| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Kira8 (AMG18; Kira-8; AMG-18) is an effective and allosteric inhibitor of rnase attenuator (kira) that inhibits IRE1α kinase and has antifibrotic properties. With an IC50 of 5.9 nM, it allosterically reduces IRE1α RNase activity. It may encourage the reversal of already-existing fibrosis.
| Targets |
IRE1α (IC50 = 5.9 nM)
|
|---|---|
| ln Vitro |
Kira8 effectively suppresses IRE1α RNase activity against XBP1 and Ins2 RNAs and prevents IRE1α oligomerization. Kira8 reverses XBP1 splicing that is stimulated by GNF-2 and more effectively than KIRA6 reduces IRE1α-driven apoptosis in INS-1 cells[1].
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| ln Vivo |
Male Ins2+/Akita mice receive intraperitoneal injections of KIRA8 (50 mg/kg) every day for 35 days. Over the course of several weeks, a notable decrease in hyperglycemia is observed[1].
Kira8 (50 mg/kg, i.p., once daily) treatment for one week significantly reduces islet XBP1 splicing and TXNIP mRNAs while preserving Ins1/Ins2, BiP, and MANF mRNAs in pre-diabetic NODs mice[1]. |
| Animal Protocol |
Male Ins2+/Akita mice[1]
50 mg/kg Injected i.p.; daily; for 35 days |
| References |
| Molecular Formula |
C31H29CLN6O3S
|
|---|---|
| Molecular Weight |
601.118364095688
|
| Exact Mass |
600.17
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| Elemental Analysis |
C, 61.94; H, 4.86; Cl, 5.90; N, 13.98; O, 7.98; S, 5.33
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| CAS # |
1630086-20-2
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| Related CAS # |
Kira8 Hydrochloride;2250019-92-0
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| PubChem CID |
118721244
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.9
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
42
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| Complexity |
971
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| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC1=C(C2=C(C=C1)C(=CC=C2)NS(=O)(=O)C3=CC=CC=C3Cl)OC4=C(C=CC=N4)C5=NC(=NC=C5)N[C@H]6CCCNC6
|
| InChi Key |
XMWUCMFVDXDRDE-NRFANRHFSA-N
|
| InChi Code |
InChI=1S/C31H29ClN6O3S/c1-20-13-14-22-23(8-4-11-27(22)38-42(39,40)28-12-3-2-10-25(28)32)29(20)41-30-24(9-6-17-34-30)26-15-18-35-31(37-26)36-21-7-5-16-33-19-21/h2-4,6,8-15,17-18,21,33,38H,5,7,16,19H2,1H3,(H,35,36,37)/t21-/m0/s1
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| Chemical Name |
2-chloro-N-[6-methyl-5-[3-[2-[[(3S)-piperidin-3-yl]amino]pyrimidin-4-yl]pyridin-2-yl]oxynaphthalen-1-yl]benzenesulfonamide
|
| Synonyms |
KIRA8; KIRA-8; KIRA 8; AMG-18; AMG 18; AMG18; Amgen IRE1α Inhibitor
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| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
Ethanol: 76.9~100 mg/mL (128~166.4 mM)
DMSO: ~65 mg/mL (~108.1 mM) H2O: ~30 mg/mL (~49.9 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 4 mg/mL (6.65 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 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. Solubility in Formulation 2: ≥ 2.31 mg/mL (3.84 mM) (saturation unknown) in 3% ethanol, 7% Tween-80, and 90% normal Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.17 mg/mL (3.61 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. Solubility in Formulation 4: ≥ 2.17 mg/mL (3.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 21.7 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6636 mL | 8.3178 mL | 16.6356 mL | |
| 5 mM | 0.3327 mL | 1.6636 mL | 3.3271 mL | |
| 10 mM | 0.1664 mL | 0.8318 mL | 1.6636 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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