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Dorsomorphin dihydrochloride

MCE 國(guó)際站：Dorsomorphin dihydrochloride

品牌：MedChemExpress (MCE)

貨號(hào)：HY-13418

CAS：1219168-18-9

Synonyms：Compound C dihydrochloride; BML-275 dihydrochloride

純度：0.9973

存儲(chǔ)條件：4°C,密封保存,，遠(yuǎn)離潮濕 *溶劑中：-80°C, 1年; -20°C, 6個(gè)月（密封保存，遠(yuǎn)離潮濕）

運(yùn)輸條件：美國(guó)大陸的室溫,；其他地方可能有所不同,。

產(chǎn)品活性：Dorsomorphin (Compound C) dihydrochloride 是一種有效，選擇性和 ATP 競(jìng)爭(zhēng)性的 AMPK 抑制劑,，Ki 為 109 nM,。Dorsomorphin dihydrochloride 通過(guò)靶向抑制 I 型受體 ALK2，ALK3 和 ALK6 來(lái)抑制 BMP 途徑,。Dorsomorphin dihydrochloride 還能夠逆轉(zhuǎn) Urolithin A (HY-100599) 導(dǎo)致的自噬 (autophagy) 激活和抗炎作用,。

體外：Dorsomorphin (compound C; 0-10 μM; 18 h) dihydrochloride 以劑量依賴(lài)性方式抑制人纖維肉瘤 HT1080 細(xì)胞中 2DG 誘導(dǎo)的 GRP78 啟動(dòng)子活性，但對(duì)衣霉素 (HY-A0098) 誘導(dǎo)的 GRP78 啟動(dòng)子活性幾乎沒(méi)有影響,。Dorsomorphin dihydrochloride 還抑制葡萄糖戒斷誘導(dǎo)的 GRP78 啟動(dòng)子活性,。Dorsomorphin dihydrochloride 對(duì) 2DG 誘導(dǎo)的 PERK 激活沒(méi)有影響，并降低 HT1080 細(xì)胞中基礎(chǔ)和 2DG 誘導(dǎo)的 AMPK 磷酸化水平[2],。 MCE尚未獨(dú)立證實(shí)這些方法的準(zhǔn)確性,。僅供參考。

體內(nèi)：Dorsomorphin (化合物 C; 10 mg/kg; 靜脈注射一次) dihydrochloride 處理導(dǎo)致總血清鐵濃度增加 60%,，降低成年小鼠鐵調(diào)素表達(dá)的基礎(chǔ)水平并增加血清鐵濃度[3],。 Dorsomorphin (0.2 mg/kg，靜脈注射,，LPS 注射前 30 分鐘) dihydrochloride 降低注射 LPS 的大鼠主動(dòng)脈中的 ICAM-1 和 VCAM-1 表達(dá)[4],。 Dorsomorphin (25 mg/kg；腹腔注射,，在雄性 BALB/c 小鼠中) dihydrochloride 在注射脂多糖 (LPS) 之前進(jìn)行處理,，與僅接受 LPS 處理的動(dòng)物相比，顯著降低了致死率[5],。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50 & Target：AMPK 109 nM (Ki) ACVR1 BMPR1A ALK6 Autophagy

銷(xiāo)售產(chǎn)品：Suc-Ala-Leu-Pro-Phe-pNA  | 187-1, N-WASP inhibitor  | Caftaric acid  | Clonidine (hydrochloride)  | Lenvatinib-d4  | N-3-Oxo-tetradecanoyl-L-homoserine lactone  | BTX161  | Pelargonidin (chloride)  | 2-Iminothiolane (hydrochloride)  | Adenosine dialdehyde

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

參考文獻(xiàn)：

[1]. Zhou G, et al. Role of AMP-activated protein kinase in mechanism of action. J Clin Invest. 2001 Oct;108(8):1167-74.[2]. Saito S, et al. Compound C prevents the unfolded protein response during glucose deprivation through a mechanism independent of AMPK and BMP signaling. PLoS One. 2012;7(9):e45845.[3]. Yu PB, et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat Chem Biol. 2008 Jan;4(1):33-41.[4]. Kim YM, et al. Compound C independent of AMPK inhibits ICAM-1 and VCAM-1 expression in inflammatory stimulants-activated endothelial cells in vitro and in vivo. Atherosclerosis. 2011 Nov;219(1):57-64.[5]. Guo Y, et al. AMPK inhibition blocks ROS-NFκB signaling and attenuates endotoxemia-induced liver injury. PLoS One. 2014 Jan 24;9(1):e86881.[6]. Zhang Y, et al. Urolithin A suppresses glucolipotoxicity-induced ER stress and TXNIP/NLRP3/IL-1β inflammation signal in pancreatic β cells by regulating AMPK and autophagy. Phytomedicine. 2021 Dec;93:153741.