| Bioactivity | PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca2+-dependent large-conductance K+-channel in human myometrial cells[1][2]. | ||||||
| Invitro | PDC31（10 μM, 50 μM）刺激人子宫肌层平滑肌细胞中的 BKCa 通道，并在 10 μM 和 50 μM 条件下，分别将开放状态通道活性平均提高 4 倍和 6 倍[2]。PDC31（1 nM-10 μM；20 分钟间隔）累积抑制离体妊娠人子宫肌层的自发收缩[2]。PDC31 由位于人类 PGF2a 受体的跨膜结构域的 ILGHXDYK 序列组成[3]。在肌条模型中，PDC31可减少 PGF2a 诱导的收缩持续时间和强度，并可延迟早产动物模型的分娩[4]。 | ||||||
| Name | PDC31 | ||||||
| CAS | 634586-40-6 | ||||||
| Sequence | d-(Ile-Leu-Gly-His-Cit-Asp-Tyr-Lys) | ||||||
| Shortening | d-(ILGHXDYK) | ||||||
| Formula | C45H71N13O13 | ||||||
| Molar Mass | 1002.12 | ||||||
| Appearance | Solid | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage | Sealed storage, away from moisture and light, under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen) |
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| Reference | [1]. Sharif NA, et al. Prostaglandin FP receptor antagonists: discovery, pharmacological characterization and therapeutic utility. Br J Pharmacol. 2019 Apr;176(8):1059-1078. [2]. Doheny HC, et al. THG113.31, a specific PGF2alpha receptor antagonist, induces human myometrial relaxation and BKCa channel activation. Reprod Biol Endocrinol. 2007 Mar 16;5:10. [3]. Friel AM, et al. Specific PGF(2alpha) receptor (FP) antagonism and human uterine contractility in vitro. BJOG. 2005 Aug;112(8):1034-42. [4]. Böttcher B, et al. A first-in-human study of PDC31 (prostaglandin F2α receptor inhibitor) in primary dysmenorrhea. Hum Reprod. 2014 Nov;29(11):2465-73. |