Ac-pGlu-OH | 53971-11-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Ac-pGlu-OH
• 英文别名: (RS)-Ac-
• CAS: 53971-11-2
• 化学式: C₇H₉NO₄
• 分子量: 171.153
• InChiKey: AYNBBSMJRSAAHP-UHFFFAOYSA-N

物化性质

• 沸点：
  399.9±35.0 °C(Predicted)
• 密度：
  1.428±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  74.7
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2933790090

反应信息

• 作为反应物：
  描述：

  Ac-pGlu-OH 在 porcine kidney acylase I 氢氧化钾 、 potassium phosphate buffer 作用下， 生成 N-Acetyl-D-pyroglutamic acid 、 L-焦谷氨酸
  参考文献：
  名称：

  Kinetic resolution of unnatural and rarely occurring amino acids: enantioselective hydrolysis of N-acyl amino acids catalyzed by acylase I

  摘要：

  DOI：

  10.1021/ja00198a055
• 作为产物：
  描述：

  乙酸酐 、 DL-焦谷氨酸 反应 0.25h， 以72%的产率得到Ac-pGlu-OH
  参考文献：
  名称：

  Amino Acid Derivatives with Anticonvulsant Activity.

  摘要：

  一系列N-烷基化、N-酰基化或自由的九环和一个直链氨基酸的苄胺衍生物作为潜在的抗癫痫药物已被合成。所得化合物的结构设计基于先前确定的结构和物理化学性质/抗癫痫活性关系，这是根据以前合成的这类化合物而设计的。通过腹腔注射(ip)给药后的小鼠，通过最大电惊厥发作测试(MES测试)、皮下(sc)戊四氮测试(sc PTZ测试)以及通过旋转棒神经毒性测试(Tox测试)对所得化合物进行评估。结果是根据它们在国家卫生研究院(NIH)的抗癫痫药物开发计划(ADDP)中的抗癫痫筛查项目(ASP)中的分类，分为三种类别之一。选取的三种化合物在口服给药后的大鼠中进行了定量测试。确定了MES ED50、sc PTZ ED50、Tox TD50并计算了它们的保护指数(PI)值。最有希望的化合物(15)在不同癫痫模型中的抗癫痫活性被检查。该化合物的相应ED50和PI值如下：对抗苯二氯酮，73和1.4；对抗戊四氮，47和2.2；对抗士的宁，73和1.4；对抗毛果芸香碱，156和0.7；对抗海人藻酸(2-羧基-4-异丙烯基-3-吡咯烷乙酸)，39和2.6；对抗AMPA(α-氨基-3-羟基-5-甲基-4-异噁唑丙酸)，10和10.3；对抗NMDA(N-甲基-D-天冬氨酸)，114和0.9。

  DOI：

  10.1248/cpb.49.629

文献信息

• N-acetylamino acids, related N-acetyl compounds and their topical use
  申请人：——

  公开号：US20030198656A1

  公开（公告）日：2003-10-23

  Compositions comprising N-acetylamino acids and/or related N-acetyl compounds are useful to alleviate or improve various cosmetic conditions and dermatological disorders, including changes or damage to skin, nail and hair associated with intrinsic aging and/or extrinsic aging, as well as changes or damage caused by extrinsic factors. The N-acetylamino acid and/or related N-acetyl compound composition may further comprise a cosmetic, pharmaceutical or other topical agent to enhance or create synergetic effects.

  由 N-乙酰基氨基酸和/或相关 N-乙酰基化合物组成的组合物可用于缓解或改善各种美容状况和皮肤病，包括与内在老化和/或外在老化相关的皮肤、指甲和头发的变化或损伤，以及由外在因素引起的变化或损伤。N-acetylamino acid 和/或相关 N-acetyl 化合物组合物可进一步包含化妆品、药物或其他外用制剂，以增强或产生协同效应。
• N-acetyl cysteine and its topical use
  申请人：——

  公开号：US20030229141A1

  公开（公告）日：2003-12-11

  Methods to alleviate or improve various cosmetic conditions and dermatological disorders, including changes or damage to skin, nail and hair associated with intrinsic aging and/or extrinsic aging, as well as changes or damage caused by extrinsic factors using compositions comprising N-acetyl-cysteine (isomeric or non-isomeric forms) and/or free acid, salt, lactone, amide or ester forms of N-acetyl-cysteine are described. The methods provided may also comprise application of a composition further containing various cosmetic, pharmaceutical or other topical agents to enhance or create synergetic effects.

  本文描述了使用包含 N-乙酰-半胱氨酸（异构体或非异构体形式）和/或 N-乙酰-半胱氨酸的游离酸、盐、内酯、酰胺或酯形式的组合物来缓解或改善各种美容状况和皮肤病的方法，包括与内在老化和/或外在老化相关的皮肤、指甲和头发的变化或损伤，以及外在因素引起的变化或损伤。所提供的方法还可包括使用进一步含有各种化妆品、药物或其他外用制剂的组合物，以增强或产生协同效应。
• NOVEL CARBAMATE AMINO ACID AND PEPTIDE PRODRUGS OF OPIATES AND USES THEREOF
  申请人：Franklin Richard

  公开号：US20120270847A1

  公开（公告）日：2012-10-25

  Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid pro-drug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.
• US6808716B2
  申请人：——

  公开号：US6808716B2

  公开（公告）日：2004-10-26
• [EN] N-ACETYLAMINO ACIDS, RELATED N-ACETYL COMPOUNDS AND THEIR TOPICAL USE<br/>[FR] ACIDES N-ACETYLAMINES, COMPOSES DE N-ACETYLES ET LEUR UTILISATION TOPIQUE
  申请人：YU RUEY J

  公开号：WO2004089329A2

  公开（公告）日：2004-10-21

  Compositions comprising N-acetylamino acids and/or related N-acetyl compounds are useful to alleviate or improve various cosmetic conditions and dermatological disorders, including changes or damage to skin, nail and hair associated with intrinsic aging and/or extrinsic aging, as well as changes or damage caused by extrinsic factors. The N-acetylamino acid and/or related N-acetyl compound composition may further comprise a cosmetic, pharmaceutical or other topical agent to enhance or create synergetic effects.