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| Cas No.: | 1589527-65-0 |
| Chemical Name: | 1-(4-(8-Amino-3-(tert-butyl)imidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl)-3-(3-(trifluoromethyl)phenyl)urea |
| Synonyms: | KIRA6;1-(4-(8-amino-3-(tert-butyl)imidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl)-3-(3-(trifluoromethyl)phenyl)urea;1-(4-(8-Amino-3-tert-butylimidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl)-3-(3-(trifluoromethyl)phenyl)urea;1-[4-(8-amino-3-tert-butylimidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl]-3-[3-(trifluoromethyl)phenyl]urea;KIRA analog, 2;KIRA 6;BDBM192720;BCP26100;s8658;KIRA 6;KIRA analog, 2;KIRA-6;1-((1E,4Z)-4-(8-amino-3 |
| SMILES: | FC(C1C([H])=C([H])C([H])=C(C=1[H])N([H])C(N([H])C1=C([H])C([H])=C(C2=C([H])C([H])=C([H])C([H])=C21)C1=C2C(N([H])[H])=NC([H])=C([H])N2C(C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=N1)=O)(F)F |
| Formula: | C28H25F3N6O |
| M.Wt: | 518.5329 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | KIRA6 allosterically inhibits IRE1α RNase kinase activity with an IC50 of 0.6 µM. |
| In Vivo: | KIRA6 has negligible toxicity up to 10 μM, providing a favorable therapeutic index to test cytoprotection. KIRA6 in BALB/c mice intraperitoneally (i.p.) dosed at 10 mg/kg shows good drug plasma AUC levels with moderate clearance (22.4 mL/min/kg). Drug half-life is 3.90 hours, Cmax is 3.3 μM, and plasma levels at 4 and 8hr are 1.2 μM and 0.33 μM, respectively. Intravitreal co-injection of KIRA6 with Tm significantly reduces XBP1 splicing, TXNIP induction, and decay of the ER-localized photoreceptor-specific Rhodopsin mRNA. KIRA6 dose-dependently inhibits Rhodopsin RNA cleavage by IRE1α. Concomitant with blockage of Terminal UPR outputs, co-injection of KIRA6 in the Tm model reduces photoreceptor loss by Optical Coherence Tomography (OCT) and histology. KIRA6 substantially protects against loss of ERG responsiveness, significantly preserving both a- and b-wave amplitudes[1]. |
| In Vitro: | KIRA6 dose-dependently inhibits IRE1α (WT) kinase activity, XBP1 RNA cleavage, Ins2 RNA cleavage and oligomerization. KIRA6 strongly inhibits JNK phosphorylation from IRE1α hyperactivation or ER stress. Also, KIRA6 dose-dependently inhibits Ins1 mRNA decay, proinsulin depletion, and apoptosis from IRE1α hyperactivation. In INS-1 cells, KIRA6 inhibits IRE1α auto-phosphorylation by Tg and XBP1 mRNA splicing by Tm in a dose-dependent manner. KIRA6 reduces ER stress-induced death of cultured cells and in pancreatic islet explants[1]. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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