1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. Evatanepag

Evatanepag  (Synonyms: CP-533536 free acid)

Cat. No.: HY-14839 Pureza: 98.58%
Instrucciones de manejo Technical Support

Evatanepag (CP-533536) is a non-prostanoid, potent and selective EP2 receptor agonist. Evatanepag can induce local bone formation in vivo. Evatanepag can be used in the research of fractures, bone defects, asthma.

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Evatanepag

Evatanepag Estructura química

No. CAS : 223488-57-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
En stock
Solution
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Revisión del cliente

Based on 2 publication(s) in Google Scholar

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Descripciòn

Evatanepag (CP-533536) is a non-prostanoid, potent and selective EP2 receptor agonist. Evatanepag can induce local bone formation in vivo. Evatanepag can be used in the research of fractures, bone defects, asthma[1][2].

IC50 & Target[1]

EP2

 

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
0.3 nM
Compound: 7f, CP-533536
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
[PMID: 19250823]
HEK293 IC50
>3200 nM
Compound: 7f, CP-533536
Inhibition of rat EP4 receptor expressed in HEK293 cells
Inhibition of rat EP4 receptor expressed in HEK293 cells
[PMID: 19250823]
HEK293 IC50
50 nM
Compound: 7f, CP-533536
Inhibition of rat EP2 receptor expressed in HEK293 cells
Inhibition of rat EP2 receptor expressed in HEK293 cells
[PMID: 19250823]
In Vitro

Evatanepag (10 nM, 30 min) inhibits hFcεRI-induced mast cells degranulation in a dose-dependent manner[2].
Evatanepag (0.1 nM-10 μM, 12 min) results in an equivalent increase in intracellular cAMP in HEK-293 cells, with an IC50 of 50 nM[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Evatanepag (0.3-3.0 mg/kg, directly injected into the marrow cavity of the tibia) promotes bone formation in rats[1].
Evatanepag (0.3, 3.0 mg/kg, intranasal administration, from day1 to day4) reduces HDM aeroallergen-induced increased RL response to methacholine in mice[2].
Evatanepag (1 mg/kg, intravenous injection) demonstrates high i.v. clearance (Cl: 56 mL/min/kg) and a short half-life (t1/2: 0.33 h)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats[1]
Dosage: 0.3, 1.0, 3.0 mg/kg
Administration: Directly injected into the marrow cavity of the tibia
Result: Dose-dependently increased in bone area, bone mineral content, bone mineral density.
Animal Model: HDM (house dust mite)-sensitized BALB/c mice[2]
Dosage: 0.3 mg/kg, 3 mg/kg
Administration: Intranasal administration, from day1 to day4
Result: Prevented aeroallergen-driven increased RL (lung resistance) at 0.3 mg/kg.
Prevented the enhanced MC activity by approximately 48% at 3 mg/kg.
Peso molecular

468.57

Fòrmula

C25H28N2O5S

No. CAS
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(C)C(C=C1)=CC=C1CN(S(C2=CN=CC=C2)(=O)=O)CC3=CC(OCC(O)=O)=CC=C3

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : ≥ 32 mg/mL (68.29 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 2.1342 mL 10.6708 mL 21.3415 mL
5 mM 0.4268 mL 2.1342 mL 4.2683 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1342 mL 10.6708 mL 21.3415 mL 53.3538 mL
5 mM 0.4268 mL 2.1342 mL 4.2683 mL 10.6708 mL
10 mM 0.2134 mL 1.0671 mL 2.1342 mL 5.3354 mL
15 mM 0.1423 mL 0.7114 mL 1.4228 mL 3.5569 mL
20 mM 0.1067 mL 0.5335 mL 1.0671 mL 2.6677 mL
25 mM 0.0854 mL 0.4268 mL 0.8537 mL 2.1342 mL
30 mM 0.0711 mL 0.3557 mL 0.7114 mL 1.7785 mL
40 mM 0.0534 mL 0.2668 mL 0.5335 mL 1.3338 mL
50 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0671 mL
60 mM 0.0356 mL 0.1778 mL 0.3557 mL 0.8892 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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Nombre del producto:
Evatanepag
Cat. No.:
HY-14839
Cantidad:
MCE Japan Authorized Agent: