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Medchemexpress/Pepstatin(Synonyms: Pepstatin A; Isovaleryl-Val-Val-Sta-Ala-Sta-OH)/HY-P0018/50mg

价格
¥1200.00
货号:HY-P0018-10mg
浏览量:90
品牌:MCE
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商品描述
Pepstatin is a potent inhibitor of aspartyl proteases, and inhibits the aspartic proteases cathepsin D, pepsin, and renin.
Description

Pepstatin is a potent inhibitor of aspartyl proteases, and inhibits the aspartic proteases cathepsin D, pepsin, and renin.

In Vivo

A low dose of pepstatin shows an inhibition of edema formation, and intraperitoneal injection of 1.25 mg/kg of pepstatin causes a 30% inhibition with a a very low toxicity[1]. Pepstatin increases LC3-II levels, while it is reverted by 3-methyladenine (3-MA)[2].

References
  • [1]. Umezawa H, et al. Pepstatin, a new pepsin inhibitor produced by Actinomycetes. J Antibiot (Tokyo). 1970 May;23(5):259-62.

    [2]. Raquel T. Lima, et al. Modulation of Autophagy by a Thioxanthone Decreases the Viability of Melanoma Cells. Molecules 2016, 21(10), 1343

Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.4580 mL 7.2898 mL 14.5796 mL
5 mM 0.2916 mL 1.4580 mL 2.9159 mL
10 mM 0.1458 mL 0.7290 mL 1.4580 mL
Please refer to the solubility information to select the appropriate solvent.
References
  • [1]. Umezawa H, et al. Pepstatin, a new pepsin inhibitor produced by Actinomycetes. J Antibiot (Tokyo). 1970 May;23(5):259-62.

    [2]. Raquel T. Lima, et al. Modulation of Autophagy by a Thioxanthone Decreases the Viability of Melanoma Cells. Molecules 2016, 21(10), 1343

Molecular Weight

685.89

Formula

C₃₄H₆₃N₅O₉

CAS No.

26305-03-3

Storage
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 25 mg/mL

* "<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity: 98.45%

Data Sheet (115 KB) SDS (389 KB)

COA (94 KB) LCMS (1269 KB)

Handling Instructions (1252 KB)
  • [1]. Umezawa H, et al. Pepstatin, a new pepsin inhibitor produced by Actinomycetes. J Antibiot (Tokyo). 1970 May;23(5):259-62.

    [2]. Raquel T. Lima, et al. Modulation of Autophagy by a Thioxanthone Decreases the Viability of Melanoma Cells. Molecules 2016, 21(10), 1343

他替瑞林口服促甲状腺素释放激素他替瑞林CAS号:103300-74-9英文名称:Taltirelin英文同义词:TA0910;Taltirelin;Taltireline;Ceredist,TA-0910;TaltirelinAcetate;TA-0910,taltirelin;TaltirelininterMediate;TALTIRELININTERMEDIATES;TaltirelinAcetate,TA-0910;L-Prolinamide,(4S)-hexahydro-1-methyl-中文名称:他替瑞林中文同义词:他替瑞林;醋酸他替瑞林;1-METHYL-4,5-DIHYDROOROTYL-HIS-PRO-NH2;(4S)-N-[(2S)-1-[(2S)-2-氨基甲酰基吡咯烷-1-基]-3-(3H-咪唑-4-基)-1-氧代丙-2-基]-1-甲基-2,6-二氧代-1,3-二氮杂己环-4-甲酰胺CBNumber:CB31177191分子式:C17H23N7O5分子量:405.41MOLFile:103300-74-9.mol化学性质安全信息用途供应商86化学性质安全信息用途供应商86他替瑞林化学性质熔点:72-75°比旋光度:25D-13.6°(c=1inwater)密度:1.447±0.06g/cm3(Predicted)储存条件:Storeat+4°C酸度系数(pKa):9.32±0.40(Predicted)安全信息他替瑞林性质、用途与生产工艺口服促甲状腺素释Chemicalbook放激素他替瑞林是一种垂体激素释放兴奋药,由日本田边三菱制药株式会社研制成功,商品名Taltirelin,属于化药新药3.1类,目前临床用于改善脊髓小脑变性患者的运动失调最为有效的药物。他替瑞林(Taltirelin)是世界上第一个批准的口服促甲状腺素释放激素(TRH),除具有内分泌作用外,还可发挥一定的中枢神经系统(CNS)作用,包括提高运动活性,拮抗利舍平诱导的体温降低,以及拮抗戊巴比妥诱导的睡眠。该品种由日本田边三菱制药株式会社开发,2000年9月首次在日本上市,用于改善脊髓小脑变性病人的共济失调。脊髓小脑共济失调(SCAs)旧称常染色体显性共济失调,是一组以共济失调、辨距不良为主要临床表现的中枢神经系统慢性变性疾病。2000年9月前,促甲状腺素释放激素(TRH)注射液是唯一用于治疗该类疾病的药物。他替瑞林是TRH的结构修饰改造药物,药理学研究显示本品经由脑TRH受体对CNS产生强而持久的多重作用。本品对CNS的兴奋作用比TRH强10~100倍,作用持续时间比TRH长约8倍。本品对TRH受体的亲和力约为TRH的1/11,因而本品的内分泌作用比TRH弱,但本品在体内比TRH稳定。另外本品对促甲状腺素(TSH)释放的作用为TRH的1/6-1/11,TSH释放是由一个包括甲状腺激素的强负反馈系统调节的,对中枢神经系统具有较强的作用,但同时其激素样作用较小,因此副作用较少。不良反应主要是消化系统反应,包括呕吐、恶心和胃不适。所有的不良反应均为轻中度,在治疗期间及(或)停药后消失。