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Kira8

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Purity:98.07%

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COA HNMR HPLC

Kira8

Catalog No. T11762LCas No. 1630086-20-2

Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.

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Pack Size	Price	Availability
1 mg	$89	In Stock
5 mg	$213	In Stock
10 mg	$322	In Stock
25 mg	$597	In Stock
50 mg	$852	In Stock
100 mg	$1,170	In Stock
1 mL x 10 mM (in DMSO)	$283	In Stock

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Product Introduction

Bioactivity

Description	Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
Targets&IC50	IRE1α:5.9 nM(IRE1α RNase)
In vitro	Kira8 more effectively causes IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2. Kira8 blocks IRE1α oligomerization and effectively inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs.
In vivo	One week of treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) causes obvious reductions in islet XBP1 splicing and TXNIP mRNAs. It also preserves Ins1/Ins2, BiP, and MANF mRNAs. Male Ins2+/Akita mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), obviously reduction of hyperglycemia becomes apparent over several weeks.
Alias	AMG-18

Chemical Properties

Molecular Weight	601.12
Formula	C31H29ClN6O3S
Cas No.	1630086-20-2

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 65 mg/mL (108.13 mM), Sonication is recommended.

H2O: insoluble

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6636 mL	8.3178 mL	16.6356 mL	83.1781 mL
5 mM	0.3327 mL	1.6636 mL	3.3271 mL	16.6356 mL
10 mM	0.1664 mL	0.8318 mL	1.6636 mL	8.3178 mL
20 mM	0.0832 mL	0.4159 mL	0.8318 mL	4.1589 mL
50 mM	0.0333 mL	0.1664 mL	0.3327 mL	1.6636 mL
100 mM	0.0166 mL	0.0832 mL	0.1664 mL	0.8318 mL

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In Vivo Formulation Calculator (Clear solution)

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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