| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
CAY10505, the dehydroxylated form of AS-252424, is a novel, potent and selective inhibitor of PI3Kγ (phosphoinositide 3-kinase) with a potential to improve hypertension-associated vascular endothelial dysfunction.
| Targets |
PI3Kγ ( IC50 = 30 nM, Neurons)
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| ln Vitro |
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| ln Vivo |
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| Cell Assay |
In neurons treated with 3.5 μM BA, 200 nM CAY10505 partially reduced the baicalein-induced Akt phosphorylation.
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| Animal Protocol |
Wistar albino rats (180-240 g) of either sex are employed in the present study. The number of rats used (n) for each group is 6. Rats are kept in Group I (normal control) on a diet of standard chow and water. Rats in Group II (hypertensive control) are unilaterally nephrectomized (uninephrectomized), given subcutaneous injections of DOCA (40 mg/kg) twice a week for six weeks, and then the untreated drinking water is changed to a 1% NaCl solution. After receiving treatment with DOCA for five weeks, rats in Group III (hypertensive rats) were given CAY10505 (0.6 mg/kg, per os (p.o)) for one week. Rats in Group IV (hypertensive rats) receive treatment with Losartan (25 mg/kg, p.o.) for one week following five weeks of DOCA treatment. Rats in Group V (hypertensive rats) receive Atorvastatin (30 mg/kg, p.o.) for 1 week after receiving DOCA for 5 weeks.
Wistar albino rats
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| References |
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| Molecular Formula |
C14H8FNO3S
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|---|---|
| Molecular Weight |
289.28162
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| Exact Mass |
289.02
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| Elemental Analysis |
C, 58.13; H, 2.79; F, 6.57; N, 4.84; O, 16.59; S, 11.08
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| CAS # |
1218777-13-9
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| Related CAS # |
1218777-13-9
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| PubChem CID |
1204893
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.663
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| LogP |
2.78
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
446
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC/1=O)SC1=C\C2=CC=C(C3=CC=C(F)C=C3)O2
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| InChi Key |
UFBTYTGRUBUUIL-KPKJPENVSA-N
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| InChi Code |
InChI=1S/C14H8FNO3S/c15-9-3-1-8(2-4-9)11-6-5-10(19-11)7-12-13(17)16-14(18)20-12/h1-7H,(H,16,17,18)/b12-7+
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| Chemical Name |
(E)-5-((5-(4-fluorophenyl)furan-2-yl)methylene)thiazolidine-2,4-dione
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| Synonyms |
CAY 10505; CAY10505; CAY-10505
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~58 mg/mL (200.5 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4569 mL | 17.2843 mL | 34.5686 mL | |
| 5 mM | 0.6914 mL | 3.4569 mL | 6.9137 mL | |
| 10 mM | 0.3457 mL | 1.7284 mL | 3.4569 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.
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.
Effects of PI3K inhibitors on the baicalein–activated HIF1α and Epo/VEGF gene transcription in neurons. Neurons were treated with 3.5 μM BA with or without 1 h pretreatment with the pan PI3K inhibitor LY294002 (LY, 10 μM), PI3Kα/β inhibitor (PI3K α inhibitor-2, 50 nM), or PI3Kγ inhibitor (CAY10505, 200 nM). PLoS One, 2013, 8(7):e69019. |
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