1. GPCR/G Protein
  2. Vasopressin Receptor
  3. Selepressin

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.

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Selepressin

Selepressin Estructura química

No. CAS : 876296-47-8

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
1 mg En stock
5 mg En stock
10 mg En stock
50 mg   Obtener un presupuesto  
100 mg   Obtener un presupuesto  

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Descripciòn

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[1][2][4].

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
0.55 1
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]
CHO-K1 EC50
1100 1
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]
CHO-K1 EC50
1100 1
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]
HEK293 EC50
2.4 1
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]
Flp-In-293 EC50
340 1
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]
Flp-In-293 EC50
340 1
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]
Flp-In-293 EC50
340 1
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 1
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
0.55 1
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]
CHO-K1 EC50
1100 1
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]
HEK293 EC50
2.4 1
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
2.4 1
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 1
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]
HEK293 EC50
2700 1
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]
HEK293 EC50
2700 1
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]
In Vitro

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.

Western Blot Analysis[2]

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.
In Vivo

Selepressin (1 μg/kg/min, left jugular vein infusion for 12 min) increases 38.5% of the mean arterial pressure (MAP) in LPS-induced, fluid-resuscitated rabbit endotoxemia model[2].
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.
Peso molecular

1048.28

Fòrmula

C46H73N13O11S2

No. CAS
Appearance

Solid

Color

White to off-white

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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)

Solvente y solubilidad
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9539 mL 4.7697 mL 9.5394 mL
5 mM 0.1908 mL 0.9539 mL 1.9079 mL
View the 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.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación

Purity: 98.17%

Referencias

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
Selepressin
Cat. No.:
HY-105239
Cantidad:
MCE Japan Authorized Agent: