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RS-25344 HCl

Cat No.:V7741 Purity: ≥98%
RS-25344 HCl is a selective cAMP-phosphodiesterase 4 (PDE IV) inhibitor (antagonist) with IC50 of 0.28 nM in human lymphocytes.
RS-25344 HCl
RS-25344 HCl Chemical Structure CAS No.: 152815-28-6
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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5mg
10mg
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Other Forms of RS-25344 HCl:

  • RS-25344
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
RS-25344 HCl is a selective cAMP-phosphodiesterase 4 (PDE IV) inhibitor (antagonist) with IC50 of 0.28 nM in human lymphocytes. It has only a weak inhibitory activity against PDE I, II, and III. The IC50 is respectively are >100 μM, 160 μM, and 330 μM. RS-25344 HCl has anti~inflammatory, memory and cognitive enhancement, and anti-tumor effects.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
RS-25344 hydrochloride (0-10 μM) has a maximal inhibitory action in the range of 100 nM and an effective concentration of 0.3 nM, making it an efficient inhibitor of sperm PDE activity [2].
ln Vivo
In wild-type C57BL/6 mice, RS-25344 hydrochloride (5 mg/kg; i.p.; twice daily for 72 hours) significantly increased the gastric weight [3]. Mice's gastric retention is increased by RS-25344 hydrochloride (1 mg/kg; intraperitoneal injection; 30 minutes before rice balls) [3].
References

[1]. Elevated intracellular cyclic AMP inhibits chemotaxis in human eosinophils. Cell Signal. 1995 Jul;7(5):527-34.

[2]. Enhancement of motility and acrosome reaction in human spermatozoa: differential activation by type-specific phosphodiesterase inhibitors. Hum Reprod. 1998 May;13(5):1248-54.

[3]. PAN-selective inhibition of cAMP-phosphodiesterase 4 (PDE4) induces gastroparesis in mice. FASEB J. 2020 Sep;34(9):12533-12548.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H14CLN5O4
Molecular Weight
411.798562526703
Exact Mass
411.073
CAS #
152815-28-6
Related CAS #
152815-28-6(RS-25344 HCl);152814-89-6 (RS-25344);
PubChem CID
19781728
Appearance
White to off-white solid powder
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
3
Heavy Atom Count
29
Complexity
618
Defined Atom Stereocenter Count
0
InChi Key
ROSFKXDQMBPYQQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H13N5O4.ClH/c25-18-16-5-2-8-21-17(16)23(14-3-1-4-15(11-14)24(27)28)19(26)22(18)12-13-6-9-20-10-7-13;/h1-11H,12H2;1H
Chemical Name
1-(3-nitrophenyl)-3-(pyridin-4-ylmethyl)pyrido[2,3-d]pyrimidine-2,4-dione;hydrochloride
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~83.33 mg/mL (~202.36 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4284 mL 12.1418 mL 24.2836 mL
5 mM 0.4857 mL 2.4284 mL 4.8567 mL
10 mM 0.2428 mL 1.2142 mL 2.4284 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Retention of food in the stomach of mice is a class effect of PAN-PDE4 inhibitors. C57BL/6 mice were treated with the structurally distinct PAN-PDE4 inhibitors Piclamilast, Rolipram, Roflumilast and RS25344 (each 5 mg/kg, i.p., twice daily) as well as the PDE3 inhibitor Cilostamide (10 mg/kg, i.p., twice daily) or solvent controls (Mock) for 72 h while animals had free access to food and water. After euthanasia, stomachs were extracted and weighed. Data represent the mean ± SEM. Female mice are represented as filled circles (●), males as open squares (□). Statistical significance was determined using one-way ANOVA with Tukey’s post hoc test and is indicated as ** (p<0.01). The chemical structures of the PDE4 inhibitors tested are shown for comparison.[3]. Will McDonough, et al. PAN-selective inhibition of cAMP-phosphodiesterase 4 (PDE4) induces gastroparesis in mice. FASEB J. 2020 Sep;34(9):12533-12548.
  • PAN-PDE4 inhibition causes acute gastroparesis. Mice were injected (i.p.) with the indicated doses of PDE inhibitors or solvent control (Mock). Thirty minutes later, a 200 μl food bolus traced with FITC-dextran was delivered by oral gavage and 30 min after that the animals were euthanized, the stomach extracted, and FITC retained in the stomach measured via fluorescence spectroscopy. Female mice are represented as filled circles (●), males as open squares (□). (A) Shown is the effect of the brain-penetrant PAN-PDE4 inhibitors Piclamilast, Rolipram, Roflumilast and RS25344, as well as the poorly brain-penetrant PAN-PDE4 inhibitor YM976, and the PDE3-selective inhibitor Cilostamide (all 1 mg/kg). (B/C/D) Shown are dose response curves for the PAN-PDE4 inhibitors Rolipram (B), Piclamilast (C), and YM976 (D). The chemical structure of YM976 is shown above the graph in (D). Data represent the mean ± SEM of FITC fluorescence retained in the stomach as % of total fluorescence of the food bolus. Statistical significance was determined using one-way ANOVA with Tukey’s post hoc test and is indicated as * (p<0.05), ** (p<0.01) and *** (p<0.001).[3]. Will McDonough, et al. PAN-selective inhibition of cAMP-phosphodiesterase 4 (PDE4) induces gastroparesis in mice. FASEB J. 2020 Sep;34(9):12533-12548.
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