[CAS NO. 1630086-20-2] Kira8
PRODUCTS SPECIFICATIONS [1630086-20-2]
DESCRIPTION [1630086-20-2]
Overview
| MDL | MFCD28404657 |
|---|---|
| Molecular Weight | 601.12 |
| Molecular Formula | C31H29ClN6O3S |
| SMILES | O=S(C1=CC=CC=C1Cl)(NC2=C3C=CC(C)=C(OC4=NC=CC=C4C5=NC(N[C@@H]6CNCCC6)=NC=C5)C3=CC=C2)=O |
5 Publications Citing Use of MCE
Summary
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC 50 of 5.9 nM [1] .
In Vitro
Kira8 blocks IRE1α oligomerization, and potently inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs. Kira8 more potently reduces IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
Ethanol : 76.92 mg/mL ( 127.96 mM ; ultrasonic and adjust pH to 5 with HCl)
DMSO : 65 mg/mL ( 108.13 mM ; Need ultrasonic)
H 2 O : 30 mg/mL ( 49.91 mM ; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 4 mg/mL (6.65 mM); Suspended solution; Need ultrasonic
-
2.
Add each solvent one by one: 3% ethanol, 7% Tween-80 , and 90% normal saline
Solubility: ≥ 2.31 mg/mL (3.84 mM); Clear solution
-
3.
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.17 mg/mL (3.61 mM); Clear solution