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Dorsomorphin dihydrochloride

Dorsomorphin dihydrochloride

产品编号 T6146   CAS 1219168-18-9
别名: Dorsomorphin (Compound C) 2HCl, Compound C dihydrochloride, Compound C 2HCl, BML-275 2HCl, 6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶, BML-275 dihydrochloride

Dorsomorphin dihydrochloride 是一种选择性和 ATP 竞争性的AMPK 抑制剂,Ki 为 109 nM。它诱导自噬,通过靶向抑制 I 型受体ALK2,ALK3和ALK6来抑制 BMP 途径。

Dorsomorphin dihydrochloride, CAS 1219168-18-9
其他形式的 Dorsomorphin dihydrochloride:
产品目录号及名称: Dorsomorphin dihydrochloride (T6146)
纯度: 99.89%
纯度: 98.89%
纯度: 98.72%
纯度: 97.74%
存储 & 溶解度
产品描述 Dorsomorphin is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.
靶点活性 AMPK:109 nM (cell free)
体外活性 Dorsomorphin (compound C) is a potent reversible inhibitor that is competitive with ATP, with Ki = 109 ± 16 nM in the absence of AMP. Incubation of cultured hepatocytes with compound C inhibited ACC inactivation by either AICAR or metformin [1]. Compound C suppressed 2-deoxy-D-glucose (2DG)-induced GRP78 promoter activity in a dose-dependent manner but had little effect on tunicamycin-induced GRP78 promoter activity. Compound C also suppressed GRP78 promoter activity induced by glucose withdrawal [2].
体内活性 6 h after dorsomorphin was administered intravenously, hepatic hepcidin mRNA levels were reduced to one-third of that of vehicle-injected mice. Alterations in hepcidin levels affect serum iron concentrations within 24 h via the altered mobilization of intracellular iron by ferroportin33. Administration of dorsomorphin over 24 h led to a 60% increase in total serum iron concentrations [3].
激酶实验 Liver AMPK was partially purified from male SD rats to the blue-Sepharose step. The 100-μl reaction mixture contained 100 μM AMP, 100 μM ATP (0.5 μCi 33P-ATP per reaction), and 50 μM SAMS in a buffer (40 mM HEPES, pH 7.0, 80 mM NaCl, 0.8 mM EDTA, 5 mM MgCl2, 0.025% BSA, and 0.8 mM DTT). The reaction was initiated with the addition of the enzyme. After a 30-minute incubation at 30°C, the reaction was stopped by addition of 80 μl 1% H3PO4. Aliquots (100 μl) were transferred to 96-well MultiScreen plates. The plate was washed three times with 1% H3PO4 followed by detection in a Top-count. The in vitro AMPK inhibition data obtained with compound C — (6-[4-(2-Piperidin-1-yl-ethoxy)-phenyl)]-3-pyridin-4-yl-pyyrazolo[1,5-a] pyrimidine — were fit to the following equation for competitive inhibition by nonlinear regression using a least-squares Marquardt algorithm in a computer program written by N. Thornberry of Merck Research Laboratories: Vi/Vo = (Km + S)/[S + Km × (1 + I/Ki)], where Vi is the inhibited velocity, Vo is the initial velocity, S is the substrate (ATP) concentration, Km is the Michaelis constant for ATP, I is the inhibitor (compound C) concentration, and Ki is the dissociation constant for compound C [1].
细胞实验 C2C12 cells were seeded into 96-well plates at 2,000 cells per well in DMEM supplemented with 2% FBS. Wells were treated in quadruplicate with BMP ligands and dorsomorphin or vehicle. Cells were harvested after 5 d in culture with 50 μl Tris-buffered saline, 1% Triton X-100. Lysates were added to p-nitro-phenylphosphate reagent in 96-well plates for 1 h, and alkaline phosphatase activity expressed as absorbance at 405 nM. Cell viability and quantity were measured by Cell-titer Glo and binding of nuclear dye CyQuant, respectively, using replicate wells treated identically to those used for alkaline phosphatase measurements [3].
动物实验 12-week-old C57BL/6 mice raised on a standard diet were injected via the tail vein with 0.2 g kg?1 of dextran (average MW = 5,000) or 0.2 g kg?1 of iron-dextran USP. Dextran was injected with vehicle only, whereas iron-dextran was injected with either vehicle or dorsomorphin (10 mg/kg). 1 h after injection, mice were killed and liver segments were collected in 500 μl of SDS-lysis buffer and mechanically homogenized. 20 μl of liver extracts were resolved by SDS-PAGE and immunoblotted. Total RNA was harvested using Trizol from mechanically homogenized mouse livers (6 h after injection with a single intraperitoneal dose of dorsomorphin (10 mg/kg) or DMSO) [3].
别名 Dorsomorphin (Compound C) 2HCl, Compound C dihydrochloride, Compound C 2HCl, BML-275 2HCl, 6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶, BML-275 dihydrochloride
分子量 472.41
分子式 C24H25N5O·2HCl
CAS No. 1219168-18-9


