首页工具

Dorsomorphin dihydrochloride

产品编号 T6146 CAS 1219168-18-9

别名: BML-275 2HCl, Compound C dihydrochloride, 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, Dorsomorphin (Compound C) 2HCl, Compound C 2HCl, BML-275 dihydrochloride

Dorsomorphin dihydrochloride (BML-275 2HCl) 是一种 AMPK 抑制剂 (Ki=109 nM)，具有选择性和 ATP 竞争性。Dorsomorphin dihydrochloride 可以抑制 BMP I 型受体 ALK2、ALK3 和 ALK6。Dorsomorphin dihydrochloride 可诱导自噬，具有抗肿瘤活性。

TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

Dorsomorphin dihydrochloride Chemical Structure

Dorsomorphin dihydrochloride, CAS 1219168-18-9

规格	价格/CNY	货期
1 mg	￥ 189	现货
2 mg	￥ 258	现货
5 mg	￥ 466	现货
10 mg	￥ 685	现货
25 mg	￥ 1,380	现货
50 mg	￥ 2,430	现货
100 mg	￥ 3,630	现货
500 mg	￥ 8,170	现货
1 mL * 10 mM (in DMSO)	￥ 466	现货

大包装超大折扣，点击咨询

其他形式的 Dorsomorphin dihydrochloride:

Dorsomorphin
现货

选择批次

纯度: 99.89%

纯度: 98.89%

纯度: 98.72%

纯度: 97.74%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Dorsomorphin dihydrochloride (BML-275 2HCl) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin dihydrochloride inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy, and possesses antitumor activity.
靶点活性	AMPK:109 nM (cell free)
体外活性	方法：人肿瘤细胞 HeLa 和 HCT116 用 Dorsomorphin dihydrochloride (1.25-80 μM) 处理 24 h，使用 CCK-8 assay 检测细胞活力。结果：Dorsomorphin 抑制 HeLa 和 HCT116 细胞的活力，IC50 值分别为 10.71 μM 和 11.34 μM。[1] 方法：ATL 患者来源的 PBMCs 细胞用 Dorsomorphin dihydrochloride (5-25 μM) 处理 24 h，使用 Flow Cytometry 检测细胞凋亡情况。结果：Dorsomorphin 以剂量依赖的方式增加了急性和慢性型 ATL 患者 PBMC 中早期凋亡细胞的频率。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Dorsomorphin dihydrochloride (10 mg/kg) 腹腔注射给携带人类肿瘤 S1T 的 NOD/SCID 小鼠，每天一次，持续二十八天。结果：Dorsomorphin 抑制了 NOD/SCID 小鼠中人 ATL 肿瘤异种移植物的生长。[2] 方法：为检测体内对 SMAD 活性的影响，将 Dorsomorphin dihydrochloride (10 mg/kg) 单次腹腔注射给 iron-dextran 处理的 C57BL/6 小鼠。结果：Dorsomorphin 消除了 iron-dextran 引起的铁介导的肝脏 SMAD1/5/8 磷酸化的增加。[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	BML-275 2HCl, Compound C dihydrochloride, 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, Dorsomorphin (Compound C) 2HCl, Compound C 2HCl, BML-275 dihydrochloride
分子量	472.41
分子式	C24H25N5O·2HCl
CAS No.	1219168-18-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 6.88 mg/mL (14.55 mM), Sonication is recommended.

H2O: 47.2 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / H2O	1 mM	2.1168 mL	10.584 mL	21.1681 mL	52.9201 mL
	5 mM	0.4234 mL	2.1168 mL	4.2336 mL	10.584 mL
	10 mM	0.2117 mL	1.0584 mL	2.1168 mL	5.292 mL
H2O	20 mM	0.1058 mL	0.5292 mL	1.0584 mL	2.646 mL
	50 mM	0.0423 mL	0.2117 mL	0.4234 mL	1.0584 mL
	100 mM	0.0212 mL	0.1058 mL	0.2117 mL	0.5292 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Li N, et al. Dorsomorphin induces cancer cell apoptosis and sensitizes cancer cells to HSP90 and proteasome inhibitors by reducing nuclear heat shock factor 1 levels. Cancer Biol Med. 2019 May;16(2):220-233. 2. Aikawa A, et al. Cell death induced by dorsomorphin in adult T-cell leukemia/lymphoma is AMPK-independent. FEBS J. 2020 Sep;287(18):4005-4015. 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.

文献引用

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.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Dorsomorphin dihydrochloride 1219168-18-9 Autophagy Chromatin/Epigenetic PI3K/Akt/mTOR signaling Stem Cells AMPK TGF-beta/Smad Dorsomorphin (Compound C) Compound C BML 275 BML275 Dihydrochloride Dorsomorphin BMP TGF-β Receptor Compound C Dihydrochloride Dorsomorphin Dihydrochloride inhibit BML-275 2HCl BML-275 Dihydrochloride Compound C dihydrochloride type ATP-competitive BML 275 Dihydrochloride 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 Dorsomorphin (Compound C) 2HCl Transforming growth factor beta receptors receptors Compound C 2HCl BML-275 dihydrochloride pathway BML-275 AMP-activated protein kinase Inhibitor BML275 inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

沪公网安备 31010602006700号

陶术

生物

TargetMol^®中国区唯一合作伙伴

点击进入陶术生物官网

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼

Dorsomorphin dihydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords