| Identification | Back Directory | [Name]
Kira8 Hydrochloride | [CAS]
2250019-92-0 | [Synonyms]
Kira8 Hydrochloride AMG-18 Hydrochloride Kira8 Hydrochloride,Kira-8 Hydrochloride KIRA8 HYDROCHLORIDE (AMG-18 HYDROCHLORIDE) (S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide hydrochloride | [Molecular Formula]
C31H30Cl2N6O3S | [MDL Number]
MFCD31656706 | [MOL File]
2250019-92-0.mol | [Molecular Weight]
637.58 |
| Hazard Information | Back Directory | [Uses]
Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM[1]. | [in vivo]
Male Ins2+/Akita mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), significant reduction of hyperglycemia become apparent over several weeks[1].
One week treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserves Ins1/Ins2, BiP and MANF mRNAs[1]. | Animal Model: | Male Ins2+/Akita mice[1] | | Dosage: | 50 mg/kg | | Administration: | Injected i.p.; daily; for 35 days | | Result: | Significant reduction of hyperglycemia became apparent over several weeks. |
| [storage]
Store at -20°C | [References]
[1] Morita S, et al. Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes. Cell Metab. 2017 Apr 4;25(4):883-897.e8. DOI:10.1016/j.cmet.2017.03.018 |
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