2310134-98-4
4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline tetrahydrochloride(LDN193189 Tetrahydrochloride)
CAS: 2310134-98-4
化学式: C25H23ClN6
| 中文名 | 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline tetrahydrochloride |
| 英文名 | LDN193189 Tetrahydrochloride |
| 英文别名 | LDN193189 Tetrahydrochloride |
| CAS | 2310134-98-4 |
| 化学式 | C25H23ClN6 |
| 分子量 | 442.95 |
| 存储条件 | 2-8°C，密封，干燥 |
| 外观 | 固体 |
| 体外研究 | LDN193189 inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with greater potency than did dorsomorphin (IC 50 =5 nM versus 470 nM) while retaining 200-fold selectivity for BMP signaling versus TGF-β signaling (IC 50 for TGF-β ≥1,000 nM). LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC 50 =5 nM and 30 nM, respectively), and the TGF-β type I receptors ALK4, ALK5 and ALK7 (IC 50 ≥500 nM) and increases selectivity for BMP signaling versus AMP-activated protein kinase, PDGFR and MAPK signaling pathways as compared to the parent compound. LDN193189 blocks the transcriptional activity induced by either constitutively active ALK2 R206H or ALK2 Q207D mutant proteins. These findings suggest that LDN193189 might affect BMP-induced osteoblast differentiation. In fact, LDN193189 inhibits the induction of alkaline phosphatase activity in C2C12 cells by BMP4 even when administered 12 h after BMP stimulation, indicating sustained BMP signaling activity is needed for osteogenic differentiation. |
| 体内研究 | In the first experiment, LDN193189 (3 mg/kg) is injected intraperitoneally twice a day after tumors became palpable 7 days post-implantation. The growth rates between the control vehicle- and LDN193189-treated mice are not significantly different after the first 5 weeks, but differences in the growth rates are detected after 6 and 7 weeks post-treatment. In the second experiment, cells are isolated from PCa-118b tumors and injected subcutaneously into SCID mice (1×10 6 cells per mouse). LDN193189 or vehicle is applied to mice 5 days post-tumor cell injection before tumors are palpable. The differences in the average growth rates between these two groups, as measured by tumor size, are significant at 6 and 7 weeks post-treatment. The tumor weights also show significant differences at the termination of the study at week 7. The X-ray of the tumors shows that the ectopic bone volume and bone density are reduced in the tumors of LDN193189-treated group compared to that of controls. Co-incubation of pulmonary arterial smooth muscle cells (PASMCs) from the pulmonary arterial hypertension (PAH) rats with UK-92480 and LDN193189 completely inhibited the anti-proliferation and up-regulation of the bone morphogenetic protein (BMPR2) and Cx40 expression by the UK-92480. |
2310134-98-4 - 简介
4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline tetrahydrochloride是一种有机化合物，其化学结构中包含喹啉和吡唑并咪唑环。
该化合物的性质是固体状的，多为白色或类似白色的粉末。它在常温下是溶于水和一些有机溶剂的。
它的用途还在不断扩展。
一般情况下，它可以通过化学合成方法合成。
安全信息：应该注意合理的操作。该化合物作为研究用途，对它的安全性和毒性的数据可能有限。在实验操作中需要遵循相关的安全操作规范，并采取适当的个人防护措施，如佩戴手套、护目镜和防护服。
该化合物的性质是固体状的，多为白色或类似白色的粉末。它在常温下是溶于水和一些有机溶剂的。
它的用途还在不断扩展。
一般情况下，它可以通过化学合成方法合成。
安全信息：应该注意合理的操作。该化合物作为研究用途，对它的安全性和毒性的数据可能有限。在实验操作中需要遵循相关的安全操作规范，并采取适当的个人防护措施，如佩戴手套、护目镜和防护服。
最后更新：2024-04-09 21:04:16
供应商列表
现货供应
产品名: LDN193189 Tetrahydrochloride 去供应商网站查看 询盘CAS: 2310134-98-4
产地: 中国上海
包装: 2mg
规格: 98%
价格: 698.00
库存: 现货
电话: 400-900-4166
手机: 18017137653
电子邮件: 3007523013@qq.com
QQ: 3007523013
微信: 18017137653
产品描述: 中文名：LDN193189 Tetrahydrochloride 英文名:LDN193189 Tetrahydrochloride CAS:2310134-98 更多
现货供应
产品名: 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline tetrahydrochloride 去供应商网站查看 询盘CAS: 2310134-98-4
产地: 上海
规格: L937425
价格: 5mg-1026,50mg-6480,10mg-1728
库存: 7天内发货
电话: 13816333479/17821173903
手机: 13816333479/17821173903
电子邮件: wangrui@macklin.cn
QQ: 2885703204/288570320
微信: 19863730987/17821173903
现货供应
产品名: LDN193189 Tetrahydrochloride 去供应商网站查看 询盘CAS: 2310134-98-4
产地: 中国上海
包装: 2mg
规格: 98%
价格: 698.00
库存: 现货
电话: 400-900-4166
手机: 18017137653
电子邮件: 3007523013@qq.com
QQ: 3007523013
微信: 18017137653
产品描述: 中文名：LDN193189 Tetrahydrochloride 英文名:LDN193189 Tetrahydrochloride CAS:2310134-98 更多
现货供应
产品名: 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline tetrahydrochloride 去供应商网站查看 询盘CAS: 2310134-98-4
产地: 上海
规格: L937425
价格: 5mg-1026,50mg-6480,10mg-1728
库存: 7天内发货
电话: 13816333479/17821173903
手机: 13816333479/17821173903
电子邮件: wangrui@macklin.cn
QQ: 2885703204/288570320
微信: 19863730987/17821173903
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