1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. RO1138452

RO1138452 (Synonyms: CAY10441)

Cat. No.: HY-108912 Purity: 98.21%
Handling Instructions

RO1138452 is a potent and selective IP (prostacyclin) receptor antagonist. RO1138452 displays high affinity for IP receptors. In human platelets, pKi is 9.3±0.1; in a recombinant IP receptor system, pKi is 8.7±0.06.

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

RO1138452 Chemical Structure

RO1138452 Chemical Structure

CAS No. : 221529-58-4

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10 mM * 1 mL in DMSO USD 132 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

RO1138452 is a potent and selective IP (prostacyclin) receptor antagonist. RO1138452 displays high affinity for IP receptors. In human platelets, pKi is 9.3±0.1; in a recombinant IP receptor system, pKi is 8.7±0.06.

IC50 & Target

IC50: 7 nM (rat I2 receptor), 52.9 nM (rabbit PAF), 724 nM (human α2A adrenoceptor), 3280 nM (rat α1B adrenoceptor), 1450 nM (human muscarinic M4 receptor), 2220 nM (human muscarinic M2 receptor), 2570 nM (human muscarinic M1 receptor), 3110 nM (human muscarinic M5 receptor), 1130 nM (rat 5-HT1B receptor ), 1190 nM (pig 5-HT2C receptor), 3040 nM (rat 5-HT2A receptor), 8580 nM (human 5-HT1A receptor ), 8910 nM (guinea-pig 5-HT4 receptor)[1]
pKi: 5.87 (rat α1B adrenoceptor), 6.49 (human α2A adrenoceptor), 8.33 (rat I2 receptor), 5.66 (human muscarinic M1 receptor), 5.81 (human muscarinic M5 receptor), 5.88 (human muscarinic M2 receptor), 6.14 (human muscarinic M4 receptor), 7.9 (rabbit PAF), 5.35 (guinea-pig 5-HT4 receptor ), 5.37 (human 5-HT1A receptor ), 5.71 (rat 5-HT2A receptor) , 6.11 (rat 5-HT1B receptor), 6.11 (pig 5-HT2C receptor)[1]

In Vitro

RO1138452 is IP receptor antagonist. The pIC50 values of RO1138452 in attenuating cAMP accumulation is 7.0±0.07. Functional antagonism of RO1138452 is studied by measuring inhibition of carbaprostacyclin-induced cAMP accumulation in CHO-K1 cells stably expressing the human IP receptor. The antagonist affinity (pKi) of RO1138452 is 9.0±0.06. Selectivity profiles for RO1138452 are determined via a panel of receptor binding and enzyme assays. RO1138452 displays affinity at imidazoline2 (I2) (8.3) and platelet activating factor (PAF) (7.9) receptors[1]. RO1138452 (10 pM-10 μM) added to cells concurrently with a fixed concentration of Taprostene (1 μM) prevents, in a concentration-dependent manner, the inhibition of CXCL9 and CXCL10 release, with p[A]50 (molar) values of -8.73±0.11 and -8.47±0.16 (p>0.05), respectively[2].

In Vivo

RO1138452 is a potent and selective antagonist for both human and rat IP receptors and that is possesses analgesic and anti-inflammatory potential. RO1138452 (1-10 mg/kg, i.v.) significantly reduces acetic acid-induced abdominal constrictions. RO1138452 (3-100 mg/kg, p.o.) significantly reduces carrageenan-induced mechanical hyperalgesia and edema formation. One hour after administration of RO1138452 (5 mg/kg, i.v.) to rats, the total plasma concentration is 0.189  μg/mL, whereas the free plasma concentrations is calculated to be 0.009 μg/mL (28 nM)[1].

Molecular Weight

309.41

Formula

C₁₉H₂₃N₃O

CAS No.

221529-58-4

SMILES

CC(C)OC1=CC=C(CC2=CC=C(NC3=NCCN3)C=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Pure form -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (107.72 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2320 mL 16.1598 mL 32.3196 mL
5 mM 0.6464 mL 3.2320 mL 6.4639 mL
10 mM 0.3232 mL 1.6160 mL 3.2320 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.08 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (8.08 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Selectivity is determined by the ability of RO1138452 (10 μM) to displace specific binding of standard radioligands at 51 receptors. When significant displacement of radioligand is observed (>70% for RO1138452), complete concentration-dependent displacement curves (in triplicate) are constructed to generate IC50 values. Displacement binding at the EP3 receptor is performed. Enzyme inhibition assays are also conducted. RO1138452 is evaluated at 10 μM in triplicate for inhibition of COX isoforms: COX-1 (ram seminal vesicle), COX-2 (sheep placenta and human umbilical vein). Arachidonic acid is used as a substrate and PGE2 accumulation is detected[1].

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

Cell Assay
[2]

BEAS-2B cells are incubated for 30 min at 37°C in supplement-free keratinocyte serum-free medium (KSFM) in the absence and presence of 100 nM RO1138452. Cells are washed with supplement-free KSFM, incubated in the same medium for defined periods, and exposed to 1 μM Taprostene. Four hours later, cells are harvested in reporter lysis buffer, and luciferase activity is measured. The viability HAECs and BEAS-2B cells is determined colorimetrically by measuring the reduction of the tetrazolium salt MTT to formazan, by mitochondrial dehydrogenases[2].

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

Animal Administration
[1]

Rats[1]
Male Sprague-Dawley rats (n=3) are administered RO1138452 (5 mg/kg, i.v.). At various times after dose administration, the rats are anesthetized by halothane (5%), blood is collected by orbital bleed into a heparinized syringe and a plasma fraction is obtained by centrifugation of the blood at 2600× g for 5 min in a clinical centrifuge. The level of RO1138452 in each sample is determined by high-performance liquid chromatography with detection by mass spectrometry[1].

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

References

Purity: 98.21%

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RO1138452
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