1. GPCR/G Protein
  2. Prostaglandin Receptor

OBE022 

Cat. No.: HY-112284
Handling Instructions

OBE022 is an oral and selective prostaglandin F (PGF) receptor antagonist, with Kis of 1 nM, 26 nM for human and rat FP receptors, respectively.

For research use only. We do not sell to patients.

OBE022 Chemical Structure

OBE022 Chemical Structure

CAS No. : 2005486-31-5

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Description

OBE022 is an oral and selective prostaglandin F (PGF) receptor antagonist, with Kis of 1 nM, 26 nM for human and rat FP receptors, respectively.

IC50 & Target[1]

Human FP Receptor

1 nM (Ki)

Rat FP Receptor

26 nM (Ki)

In Vitro

OBE022 and OBE002 are assayed for FP binding affinity by competitive binding analysis with 3H-PGF2α using HEK293 cells stably transfected with the FP receptor. Binding affinities (Ki) of OBE022 for the human and rat FP receptor are 1 nM and 26 nM respectively. For OBE002, Kis are 6 nM for the human and 313 nM for the rat FP receptor. The binding of both OBE022 and OBE002 is reversible and competitive since increasing concentrations of either compound causes successive decreases in the slope of the binding curves, consistent with an increase in equilibrium dissociation constant (KD) without a reduction in receptor density[1].

In Vivo

Time-course of the cumulative percentage of delivers mice after RU486-induced preterm parturition at GD17, in OBE022, nifedipine or vehicle treatment groups. Oral treatment with OBE022 delays the preterm birth caused by RU486 administration as reflected by a shift to the right of the percentage of delivery curve. The effect of oral treatment with nifedipine is comparable. Both OBE022 and nifedipine show a trend to increase the time of first pup delivery. As an important consequence of the prolongation of gestation, dams deliver viable pups. Combination of OBE022 and nifedipine cause a synergistic effect on the delay of RU486-induced preterm birth as reflected by a more pronounced shift to the right of the percentage of delivery curve, in comparison to OBE022 or nifedipine alone. Also, a larger increase of the time of first pup delivery is observed[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6674 mL 8.3369 mL 16.6739 mL
5 mM 0.3335 mL 1.6674 mL 3.3348 mL
10 mM 0.1667 mL 0.8337 mL 1.6674 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
Primigravid CD1 mice, on day 17 of pregnancy (about 85% gestation) at the beginning of the experiments, are used. Approximately 3 hours before induction of preterm labor (Day 1 (D1) at 10h00), the pregnant mice at gestational day 17, are placed in individual cages with food and water ad libitum. Pregnant mice receive on D1 (at day time: 13h00) a single subcutaneous (s.c.) injection of RU486 at a dose of 2.5 mg/kg in a final volume of 10 mL/kg of sesame oil. OBE022 (10, 30 and 100 mg/kg) or nifedipine (5 mg/kg) are administered orally (p.o.) at a volume of 5 mL/kg once on D1 (18h00), twice on D2 (8h00 and 18h00) and once on D3 (8h00) for a total of 4 administrations. For combination treatment, mice receive OBE022 plus nifedipine using the same experimental design as single treatment[1].

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

References
Molecular Weight

599.74

Formula

C₃₀H₃₄FN₃O₅S₂

CAS No.

2005486-31-5

SMILES

O=C(N[[email protected]](C1=CC=C(F)C=C1)CCOC([[email protected]](C(C)C)N)=O)[[email protected]](SCC2)N2S(C(C=C3)=CC=C3C4=CC=CC=C4)(=O)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
OBE022
Cat. No.:
HY-112284
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OBE022

Cat. No.: HY-112284