021-51111890
购物车（0）
sales@molnova.cn
SB-649868
CAS No. 380899-24-1
SB-649868 ( SB 649868 | SB649868 )
产品货号. M14316 CAS No. 380899-24-1
一种有效的、选择性的、口服生物可利用的双重食欲素 OX1/OX2R 拮抗剂，pKi 分别为 9.4 和 9.5。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥2633 | 有现货 |
|
| 10MG | ￥4147 | 有现货 |
|
| 25MG | ￥6747 | 有现货 |
|
| 50MG | ￥9315 | 有现货 |
|
| 100MG | ￥12555 | 有现货 |
|
| 200MG | 获取报价 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
-
产品名称SB-649868
-
注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
-
产品简述一种有效的、选择性的、口服生物可利用的双重食欲素 OX1/OX2R 拮抗剂，pKi 分别为 9.4 和 9.5。
-
产品描述A potent, selective, orally bioavailable, dual orexin OX1/OX2R antagonist with pKi of 9.4 and 9.5 respectively; displays >1,000-fold selectivity for the orexin target receptors in a broad panel of GPCRs, ion channels and enzymes; demonstrates high effectivity in pre-clinical model of sleep disorders.Sleep Disorder Phase 2 Discontinued(In Vitro):SB-649868 is identified as one the most in vitro potent dual OX1 and OX2 receptor antagonist known at that time (pKi=9.4 and 9.5 at the OX1 and OX2 receptor, respectively) . SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67; OX2=9.64). SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values: OX1=9.27; OX2=8.91. Increasing concentrations of SB-649868 (0.3 nM-30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior. The calculated apparent pKb values are 9.67±0.03 and 9.64±0.07 for OX1 and OX2.
-
体外实验SB-649868 is identified as one the most in vitro potent dual OX1 and OX2 receptor antagonist known at that time (pKi=9.4 and 9.5 at the OX1 and OX2 receptor, respectively) . SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67; OX2=9.64). SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values: OX1=9.27; OX2=8.91. Increasing concentrations of SB-649868 (0.3 nM-30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior. The calculated apparent pKb values are 9.67±0.03 and 9.64±0.07 for OX1 and OX2.
-
体内实验——
-
同义词SB 649868 | SB649868
-
通路GPCR/G Protein
-
靶点Orexin Receptor
-
受体Orexin Receptor
-
研究领域Neurological Disease
-
适应症Sleep Disorder
化学信息
-
CAS Number380899-24-1
-
分子量477.554
-
分子式C26H24FN3O3S
-
纯度>98% (HPLC)
-
溶解度In Vitro:?DMSO : 100 mg/mL (209.40 mM)
-
SMILESO=C(C1=C2C=COC2=CC=C1)NC[C@H]3N(C(C4=C(C5=CC=C(F)C=C5)SC(C)=N4)=O)CCCC3
-
化学全称(S)-N-((1-(5-(4-fluorophenyl)-2-methylthiazole-4-carbonyl)piperidin-2-yl)methyl)benzofuran-4-carboxamide
运输与储存
-
储存条件(-20℃)
-
运输条件With Ice Pack
-
稳定性≥ 2 years
参考文献
1. Renzulli C, et al. Drug Metab Dispos. 2011 Feb;39(2):215-27.
2. Bettica P, et al .Neuropsychopharmacology. 2012 Apr;37(5):1224-33.
3. Piccoli L, et al. Neuropsychopharmacology. 2012 Aug;37(9):1999-2011.
4. Di Fabio R, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7.
产品手册
关联产品
-
SB-334867 free base
第一个选择性 Orexin-1 受体拮抗剂，pKb 为 7.4。
-
[Ala11,D-Leu15]-Orex...
Highly potent and selective OX2 receptor agonist; displays 400-fold selectivity over OX1 receptors. EC50 values are 0.13 and 52 nM for human OX2 and OX1 receptors respectively.
-
L-368,899 hydrochlor...
L-368,899 盐酸盐是一种有效的、选择性的、口服生物可利用的、非肽催产素受体拮抗剂，用作宫缩剂时，对大鼠子宫和人子宫催产素受体的 IC50 值分别为 8.9 nM 和 26 nM。