Powder: -20°C for 3 years | In solvent: -80°C for 2 years


DMSO: 10 mM, with gentle warming

H2O: 47.2 mg/mL (100 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )


1. Zhou G, et al. Role of AMP-activated protein kinase in mechanism of metformin 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. 5. Fan C, Feng J, Tang C, et al. Melatonin suppresses ER stress-dependent proapoptotic effects via AMPK in bone mesenchymal stem cells during mitochondrial oxidative damage[J]. Stem Cell Research & Therapy. 2020, 11(1): 1-22.


1. Xu J, Ao Y L, Huang C, et al. Harmol promotes α-synuclein degradation and improves motor impairment in Parkinson’s models via regulating autophagy-lysosome pathway. npj Parkinson's Disease. 2022, 8(1): 1-12. 2. Fan C, Feng J, Tang C, et al. Melatonin suppresses ER stress-dependent proapoptotic effects via AMPK in bone mesenchymal stem cells during mitochondrial oxidative damage. Stem Cell Research & Therapy. 2020, 11(1): 1-22 3. Qiu W Q, Pan R, Tang Y, et al. Lychee seed polyphenol inhibits Aβ-induced activation of NLRP3 inflammasome via the LRP1/AMPK mediated autophagy induction. Biomedicine & Pharmacotherapy. 2020, 130: 110575. 4. Cao P, Wang Y, Zhang C, et al.Quercetin ameliorates non-alcoholic fatty liver disease (NAFLD) via the promotion of AMPK-mediated hepatic mitophagy.The Journal of Nutritional Biochemistry.2023: 109414.
Kazinol B 4-Hydroxycinnamamide Shizukaol D 3α-Hydroxymogrol HL271 XMD-17-51 Kazinol A Ampkinone


神经元分化化合物库 表型筛选靶点鉴定库 TGF-β/Smad靶点化合物库 抗胰腺癌化合物库 抗肝癌化合物库 糖代谢化合物库 自噬库 细胞焦亡化合物库 抗代谢疾病化合物库 抗癌化合物库


对于不同动物的给药剂量换算,您也可以参考 更多...


请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

% Tween 80
% ddH2O
计算 重置








Dorsomorphin dihydrochloride 1219168-18-9 Autophagy Chromatin/Epigenetic PI3K/Akt/mTOR signaling Stem Cells AMPK TGF-beta/Smad Dorsomorphin (Compound C) 2HCl BMP BML-275 TGF-β Receptor BML275 inhibit Compound C dihydrochloride BML 275 Compound C 2HCl BML-275 2HCl type ATP-competitive 6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶 BML-275 dihydrochloride Dorsomorphin Transforming growth factor beta receptors receptors Compound C pathway AMP-activated protein kinase Inhibitor inhibitor