|4-(6-(4-(哌嗪-1-基)苯基)吡唑并[1,5-a]嘧啶-3-基)喹啉盐酸盐|CsnPharm

CAS No.: 1062368-62-0

4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline hydrochloride Catalog No. CSN13849

Synonyms: LDN-193189 Hydrochloride

LDN-193189 HCl is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 ALK2

IC50:5nM ALK3

IC50:30nM
描述BMPs (Bone morphogenetic proteins) represent the largest subgroup in the TGFβ family of extracellular ligands. Their signaling transduction requires the interaction with the type I and type II transmembrane receptor kinase. Type I receptors, such as ALK1/ACVRL1, ALK2/ACVR1, ALK3/BMPR1A and ALK6/BMPR1B all participate in BMP signalling and phosphorylate SMAD1/5/ 8 phosphorylate SMAD family transcription factors. Dysregulation of this pathway links to many disease conditions, for example, fibrodysplasia ossificans progressive^[1]. LDN-193189 is a selective inhibitor of BMP type I receptors with IC50 values of 5 nM and 30 nM for ALK2 and ALK3 (measured by p-Smad1/5/8 in PASMCs), respectively, with substantially weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM). PASMCs treated with LDN-193189 on concentration at 2 - 250 nM showed dose-dependent inhibition on p-Smad1/5/8 induced by BMP4 (10 ng/ml), while retaining 200-fold selectivity for BMP signaling versus TGF-β signaling (IC50≥1000 nM). Even LDN-193189 can block the transcriptional activity induced by either constitutively active ALK2^R206H or ALK2^Q207D mutant proteins. Intraperitoneal injection with LDN-193189 on dose of 3 mg/kg, every 12 h, resulted in a reduction in ectopic ossification and functional impairment in ALK2^Q207D mutant mice^[2]. Use of LDN-193189 combined with different small molecular led to the effective generation from ESCs of paraxial mesodermal progeny, and to their further differentiation in vitro through sclerotome specification into growth plate-like chondrocytes^[3]. Inhibition of BMP signaling by LDN-193189 can inhibit endothelial cell differentiation in the ventral blood island^[4].
作用机制LDN-193189 targets to the ATP-binding pocket located within the intracellular kinase domain of the receptors^[1].

动物研究

剂量

Mice: 2.5 mg/kg^[5] (i.p.), 10 mg/kg^[6] (i.p.), max = 35 mg/kg^[7] (p.o.)

给药途径

i.p., p.o.

动物药代数据

Animal	Mice^[8]
Dose	3 mg/kg
Administration	i.p.
C_max	1.54 μM
T_1/2	1.6 h
AUC_∞	994 ng·h/ml
T_max	< 5 min

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2576 mL
- 11.2881 mL
- 22.5763 mL
- 5 mM
- 0.4515 mL
- 2.2576 mL
- 4.5153 mL
- 10 mM
- 0.2258 mL
- 1.1288 mL
- 2.2576 mL

技术信息

CAS号	1062368-62-0	储存条件	粉末 Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C25H23ClN6	运输	蓝冰
分子量	442.94	别名	LDN-193189 Hydrochloride

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靶点	Description	IC50
ALK2		IC50:5nM
ALK3		IC50:30nM

4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline hydrochloride Catalog No. CSN13849

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