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RO1138452 (Synonyms: CAY10441)

Name: RO1138452
Brand: TargetMol
SKU: T4436
Price: 44 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T4436 Copy Product Info

Purity: 99.50%

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RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1].

RO1138452

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Catalog No. T4436

Synonyms CAY10441

Cas No. 221529-58-4

Pack Size	Price	USA Stock	Global Stock
1 mg	$44	In Stock	In Stock
2 mg	$63	In Stock	In Stock
5 mg	$97	In Stock	In Stock
10 mg	$155	In Stock	In Stock
25 mg	$347	In Stock	In Stock
50 mg	$597	In Stock	In Stock
100 mg	$852	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$97	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.50%

Appearance:Solid

Color:White to Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1].
Targets&IC50	5-HT2A receptor (rat):5.71 (pKi), 5-HT2A receptor (rat):3040 nM, 5-HT1B receptor (rat):6.11 (pKi), 5-HT1B receptor (rat):1130 nM, 5-HT2C (porcine):6.11 (pKi), 5-HT2C (porcine):1190 nM, PAF Receptor (rabbit):52.9 nM, PAF Receptor (rabbit):7.9 (pKi), I2R (rat):7 nM, I2R (rat):8.33 (pKi), α1B-adrenoceptor (rat):5.87 (pKi), α1B-adrenoceptor (rat):3280 nM, Muscarinic M4 receptor (human):1450 nM, Muscarinic M4 receptor (human):6.14 (pKi), Muscarinic M2 receptor (human):2220 nM, Muscarinic M2 receptor (human):5.88 (pKi), 5-HT1A receptor (human):8580 nM, 5-HT1A receptor (human):5.37 (pKi), Muscarinic M1 receptor (human):5.66 (pKi), Muscarinic M1 receptor (human):2570 nM, α2A-adrenoceptor (human):6.49 (pKi), α2A-adrenoceptor (human):724 nM, 5-HT4 receptor (guinea pig):5.35 (pKi), 5-HT4 receptor (guinea pig):8910 nM, Muscarinic M5 receptor (human):5.81 (pKi), Muscarinic M5 receptor (human):3110 nM
Synonyms	CAY10441

Chemical Properties

Molecular Weight	309.41
Formula	C₁₉H₂₃N₃O
Cas No.	221529-58-4
Smiles	CC(C)Oc1ccc(Cc2ccc(NC3=NCCN3)cc2)cc1
Relative Density.	1.13 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 45 mg/mL (145.44 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.46 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.2320 mL	16.1598 mL	32.3196 mL	161.5979 mL
5 mM	0.6464 mL	3.2320 mL	6.4639 mL	32.3196 mL
10 mM	0.3232 mL	1.6160 mL	3.2320 mL	16.1598 mL
20 mM	0.1616 mL	0.8080 mL	1.6160 mL	8.0799 mL
50 mM	0.0646 mL	0.3232 mL	0.6464 mL	3.2320 mL
100 mM	0.0323 mL	0.1616 mL	0.3232 mL	1.6160 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc