923262-96-8
SAR407899 (hydrochloride)(SAR407899 (hydrochloride))
CAS: 923262-96-8
化学式: C14H17ClN2O2
| 中文名 | SAR407899 (hydrochloride) |
| 英文名 | SAR407899 (hydrochloride) |
| 别名 | 6-(4-哌啶基氧基)-1(2H)-异喹啉酮盐酸盐 6-(哌啶-4-氧基)异喹啉-1(2H)-酮盐酸盐 ROCK激酶抑制剂(SAR407899 HYDROCHLORIDE) |
| 英文别名 | SAR407899 SAR 407899 SAR-407899 SAR407899 HCl SAR407899 (hydrochloride) 6-(piperidin-4-yloxy)isoquinolin-1(2h)-one hcl 6-(4-Piperidinyloxy)-1(2H)-isoquinolinone hydrochloride 6-(piperidin-4-yloxy)isoquinolin-1(2H)-one hydrochloride |
| CAS | 923262-96-8 |
| 化学式 | C14H17ClN2O2 |
| 分子量 | 280.74998 |
| 溶解度 | 溶于DMSO |
| 存储条件 | -20℃ |
| 产品用途 | SAR407899 is a potent and selective Rho kinase inhibitor with promising antihypertensive activity. SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries. SAR407899 is equipotent against human and rat-derived Rho-kinase 2 with inhibition constant values of 36 nM and 41 nM, respectively. SAR407899 is approximately 8-fold more active than fasudil. SAR407899 potently (mean IC(50) values: 122 to 280 nM) and species-independently relaxed precontracted isolated arteries of different species and different vascular beds. The antihypertensive effect of SAR407899 was superior to that of fasudil and Y-27632. |
| 上游原料 | 4-氟-2-甲基苯腈 |
| 参考资料 展开查看 | 1: Löhn M, Plettenburg O, Kannt A, Kohlmann M, Hofmeister A, Kadereit D, Monecke P, Schiffer A, Schulte A, Ruetten H, Ivashchenko Y. End-organ protection in hypertension by the novel and selective Rho-kinase inhibitor, SAR407899. World J Cardiol. 2015 Jan 26;7(1):31-42. doi: 10.4330/wjc.v7.i1.31. PubMed PMID: 25632317; PubMed Central PMCID: PMC4306204. 2: Babelova A, Jansen F, Sander K, Löhn M, Schäfer L, Fork C, Ruetten H, Plettenburg O, Stark H, Daniel C, Amann K, Pavenstädt H, Jung O, Brandes RP. Activation of Rac-1 and RhoA contributes to podocyte injury in chronic kidney disease. PLoS One. 2013 Nov 7;8(11):e80328. doi: 10.1371/journal.pone.0080328. eCollection 2013. PubMed PMID: 24244677; PubMed Central PMCID: PMC3820652. 3: Guagnini F, Ferazzini M, Grasso M, Blanco S, Croci T. Erectile properties of the Rho-kinase inhibitor SAR407899 in diabetic animals and human isolated corpora cavernosa. J Transl Med. 2012 Mar 23;10:59. doi: 10.1186/1479-5876-10-59. PubMed PMID: 22444253; PubMed Central PMCID: PMC3328245. 4: Grisk O, Schlüter T, Reimer N, Zimmermann U, Katsari E, Plettenburg O, Löhn M, Wollert HG, Rettig R. The Rho kinase inhibitor SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries. J Hypertens. 2012 May;30(5):980-9. doi: 10.1097/HJH.0b013e328351d459. PubMed PMID: 22388233. |
923262-96-8 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.562 ml | 17.809 ml | 35.619 ml |
| 5 mM | 0.712 ml | 3.562 ml | 7.124 ml |
| 10 mM | 0.356 ml | 1.781 ml | 3.562 ml |
| 5 mM | 0.071 ml | 0.356 ml | 0.712 ml |
最后更新：2024-01-02 23:10:35
923262-96-8 - 动物实验
Rabbits are treated either intravenously (i.v., in an ear vein) with increasing doses of SAR407899 (0.3, 1, 3, 10 mg/kg) or orally with SAR407899 (1, 3, 10, 30 mg/kg) or sildenafil (2 or 6 mg/kg). Each animal is used several times for different doses and different agents, always with a week's washout. The length (mm) of uncovered penile mucosa (penile erection parameter) is measured at different time-points, using a sliding digital caliper. The results are expressed as mean ± SEM penile length of 3-5 rabbits.
最后更新：2023-08-16 21:32:38
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现货供应
产品名: SAR407899 (hydrochloride) 去供应商网站查看 询盘CAS: 923262-96-8
产地: 中国上海
包装: 10mg
规格: 99%
价格: 8122.00
库存: 5个工作日
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：SAR407899 (hydrochloride) 英文名:SAR407899 (hydrochloride) CAS:923262-96-8 规格:9 更多
现货供应
产品名: SAR407899 hydrochloride 去供应商网站查看 询盘CAS: 923262-96-8
产地: 上海
规格: S911625
价格: 5mg-661
库存: 7天内发货
电话: 13816333479/13918391375
手机: 13816333479/13918391375
电子邮件: wangrui@macklin.cn
QQ: 2885703204/285395191
微信: 19863730987/13918391375
现货供应
产品名: SAR407899 (hydrochloride) 去供应商网站查看 询盘CAS: 923262-96-8
产地: 上海
规格: 99%
价格: 5mg 560,10mg 800,25mg 1600,100mg 4800
库存: 现货
电话: 18301782025
手机: 18301782025
电子邮件: 3008007403@qq.com
QQ: 3008007403
微信: 18301782025
产品描述: SAR407899 (hydrochloride) 99% MedMol 货号：S87293
现货供应
产品名: SAR407899 (hydrochloride) 去供应商网站查看 询盘CAS: 923262-96-8
产地: 中国上海
包装: 10mg
规格: 99%
价格: 8122.00
库存: 5个工作日
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：SAR407899 (hydrochloride) 英文名:SAR407899 (hydrochloride) CAS:923262-96-8 规格:9 更多
现货供应
产品名: SAR407899 hydrochloride 去供应商网站查看 询盘CAS: 923262-96-8
产地: 上海
规格: S911625
价格: 5mg-661
库存: 7天内发货
电话: 13816333479/13918391375
手机: 13816333479/13918391375
电子邮件: wangrui@macklin.cn
QQ: 2885703204/285395191
微信: 19863730987/13918391375
现货供应
产品名: SAR407899 (hydrochloride) 去供应商网站查看 询盘CAS: 923262-96-8
产地: 上海
规格: 99%
价格: 5mg 560,10mg 800,25mg 1600,100mg 4800
库存: 现货
电话: 18301782025
手机: 18301782025
电子邮件: 3008007403@qq.com
QQ: 3008007403
微信: 18301782025
产品描述: SAR407899 (hydrochloride) 99% MedMol 货号：S87293
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