Alprostadil (Synonyms: Prostaglandin E1, PGE1;Prostaglandin E1) |
| Catalog No.GC17347 |
Alprostadil은 프로스태노이드 수용체와 결합하는 리간드로 EP3, EP4, EP2, IP 및 EP1 수용체에 대해 각각 1.1 nM, 2.1 nM, 10 nM, 33 nM, 36 nM의 결합 친화도 Kis를 나타낸다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 745-65-3
Sample solution is provided at 25 µL, 10mM.
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Alprostadil은 프로스태노이드 수용체와 결합하는 리간드로 EP3, EP4, EP2, IP 및 EP1 수용체에 대해 각각 1.1 nM, 2.1 nM, 10 nM, 33 nM, 36 nM의 결합 친화도 Kis를 나타낸다. Alprostadil은 플레이텟 집단화와 옌젠 A2 생산을 억제하고 유전 및 신장 기능 보호의 효과가 있다 [1-3].
Alprostadil (0.1-50 ng/ml; 8-26시간)은 HUVEC 세포에서 eNOS와 VEGF 단백질 및 mRNA 표현을 상향 조절하고 HIF-1α를 감소시킨다[4]. Alprostadil (10 ng/mL; 24시간)은 낮은 산소 유도 인자 1α를 규율하여 폐동맥고혈압에서 메센치멜 스템 셀의 조사포토시스를 줄이고 귀농을 향상시킨다[5].
Alprostadil (5 μg/kg; i.p)은 JAK2/STAT3 신호 경로를 억제하여 팬크레아 조직 손상을 줄이고 팬크레아 세포 조사포토시스를 연기시키고 인플러멜토리와 항산화를 줄여서 급성 팬크레아티스 대쥐 모델에서 팬크레아를 보호한다[6]. Alprostadil (0.3125, 0.625, 1.25 mg/kg/일; i.p)은 E-prostanoid (EP) 3 수용체 활성화와 Netrin-1의 상향 조절을 통해 AngII 유도의 심비대를 완화시킨다[7].
References:
[1]. Kiriyama M, Ushikubi F, et,al. Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1997 Sep;122(2):217-24. doi: 10.1038/sj.bjp.0701367. PMID: 9313928; PMCID: PMC1564924.
[2]. Cattaneo MG, Pola S, et,al. Alprostadil suppresses angiogenesis in vitro and in vivo in the murine Matrigel plug assay. Br J Pharmacol. 2003 Jan;138(2):377-85. doi: 10.1038/sj.bjp.0705051. PMID: 12540529; PMCID: PMC1573673.
[3]. Hauck EW, Altinkilic BM, et,al. Prostaglandin E1 long-term self-injection programme for treatment of erectile dysfunction--a follow-up of at least 5 years. Andrologia. 1999;31 Suppl 1:99-103. doi: 10.1111/j.1439-0272.1999.tb01458.x. PMID: 10643527.
[4]. Haider DG, Bucek RA, et,al. PGE1 analog alprostadil induces VEGF and eNOS expression in endothelial cells. Am J Physiol Heart Circ Physiol. 2005 Nov;289(5):H2066-72. doi: 10.1152/ajpheart.00147.2005. Epub 2005 Jun 10. PMID: 15951350.
[5]. Jiang DT, Tuo L, et,al. Prostaglandin E1 reduces apoptosis and improves the homing of mesenchymal stem cells in pulmonary arterial hypertension by regulating hypoxia-inducible factor 1 alpha. Stem Cell Res Ther. 2022 Jul 16;13(1):316. doi: 10.1186/s13287-022-03011-x. PMID: 35842683; PMCID: PMC9288720.
[6]. Fei S, Li W, et,al. Protective Effect of Alprostadil on Acute Pancreatitis in Rats via Inhibiting Janus Kinase 2 (JAK2)/STAT3 Signal Transduction Pathway. Med Sci Monit. 2019 Oct 13;25:7694-7701. doi: 10.12659/MSM.919148. PMID: 31606729; PMCID: PMC6807527.
[7]. Shen Y, Wang X, et,al. Prostaglandin E1 attenuates AngII-induced cardiac hypertrophy via EP3 receptor activation and Netrin-1upregulation. J Mol Cell Cardiol. 2021 Oct;159:91-104. doi: 10.1016/j.yjmcc.2021.06.009. Epub 2021 Jun 18. PMID: 34147480.
| 세포 실험 [1]: | |
세포 라인 | 인간 삭주동맥 내피세포(HUVEC) |
제조 방법 | Alprostadil은 정상 산소 조건에서 HUVEC와 8시간 동안 0.1, 1.0, 5.0, 10.0 또는 50.0 ng/ml로 배양되었습니다.세포는 정상 산소 또는 저산소 조건(6% O2-94% N2)에서 추가로 12 또는 18시간 동안 알프로스태딜의존하여 노출되었습니다. |
반응 조건 | 0.1-50 ng/ml; 8-26시간 동안 |
응용 분야 | Alprostadil과의 배양은 정상 산소 조건에서 eNOS와 VEGF의 mRNA 표현을 도스 의존적으로 상향 조절하고 HIF-1α 표현을 하향 조절했습니다. 저산소 조건에 비해 HUVEC의 저산소 노출은 eNOS, VEGF 및 HIF-1α의 mRNA와 단백질을 증가시켰습니다. |
| 동물 실험 [2]: | |
동물 모형 | 수컷 Sprague-Dawley 쥐 (급성 췌장염 모델) |
제조 방법 | 쥐는AP 모델링 30분 전에 Alprostadil 5 μg/kg을 복강 내 주사로 투여되었습니다. 48시간 후에 쥐는 희생되었습니다. |
제형 | 5 ug/kg; i.p |
응용 분야 | Alprostadil은 산화 스트레스를 줄이고 프로염증성 사이토카인 분비를 억제할 수 있습니다. |
참고문헌: [1]. Haider DG, Bucek RA, et,al. PGE1 analog alprostadil induces VEGF and eNOS expression in endothelial cells. Am J Physiol Heart Circ Physiol. 2005 Nov;289(5):H2066-72. doi: 10.1152/ajpheart.00147.2005. Epub 2005 Jun 10. PMID: 15951350.[2]. Fei S, Li W, et,al. Protective Effect of Alprostadil on Acute Pancreatitis in Rats via Inhibiting Janus Kinase 2 (JAK2)/STAT3 Signal Transduction Pathway. Med Sci Monit. 2019 Oct 13;25:7694-7701. doi: 10.12659/MSM.919148. PMID: 31606729; PMCID: PMC6807527. | |
| Cas No. | 745-65-3 | SDF | |
| Synonyms | Prostaglandin E1, PGE1;Prostaglandin E1 | ||
| Chemical Name | 7-[(1R,2R,3R)-3-hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-5-oxocyclopentyl]heptanoic acid | ||
| Canonical SMILES | CCCCCC(C=CC1C(CC(=O)C1CCCCCCC(=O)O)O)O | ||
| Formula | C20H34O5 | M.Wt | 354.48 |
| Solubility | ≥ 13.4mg/mL in DMSO | Storage | Store at -20°C, stored under nitrogen,unstable in solution, ready to use. |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.821 mL | 14.1052 mL | 28.2103 mL |
| 5 mM | 564.2 μL | 2.821 mL | 5.6421 mL |
| 10 mM | 282.1 μL | 1.4105 mL | 2.821 mL |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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