S80610 |
TAK-715 |
源葉(MedMol) | 99% |
- 提示:詳情請下載說明書。
- 產(chǎn)品描述: TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model
- 靶點: p38α:7.1 nM (IC50);p38β:200 nM (IC50);p38δ:>10 μM (IC50);p38γ:>10 μM (IC50);CK1δ;CK1ε ;p38MAPK;CaseinKinase;JNK
- 體內(nèi)研究:
TAK-715 (compound 8h; 3-30 mg/kg; PO) significantly reduces the secondary paw volume.TAK-715 (10 mg/kg; PO) has a Cmax of 0.19 μg/mL and an AUC of 1.16 μg?h/mL.
- 參考文獻(xiàn):
1. Miwatashi S, et al. Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent. J Med Chem, 2005, 48(19), 5966-5979. 2. Verkaar F, et al. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/?. Chem Biol, 2011, 18(4), 485-494. 3. Huiwen Ren, et al. Inhibition of α1-adrenoceptor reduces TGF-β1-induced epithelial-to-mesenchymal transition and attenuates UUO-induced renal fibrosis in mice. FASEB J. 2020 Nov;34(11):14892-14904.
- 溶解性: DMSO : ≥ 100 mg/mL (250.31 mM)
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.503 ml 12.515 ml 25.031 ml 5 mM 0.501 ml 2.503 ml 5.006 ml 10 mM 0.25 ml 1.252 ml 2.503 ml 50 mM 0.05 ml 0.25 ml 0.501 ml
- 注意:部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。
輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)