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KIRA6 (KIRA-6) is a novel, potent, allosteric IRE1 inhibitor with anti-inflammatory and immune-modulating properties (IC50 of 0.6 µM). KIRA6 was created to block IRE1α-mediated cell death and has since been shown to support cell survival and stop ER stress-induced cell aging in vivo.
| Targets |
IRE1α (IC50 = 0.6 µM)
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|---|---|
| ln Vitro |
KIRA6 inhibits Tg's autophosphorylation of IRE1α and Tm's splicing of XBP1 mRNA in INS-1 cells in a dose-dependent manner[1].
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| ln Vivo |
KIRA6 protects the functional viability of photoreceptors intravitreally in rat models of ER stress-induced retinal degeneration. Systematically, KIRA6 protects pancreatic β-cells in Akita diabetic mice, boosts insulin, and lowers hyperglycemia. In vivo, KIRA6 inhibits IRE1α to maintain cell viability and function in a variety of cells and rodent tissues under ER stress. When administered intraperitoneally (i.p.) to BALB/c mice at a dose of 10 mg/kg, KIRA6 has a good plasma AUC (AUC 0-24h = 14.3 μM*h) and a moderate clearance (22.4 mL/min/kg). The drug has a 3.90-hour half-life, a Cmax of 3.3 μM, and plasma levels at 4 and 8 hours of 1.2 μM and 0.33 μM, respectively[1].
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| Cell Assay |
Drugs were administered to cells at different concentrations.
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| Animal Protocol |
BALB/c mice
10 mg/kg i.p. |
| References |
| Molecular Formula |
C28H25F3N6O
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|---|---|
| Molecular Weight |
518.5329
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| Exact Mass |
518.204
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| Elemental Analysis |
C, 64.86; H, 4.86; F, 10.99; N, 16.21; O, 3.09
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| CAS # |
1589527-65-0
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| Related CAS # |
1589527-65-0
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| PubChem CID |
73425700
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| Appearance |
Solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.645
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| LogP |
6.26
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
38
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| Complexity |
834
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C1C=CC=C(C=1)NC(NC1=CC=C(C2=CC=CC=C21)C1=C2C(N)=NC=CN2C(C(C)(C)C)=N1)=O)(F)F
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| InChi Key |
NOHQEAFAESMMDX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H25F3N6O/c1-27(2,3)25-36-22(23-24(32)33-13-14-37(23)25)20-11-12-21(19-10-5-4-9-18(19)20)35-26(38)34-17-8-6-7-16(15-17)28(29,30)31/h4-15H,1-3H3,(H2,32,33)(H2,34,35,38)
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| Chemical Name |
1-[4-(8-amino-3-tert-butylimidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl]-3-[3-(trifluoromethyl)phenyl]urea
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| Synonyms |
KIRA6; KIRA 6; KIRA-6
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25~60 mg/mL (48.2~115.7 mM)
Ethanol: ~60 mg/mL (~115.7 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (0.96 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (0.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (0.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9285 mL | 9.6426 mL | 19.2853 mL | |
| 5 mM | 0.3857 mL | 1.9285 mL | 3.8571 mL | |
| 10 mM | 0.1929 mL | 0.9643 mL | 1.9285 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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