计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC 50 of 135 nM for ROCK-2 , and K i s of 36 nM and 41 nM for human and rat ROCK-2 , respectively. SAR407899 shows stable inhibition of migrasome formation.
In Vitro
SAR407899 is a potent and ATP-competitive ROCK inhibitor, with K i s of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 inhibits ROCK-2 better than ROCK-1, with IC 50 s of 102 ± 19 nM and 276 ± 26 nM, respectively, in the presence of 40 μM ATP. SAR407899 also less potently inhibits PKC-Δ and MSK-1, with IC 50 s of 5.4 and 3.1 μM, respectively. SAR407899 (0.1, 0.3, 1.0, and 3.0 μM) specifically inhibits the ROCK-mediated phosphorylation of MYPT T696 in HeLa cells stimulated with PHEN, and shows such effects at 1 μM and 10 μM in primary rat aortic smooth muscle cells. SAR407899 (3 μM) completely blocks thrombin-induced shrinkage of human umbilical vein endothelial cells (HUVECs) and stress fiber formation. SAR407899 concentration-dependently inhibits 5-bromodeoxyuridine incorporation into the cells with an IC 50 of 5.0 ± 1.3 μM. SAR407899 also effectively inhibits THP-1 migration with an IC 50 of 2.5 ± 1.0 μM. SAR407899 shows a potent vasorelaxant activity in a broad variety of isolated arteries taken from different vascular beds and species, with a range of IC 50 values between 122 and 280 nM. SAR407899 dose-dependently relaxes the phenylephrine pre-contracted smooth muscle, with IC 50 s of 0.07 and 0.05 μM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SAR407899 (3 mg/kg, i.v.) inhibits ROCK-mediated phosphorylation of MYPT T696 in thoracic aorta of spontaneously hypertensive rats (SHRs). SAR407899 (0.01-0.30 mg/kg, i.v.) efficiently reduces pressor responses to vasoconstrictor agents in rats. SAR407899 (1, 3, 10, and 30 mg/kg, p.o.) dose dependently lowers blood pressure in hypertensive SHRs . SAR407899 (1-3 mg/kg, i.v. or 3, 10 mg/kg, p.o.) increases the length of the penis in healthy rabbits. SAR407899 (3-10 mg/kg, p.o.) also dose-dependently increases penile length in diabetic rabbits. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal administration
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 . aladdin has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:ROCK-2 102 nM (IC 50 ) ROCK-1 276 nM (IC 50 )
规格
规格或纯度
10mM in DMSO
英文名称
SAR407899
生化机理
SAR407899 是一种选择性、强效和 ATP 竞争性 ROCK 抑制剂，对 ROCK-2 的 IC 50 为 135 nM，对人类和大鼠 ROCK-2 的 K i s 分别为 36 nM 和 41 nM。SAR407899 能稳定抑制迁移体的形成。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CNCCC1OC2=CC3=C(C=C2)C(=O)NC=C3
关联CAS
PubChem CID
分子量
244.29
技术文档
高级数据
关联靶点（人）
ROCK2
Tclin
Rho 相关蛋白激酶 2(Rho-associated protein kinase 2)
(1 活性数据)
ROCK1
Tclin
Rho 相关蛋白激酶 1(Rho-associated protein kinase 1)
(1 活性数据)
PKN1
Tchem
丝氨酸/苏氨酸蛋白激酶N1(Serine/threonine-protein kinase N1)
(1 活性数据)
PKN2
Tchem
丝氨酸/苏氨酸蛋白激酶N2(Serine/threonine-protein kinase N2)
(1 活性数据)
PRKG1
Tchem
cGMP依赖性蛋白激酶1(cGMP-dependent protein kinase 1)
(1 活性数据)
PRKCD
Tclin
蛋白激酶 C δ 型(Protein kinase C delta type)
(1 活性数据)
CDC42BPA
Tchem
丝氨酸/苏氨酸蛋白激酶 MRCK α(Serine/threonine-protein kinase MRCK alpha)
(1 活性数据)
BMP2K
Tchem
BMP-2诱导蛋白激酶(BMP-2-inducible protein kinase)
(1 活性数据)
Tchem
未表征蛋白 FLJ45252(Uncharacterized protein FLJ45252)
(1 活性数据)
AAK1
Tchem
AP2 相关蛋白激酶 1(AP2-associated protein kinase 1)
(1 活性数据)
PRKACA
Tchem
cAMP 依赖性蛋白激酶催化亚基 α(cAMP-dependent protein kinase catalytic subunit alpha)
(1 活性数据)
CDC42BPB
Tchem
丝氨酸/苏氨酸蛋白激酶 MRCK β(Serine/threonine-protein kinase MRCK beta)
(1 活性数据)
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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