TM30643 | 844639-56-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: TM30643
• 英文别名: Y44Qme68PZ；2-[3-[(4-fluorophenyl)sulfonylamino]-1,2,3,4-tetrahydrocarbazol-9-yl]acetic acid
• CAS: 844639-56-1
• 化学式: C₂₀H₁₉FN₂O₄S
• 分子量: 402.446
• InChiKey: NONWUVBJQKYHHO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  28
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  96.8
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  4-氟苯磺酰氯 在 lithium hydroxide 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 17.0h， 生成 TM30643
  参考文献：
  名称：

  Minor Structural Modifications Convert the Dual TP/CRTH2 Antagonist Ramatroban into a Highly Selective and Potent CRTH2 Antagonist

  摘要：

  Ramatroban, a thromboxane A(2) receptor (TP) antagonist with clinical efficacy in asthma and allergic rhinitis, was recently shown to also antagonize the prostaglandin D-2 receptor CRTH2. Here we report that minor structural changes to ramatroban result in a compound (13) with complete lack of activity on TP but sub-nanomolar potency toward CRTH2. This is the first selective CRTH2 antagonist described to date, and should prove highly valuable in further elucidating the biological significance of CRTH2.

  DOI：

  10.1021/jm049036i

文献信息

• SINGLE NUCLEOTIDE POLYMORPHIC ALLELES OF HUMAN DP-2 GENE FOR DETECTION OF SUSCEPTIBILITY TO HAIR GROWTH INHIBITION BY PGD2
  申请人：The Trustees of the University of Pennsylvania

  公开号：EP3328500A1

  公开（公告）日：2018-06-06
• COMPOSITIONS AND METHODS FOR REGULATING HAIR GROWTH
  申请人：The Trustees of the University of Pennsylvania

  公开号：US20150072963A1

  公开（公告）日：2015-03-12

  The invention relates to compositions and methods for regulating hair growth. Specifically, the invention relates to regulating hair growth by regulating the activity one of the prostaglandin D2 (PGD2) receptors, DP-2 (GPR44). Compositions and methods for regulating hair growth include inhibiting hair growth by administering a DP-2 agonist, or stimulating hair growth by administering a DP-2 antagonist.
• PTGDR-1 AND/OR PTGDR-2 ANTAGONISTS FOR PREVENTING AND/OR TREATING SYSTEMIC LUPUS ERYTHEMATOSUS
  申请人：INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM)

  公开号：US20180021302A1

  公开（公告）日：2018-01-25

  The present invention concerns a PTGDR-1 antagonist, a PTGDR-2 antagonist, a dual PTGDR-1/PTGDR-1 antagonist, or a combination of PTGDR-1 antagonist and PTGDR-2 antagonist, and pharmaceutical compositions containing them, for use for preventing and/or treating SLE.
• [EN] SINGLE NUCLEOTIDE POLYMORPHIC ALLELES OF HUMAN DP-2 GENE FOR DETECTION OF SUSCEPTIBILITY TO HAIR GROWTH INHIBITION BY PGD2<br/>[FR] ALLÈLES POLYMORPHES DE NUCLÉOTIDE UNIQUE DE GÈNE DP-2 HUMAIN POUR LA DÉTECTION DE LA SENSIBILITÉ À L'INHIBITION DE LA CROISSANCE DE CHEVEUX PAR PGD2
  申请人：UNIV PENNSYLVANIA

  公开号：WO2017019858A1

  公开（公告）日：2017-02-02

  DP-2 antagonists reversed PGD2-mediated human hair growth inhibition in a dose-dependent manner in vitro by reducing PGD2-triggered apoptosis and maintaining proliferation of keratinocytes. Hair follicles from approximately half of the alopecia patients exhibited little susceptibility to PGD2's effect in vitro. SNPs in the human DP-2 gene were identified that are associated with hair growth inhibition by PGD2. These findings underscore the role of DP-2 in regulating hair growth and indicate that DP-2 can be an effective approach in preventing and/or treating androgenetic alopecia in patients sensitive to PGD2. Furthermore, the SNPs identified here can be used to identify patients who will benefit from treatment.