Reagents and instruments for immunology, cell biology and molecular biology.

RO1138452 [221529-58-4]

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Cat# NB-64-28695-10mg

Size : 10mg

Brand : Neo Biotech

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RO1138452

(Synonyms: CAY10441) Copy Product Info

Synonyms: CAY10441

Catalog No. T4436 Copy Product Info

Purity: 99.50%

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].

Cas No. 221529-58-4

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

Product Information

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	α1B-adrenoceptor (rat):3280 nM, Muscarinic M5 receptor (human):5.81 (pKi), 5-HT2C (porcine):6.11 (pKi), Muscarinic M5 receptor (human):3110 nM, α2A-adrenoceptor (human):724 nM, PAF Receptor (rabbit):7.9 (pKi), 5-HT4 receptor (guinea pig):5.35 (pKi), I2R (rat):7 nM, Muscarinic M2 receptor (human):2220 nM, Muscarinic M2 receptor (human):5.88 (pKi), Muscarinic M4 receptor (human):6.14 (pKi), α1B-adrenoceptor (rat):5.87 (pKi), 5-HT1B receptor (rat):6.11 (pKi), 5-HT4 receptor (guinea pig):8910 nM, α2A-adrenoceptor (human):6.49 (pKi), I2R (rat):8.33 (pKi), 5-HT1B receptor (rat):1130 nM, Muscarinic M4 receptor (human):1450 nM, 5-HT1A receptor (human):8580 nM, 5-HT2C (porcine):1190 nM, PAF Receptor (rabbit):52.9 nM, Muscarinic M1 receptor (human):2570 nM, 5-HT1A receptor (human):5.37 (pKi), 5-HT2A receptor (rat):3040 nM, 5-HT2A receptor (rat):5.71 (pKi), Muscarinic M1 receptor (human):5.66 (pKi)
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 Powder: -20°C for 3 years | In solvent: -80°C for 1 year 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.

Calculator

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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, and a total of 10 animals are to be administered, using a formulation of 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 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 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 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.

1 Enter information below:

Dosagemg/kg

Average weight of animalsg

Dosing volume per animalµL

Number of animals

2 Enter the in vivo formulation:

% DMSO

% Tween 80

% Saline/PBS/ddH₂O