SPHINX31
SPHINX31 Basic information
- Product Name:
- SPHINX31
- Synonyms:
-
- SPHINX31
- CS-2837
- 2-Furancarboxamide, 5-(4-pyridinyl)-N-[2-[4-(2-pyridinylmethyl)-1-piperazinyl]-5-(trifluoromethyl)phenyl]-
- N-(2-(4-(Pyridin-2-ylmethyl)piperazin-1-yl)-5-(trifluoromethyl)phenyl)-5-(pyridin-4-yl)furan-2-carboxamide
- Serine-arginine protein kinases,retinal permeability,eye disease,neovascular,Inhibitor,Norway Brown rats,SPHINX 31,SRPK,SPHINX31,inhibit,Vascular endothelial growth factor receptor,HuCCA-1,VEGFR,SPHINX-31,diabetics,angiogenic
- SPHINX31, 10 mM in DMSO
- CAS:
- 1818389-84-2
- MF:
- C27H24F3N5O2
- MW:
- 507.51
- Mol File:
- 1818389-84-2.mol
SPHINX31 Chemical Properties
- Boiling point:
- 569.0±50.0 °C(Predicted)
- Density
- 1.342±0.06 g/cm3(Predicted)
- storage temp.
- under inert gas (nitrogen or Argon) at 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
SPHINX31 Usage And Synthesis
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.
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