KIRA8 (AMG-18)
| 中文名稱 | KIRA8 (AMG-18) |
|---|---|
| 中文同義詞 | (S)-2-氯-N-(6-甲基-5-((3-(2-(哌啶-3-基氨基)嘧啶-4-基)吡啶-2-基)氧基)萘-1-基)苯磺酰胺;化合物KIRA8;(S)-2-氯-N-[6-甲基-5-[[3-[2-(3-哌啶基氨基)-4-嘧啶基]-2-吡啶基]氧基]-1-萘基]苯磺酰胺;化合物KIRA8,10 MM DMSO 溶液;Kira8 ,E2652;Kira8試劑;Kira8試劑 |
| 英文名稱 | Amgen IRE1α Inhibitor |
| 英文同義詞 | Amgen IRE1α Inhibitor;Kira8;IRE-1 INHIBITOR;KIRA8 (AMG-18);Benzenesulfonamide, 2-chloro-N-[6-methyl-5-[[3-[2-[(3S)-3-piperidinylamino]-4-pyrimidinyl]-2-pyridinyl]oxy]-1-naphthalenyl]-;(S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide;Amgen IRE1a Inhibitor;Inositol requiring enzyme 1,inhibit,AMG18,AMG 18,Kira 8,Kira8,Inhibitor,IRE1,Kira-8 |
| CAS號 | 1630086-20-2 |
| 分子式 | C31H29ClN6O3S |
| 分子量 | 601.12 |
| EINECS號 | |
| 相關(guān)類別 | |
| Mol文件 | 1630086-20-2.mol |
| 結(jié)構(gòu)式 |  |
KIRA8 (AMG-18) 性質(zhì)
| 沸點(diǎn) | 812.6±75.0 °C(Predicted) |
|---|---|
| 密度 | 1.383±0.06 g/cm3(Predicted) |
| 儲存條件 | Store at -20°C |
| 溶解度 | 水：30.0（最大濃度 mg/mL）；49.91（最大濃度 mM） |
| 形態(tài) | 固體 |
| 酸度系數(shù)(pKa) | 7.66±0.30(Predicted) |
| 顏色 | 淺黃至黃色 |
| InChIKey | XMWUCMFVDXDRDE-NRFANRHFSA-N |
| SMILES | [S](=O)(=O)(Nc2c3c(c(c(cc3)C)Oc4ncccc4c5nc(ncc5)N[C@@H]6CNCCC6)ccc2)c1c(cccc1)Cl |
Kira8 (AMG-18) 是一種單選擇性 IRE1α 抑制劑，可以變構(gòu)減弱 IRE1α RNase 活性，IC50 為 5.9 nM。
IRE1α
IC50: 5.9 nM (IRE1α RNase)
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.
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.
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.
| Animal Model: | Male Ins2 +/Akita mice |
| Dosage: | 50 mg/kg |
| Administration: | Injected i.p.; daily; for 35 days |
| Result: | Significant reduction of hyperglycemia became apparent over several weeks. |
安全信息
| WGK Germany | WGK 3 |
|---|---|
| 存儲類別 | 11 - 可燃固體 |
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-114368 | Kira8 | 1630086-20-2 | 1 mg | 1050元 |
| 2026/06/05 | HY-114368 | KIRA8 (AMG-18) Kira8 | 1630086-20-2 | 5 mg | 2300元 |