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

RO1138452  (Synonyms: CAY10441)

Cat. No.: HY-108912 Purity: ≥98.0%
COA Handling Instructions

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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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
1 mg USD 57 In-stock
5 mg USD 120 In-stock
10 mg USD 190 In-stock
25 mg USD 420 In-stock
50 mg USD 720 In-stock
100 mg USD 1250 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

RO1138452 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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[1]

Rat I2 Receptor

7 nM (IC50)

Rat I2 Receptor

8.33 (pKi)

Rabbit PAF Receptor

52.9 nM (IC50)

Human α2A adrenoceptor

724 nM (IC50)

Rat α1B adrenoceptor

3280 nM (IC50)

Human Muscarinic M4 Receptor

1450 nM (IC50)

Human muscarinic M2 Receptor

2220 nM (IC50)

Human muscarinic M1 Receptor

2570 nM (IC50)

Human muscarinic M5 Receptor

3110 nM (IC50)

Rat 5-HT1B Receptor

1130 nM (IC50)

pig 5-HT2C Receptor

1190 nM (IC50)

Rat 5-HT2A Receptor

3040 nM (IC50)

Human 5-HT1A Receptor

8580 nM (IC50)

Guinea-pig 5-HT4 Receptor

8910 nM (IC50)

Rat α1B adrenoceptor

5.87 (pKi)

Human α2A adrenoceptor

6.49 (pKi)

Human muscarinic M1 Receptor

5.66 (pKi)

Human muscarinic M5 Receptor

5.81 (pKi)

Human muscarinic M2 Receptor

5.88 (pKi)

Human muscarinic M4 Receptor

6.14 (pKi)

Rabbit PAF Receptor

7.9 (pKi)

Guinea-pig 5-HT4 Receptor

5.35 (pKi)

Human 5-HT1A Receptor

5.37 (pKi)

Rat 5-HT2A Receptor

5.71 (pKi)

Rat 5-HT1B Receptor

6.11 (pKi)

Pig 5-HT2C Receptor

6.11 (pKi)

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].

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

RO1138452 Related Antibodies
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].

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

309.41

Formula

C19H23N3O
CAS No.
Appearance

Solid

Color

Light yellow to brown

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (323.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 50 mg/mL (161.60 mM; Need ultrasonic)

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
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.

  • Molarity Calculator

  • Dilution Calculator

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 10 mg/mL (32.32 mM); Clear solution; Need ultrasonic

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥98.0%

COA (244 KB) HNMR (241 KB)

Handling Instructions (2659 KB)
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

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
Ethanol / DMSO 1 mM 3.2320 mL 16.1598 mL 32.3196 mL 80.7989 mL
5 mM 0.6464 mL 3.2320 mL 6.4639 mL 16.1598 mL
10 mM 0.3232 mL 1.6160 mL 3.2320 mL 8.0799 mL
15 mM 0.2155 mL 1.0773 mL 2.1546 mL 5.3866 mL
20 mM 0.1616 mL 0.8080 mL 1.6160 mL 4.0399 mL
25 mM 0.1293 mL 0.6464 mL 1.2928 mL 3.2320 mL
30 mM 0.1077 mL 0.5387 mL 1.0773 mL 2.6933 mL
40 mM 0.0808 mL 0.4040 mL 0.8080 mL 2.0200 mL
50 mM 0.0646 mL 0.3232 mL 0.6464 mL 1.6160 mL
60 mM 0.0539 mL 0.2693 mL 0.5387 mL 1.3466 mL
80 mM 0.0404 mL 0.2020 mL 0.4040 mL 1.0100 mL
100 mM 0.0323 mL 0.1616 mL 0.3232 mL 0.8080 mL
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RO1138452 Related Classifications

Help & FAQs
  • 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.

Keywords:

RO1138452221529-58-4CAY10441RO 1138452RO-1138452CAY 10441CAY-10441Prostaglandin ReceptorInhibitorinhibitorinhibit

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