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Merck

171260

Dorsomorphin

≥95% (HPLC), solid, AMPK inhibitor, Calbiochem

別名:

AMPK Inhibitor, Compound C, 6-[4-(2-Piperidin-1-yl-ethoxy)-phenyl)]-3-pyridin-4-yl-pyrrazolo[1,5-a]-pyrimidine, Dorsomorphin, BMP Inhibitor I, AMPK Inhibitor I

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この商品について

実験式（ヒル表記法）:
C24H25N5O
CAS番号:
866405-64-3
分子量:
399.49
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD08705402
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light

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製品名

AMPK Inhibitor, Compound C, AMPK Inhibitor, Compound C, CAS 866405-64-3, is a cell-permeable compound that inhibits KDR/VEGFR2, ALK2/BMPR-I, and AMPK kinase activities (IC50 = 25.1, 148, and 234.6 nM, respectively).

SMILES string

[n]21ncc(c2ncc(c1)c4ccc(cc4)OCCN5CCCCC5)c3ccncc3

InChI

1S/C24H25N5O/c1-2-12-28(13-3-1)14-15-30-22-6-4-19(5-7-22)21-16-26-24-23(17-27-29(24)18-21)20-8-10-25-11-9-20/h4-11,16-18H,1-3,12-15H2

InChI key

XHBVYDAKJHETMP-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

light yellow

solubility

2% HCl: 10 mg/mL, 2% acetic acid: 10 mg/mL, methanol: 3 mg/mL, DMSO: 4 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

関連するカテゴリー

General description

A cell-permeable pyrrazolopyrimidine compound that inhibits against KDR/VEGFR2, ALK2/BMPR-I, AMPK kinase activity (IC50 = 25.1, 148, and 234.6 nM, respectively), while exhibiting much reduced or little effect toward ALK5/TGFβR-I, ZAPK, Syk, PKCθ, PKA, or JAK3. Shown to block both BMP pathway-dependent dorsoventral development (EC100 = 2.5 µM) and VEGF signaling-dependent intersomitic vessel formation (EC50 = 5 µM) in zebrafish embryo in vivo. Commonly used in combination with AMPK activators AICAR (Cat. No. 123040) and/or Metformin (Cat. No. 317240) for studying AMPK-dependent cellular events in vitro and physiological responses in animals in vivo. Also available as a 10 mM solution in DMSO (Cat. No. 171261).

Biochem/physiol Actions

Cell permeable: yes
EC100 = 2.5 µM against BMP pathway-dependent dorsoventral development; EC50 = 5 µM against VEGF signaling-dependent intersomitic vessel formation in zebrafish embryo in vivo
Primary Target
AMPK
Product competes with ATP.
Reversible: yes
Target IC50: 25.1, 148, and 234.6 nM, against KDR/VEGFR2, ALK2/BMPR-I, AMPK kinase activity, respectively

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Hao, J., et al. 2010. ACS Chem.Biol.5, 245.
Yu, P.B., et al. 2008. Nat. Chem. Biol4, 33.
Kim, E.K., et al. 2004. J. Biol. Chem.279, 19970.
Lee, M., et al. 2003. J. Biol. Chem.278, 39653.
Inoki, K., et al. 2003. Cell115, 577.
Fryer, L.G., 2002. FEBS Lett.531, 189.
Zhou, G., et al. 2001. J. Clin. Invest.108, 1167.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

保管分類

11 - Combustible Solids

wgk

WGK 3

適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

171260-100MG: + 171260-10MG: + 171260-1MG: + 171260-MG: + 171260-5MG: + 171260-1.1ML: + 171260-5UNMG:

jan

試験成績書（COA）

製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。

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文書ライブラリで、最近購入した製品の文書を検索できます。

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Mohamadreza Savaee et al.
Reports of biochemistry & molecular biology, 11(1), 157-165 (2022-06-30)
Prostate cancer is known as one of the most prevalent health disorders in the male population globally. The aim of the current study was to evaluate the effects of separate and concomitant use of MK-2206 and salinomycin on prostate cancer
Xi Mei et al.
Behavioural brain research, 379, 112344-112344 (2019-11-11)
The pathogenesis of postoperative cognitive impairment of obstructive sleep apnea-hypopnea syndrome (OSAHS) individuals remains unclear. AMP activated protein kinase (AMPK) is a ubiquitous sensor/effector of cell stresses. Thus we detected the role and underlying mechanisms of AMPK in postoperative cognitive
Jian Wen et al.
The Turkish journal of gastroenterology : the official journal of Turkish Society of Gastroenterology, 32(1), 97-105 (2021-04-25)
Bile acid metabolism is a contributing factor that promotes cholelithiasis. Recent studies have suggested novel roles of leptin in the formation of gallbladder stones (GS); however, no evidence confirmed the function of leptin in the formation of primary intrahepatic bile
Weixin Li et al.
Immunopharmacology and immunotoxicology, 43(4), 431-442 (2021-06-24)
Acute lung injury (ALI) is a devastating lung disease characterized by uncontrolled pulmonary inflammation and oxidative stress. Currently, no effective therapeutic strategies are available for ALI and its prognosis remains poor. The present study aims to investigate the role and
Dong Liang et al.
Scientific reports, 6, 21914-21914 (2016-02-24)
Mesenchymal stem cells (MSCs)-based therapy provides a promising avenue for the management of peripheral arterial disease (PAD). However, engrafted MSCs are subjected to acute cell death in the ischemic microenvironment. Apelin has been shown to protect bone marrow MSCs against
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グローバルトレードアイテム番号

カタログ番号GTIN
171260-5MGCN04055977207163
171260-10MGCN04055977207156
171260-1MGCN04055977207149

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