| Identification | Back Directory | [Name]
ApiliMod (Mesylate) | [CAS]
870087-36-8 | [Synonyms]
STA5326 mesylate
Apilimodmesilate
STA-5326 mesylate
STA 5326 mesylate
ApiliMod (Mesylate)
Apilimod dimesylate
Apilimodmesylate, >98%
STA 5326 MESYLATE; STA5326 MESYLATE; STA-5326 MESYLATE
(E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine methanesulfonate
(E)-4-(6-(2-(3-Methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine dimethanesulfonate | [Molecular Formula]
C24H30N6O5S | [MDL Number]
MFCD28167749 | [MOL File]
870087-36-8.mol | [Molecular Weight]
514.6 |
| Hazard Information | Back Directory | [Uses]
Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively[1]. Apilimod is a potent and highly selective PIKfyve inhibitor. | [in vivo]
Apilimod (10 mg/kg, p.o.) is effective not only when administered throughout the entire experiment, but also when administration is initiated on day 30 when disease is clearly measurable but not maximal. Apilimod causes a significant reduction in cell number only in the Th1 model, with an average percentage of inhibition of 51%±8% relative to the vehicle control. Apilimod treatment has no effect in the Th2 setting[1]. Apilimod (5 or 20 mg/kg, p.o.) reduces the level of IL-12 p40 in serum without altering body weight in EAU mice. Oral administration of Apilimod reduces the severity of experimental autoimmune uveoretinitis (EAU) by clinical and histopathological analysis[2]. | [IC 50]
IL-4; IL-5; IL-8; IL-12; IL-23 | [storage]
Store at -20°C | [References]
[1] Wada Y, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007 Feb 1;109(3):1156-64. DOI:10.1182/blood-2006-04-019398
[2] Billich A. Drug evaluation: apilimod, an oral IL-12/IL-23 inhibitor for the treatment of autoimmune diseases and common variable immunodeficiency.IDrugs. 2007 Jan;10(1):53-9. PMID:17187316
[3] Keino H, et al. Therapeutic effect of the potent IL-12/IL-23 inhibitor STA-5326 on experimental autoimmune uveoretinitis. Arthritis Res Ther. 2008;10(5):R122. DOI:10.1186/ar2530 |
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