PDC31
Based on 1 Customer Validation
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.67%
- CAS 番号: 634586-40-6
- 分子式: C45H71N13O13
- 分子量:1002.12
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保管条件:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
生物活性
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FP Receptor ~30 nM (Ki) |
PGF2α |
PDC31 (10 μM, 50 μM; ) stimulates the BKCa channel in human myometrial smooth muscle cells, and enhances open state channel activity with average 4 and 6-fold by 10 and 50 μM, respectively[2].
PDC31 (1 nM-10 μM; 20 min intervals) cumulatively inhibits spontaneous contractions in isolated pregnant human myometrium[2].
PDC31 consists of ILGHXDYK, associated sequence is based on a transmembrane domain of the human PGF2a receptor[3]. PDC31 has been shown to reduce the duration and strength of PGF2a-induced contractions in myometrial strip models and to delay delivery in animal models of preterm labor[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 634586-40-6
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性状 Solid
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分子量 1002.12
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分子式 C45H71N13O13
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Color White to off-white
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別名
THG113.31; ILGHXDYK
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配列
d-(Ile-Leu-Gly-His-Cit-Asp-Tyr-Lys)
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シーケンスの短縮
d-(ILGHXDYK)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
溶剤 & 溶解度
H2O : 100 mg/mL (99.79 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
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- Español - ES (254 KB)
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- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Sharif NA, et al. Prostaglandin FP receptor antagonists: discovery, pharmacological characterization and therapeutic utility. Br J Pharmacol. 2019 Apr;176(8):1059-1078. [Content Brief]
[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. [Content Brief]
[3]. Friel AM, et al. Specific PGF(2alpha) receptor (FP) antagonism and human uterine contractility in vitro. BJOG. 2005 Aug;112(8):1034-42. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.9979 mL | 4.9894 mL | 9.9788 mL | 24.9471 mL |
| 5 mM | 0.1996 mL | 0.9979 mL | 1.9958 mL | 4.9894 mL | |
| 10 mM | 0.0998 mL | 0.4989 mL | 0.9979 mL | 2.4947 mL | |
| 15 mM | 0.0665 mL | 0.3326 mL | 0.6653 mL | 1.6631 mL | |
| 20 mM | 0.0499 mL | 0.2495 mL | 0.4989 mL | 1.2474 mL | |
| 25 mM | 0.0399 mL | 0.1996 mL | 0.3992 mL | 0.9979 mL | |
| 30 mM | 0.0333 mL | 0.1663 mL | 0.3326 mL | 0.8316 mL | |
| 40 mM | 0.0249 mL | 0.1247 mL | 0.2495 mL | 0.6237 mL | |
| 50 mM | 0.0200 mL | 0.0998 mL | 0.1996 mL | 0.4989 mL | |
| 60 mM | 0.0166 mL | 0.0832 mL | 0.1663 mL | 0.4158 mL | |
| 80 mM | 0.0125 mL | 0.0624 mL | 0.1247 mL | 0.3118 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.