏 Cyclosporin A 具有的免疫抑制活性。
體外研究

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.

體內(nèi)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).

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