| Identification | Back Directory | [Name]
SPHINX31 | [CAS]
1818389-84-2 | [Synonyms]
CS-2837
SPHINX31
2-Furancarboxamide, 5-(4-pyridinyl)-N-[2-[4-(2-pyridinylmethyl)-1-piperazinyl]-5-(trifluoromethyl)phenyl]- | [Molecular Formula]
C27H24F3N5O2 | [MDL Number]
MFCD31810499 | [MOL File]
1818389-84-2.mol | [Molecular Weight]
507.51 |
| Chemical Properties | Back Directory | [Boiling point ]
569.0±50.0 °C(Predicted) | [density ]
1.342±0.06 g/cm3(Predicted) | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
DMSO:17.5(Max Conc. mg/mL);34.48(Max Conc. mM)
Ethanol:12.0(Max Conc. mg/mL);23.65(Max Conc. mM) | [form ]
A crystalline solid | [pka]
11.83±0.70(Predicted) | [color ]
White to off-white | [InChIKey]
VURLRACCOCGFDB-UHFFFAOYSA-N | [SMILES]
O1C(C2C=CN=CC=2)=CC=C1C(NC1=CC(C(F)(F)F)=CC=C1N1CCN(CC2=NC=CC=C2)CC1)=O |
| Hazard Information | Back Directory | [Uses]
SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A165a isoform. SPHINX31 can be used to research neovascular eye disease[1][2][3]. | [in vivo]
SPHINX31 (200 μg/mL; twice daily topical eye drops) protects the retinal endothelial permeability barrier from diabetes-associated loss of integrity[3]. | Animal Model: | Norway Brown rats (intraperitoneally injected with 50 mg/kg Streptozotocin (HY-10219) to induce type I diabetes)[3] | | Dosage: | 200 μg/mL | | Administration: | Twice daily topical eye drops | | Result: | Reduced retinal permeability in the diabetics (7.92 ± 1.65 × 10-4 cms-1) less than before induction of diabetes (8.15 ± 2.33 × 10-4 cms-1), and less than the control group (8.85 ± 1.29 × 10-4 cms-1), while the diabetes group was 12.67 ± 1.09 × 10-4 cms-1. |
| [References]
[1] Batson J, et al. Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease. ACS Chem Biol. 2017 Mar 17;12(3):825-832. DOI:10.1021/acschembio.6b01048
[2] Supradit K, et al. Inhibition of serine/arginine-rich protein kinase-1 (SRPK1) prevents cholangiocarcinoma cells induced angiogenesis. Toxicol In Vitro. 2022 Aug;82:105385. DOI:10.1016/j.tiv.2022.105385
[3] C. Allen, et al. The SRPK1 inhibitor SPHINX31 prevents increased retinal permeability in a rodent model of diabetes. Acta Ophthalmologica. Volume 95, Issue S259. |
|
|