Selepressin
Based on 1 Customer Validation
Selepressin (FE 202158) is a selective vasopressin V1A receptor agonist. Selepressin is a potent vasopressor. Selepressin can be used in the research of septic shock.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 98.17%
- CAS 番号: 876296-47-8
- 分子式: C46H73N13O11S2
- 分子量:1048.28
-
保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Vasopressin Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
1100 nM
Compound: 45, FE 202158
|
Agonist activity at human OT receptor expressed in CHO-K1 cells by luciferase reporter gene assay
Agonist activity at human OT receptor expressed in CHO-K1 cells by luciferase reporter gene assay
|
[PMID: 21688787] |
| Flp-In-293 | EC50 |
340 nM
Compound: 45, FE 202158
|
Agonist activity at recombinant human vasopressin V1b receptor expressed in Flp-In-293 cells by luciferase reporter gene assay
Agonist activity at recombinant human vasopressin V1b receptor expressed in Flp-In-293 cells by luciferase reporter gene assay
|
[PMID: 21688787] |
| HEK293 | EC50 |
0.55 nM
Compound: 45, FE 202158
|
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
|
[PMID: 21688787] |
| HEK293 | EC50 |
2.4 nM
Compound: 45, FE 202158
|
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
|
[PMID: 21688787] |
| HEK293 | EC50 |
2700 nM
Compound: 45, FE 202158
|
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
|
[PMID: 21688787] |
Selepressin (100 nM, 48 or 72 h) ameliorates thrombin or VEGF-induced HLMVECs barrier dysfunction[4].
Selepressin (1-1000 nM, 72 h) prevents the LPS-Induced loss of VE-cadherin and cortical actin in HLMVECs[4].
Selepressin (100 nM, 48 h) induces the expression of the barrier-protective p53 in HLMVECs[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HLMVECs
-
Concentration:1, 10, 100, 1000 nM
-
Incubation Time:24 h, 48 h
-
Result:Induced p53 expression levels, but only after treatment of 48 hours at 100 nM.
Selepressin (7 pmol/kg/min, 10 μL/min, i.v. infusion) blocks vascular leak in ovine severe sepsis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:LPS-induced, fluid-resuscitated rabbit endotoxemia model[2].
-
Dosage:1 μg/kg/min
-
Administration:Left jugular vein infusion for 12 min
-
Result:Decreased mesenteric blood flow (MBF) and increased mesenteric vascular resistance in non-endotoxemic and endotoxemic rabbits.
化学情報
-
CAS 番号 876296-47-8
-
性状 Solid
-
分子量 1048.28
-
分子式 C46H73N13O11S2
-
Color White to off-white
-
別名
FE 202158
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (95.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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
-
データシート (280 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Russell JA, et al. Selepressin, a novel selective vasopressin V1A agonist, is an effective substitute for norepinephrine in a phase IIa randomized, placebo-controlled trial in septic shock patients. Crit Care. 2017 Aug 15;21(1):213. [Content Brief]
[2]. Milano SP, et al. Selepressin, a novel selective V1A receptor agonist: Effect on mesenteric flow and gastric mucosa perfusion in the endotoxemic rabbit. Peptides. 2020 Jul;129:170318. [Content Brief]
[3]. Barabutis N, et al. Protective Mechanism of the Selective Vasopressin V1A Receptor Agonist Selepressin against Endothelial Barrier Dysfunction. J Pharmacol Exp Ther. 2020 Nov;375(2):286-295. [Content Brief]
[4]. Maybauer MO, et al. The selective vasopressin type 1a receptor agonist selepressin (FE 202158) blocks vascular leak in ovine severe sepsis*. Crit Care Med. 2014 Jul;42(7):e525-e533. [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). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9539 mL | 4.7697 mL | 9.5394 mL | 23.8486 mL |
| 5 mM | 0.1908 mL | 0.9539 mL | 1.9079 mL | 4.7697 mL | |
| 10 mM | 0.0954 mL | 0.4770 mL | 0.9539 mL | 2.3849 mL | |
| 15 mM | 0.0636 mL | 0.3180 mL | 0.6360 mL | 1.5899 mL | |
| 20 mM | 0.0477 mL | 0.2385 mL | 0.4770 mL | 1.1924 mL | |
| 25 mM | 0.0382 mL | 0.1908 mL | 0.3816 mL | 0.9539 mL | |
| 30 mM | 0.0318 mL | 0.1590 mL | 0.3180 mL | 0.7950 mL | |
| 40 mM | 0.0238 mL | 0.1192 mL | 0.2385 mL | 0.5962 mL | |
| 50 mM | 0.0191 mL | 0.0954 mL | 0.1908 mL | 0.4770 mL | |
| 60 mM | 0.0159 mL | 0.0795 mL | 0.1590 mL | 0.3975 mL | |
| 80 mM | 0.0119 mL | 0.0596 mL | 0.1192 mL | 0.2981 mL |