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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1240308-45-5
- 规格：
1 mg/5 mg
| 规格： | 1 mg | 产品价格： | ￥900.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥2110.0 |
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A-971432
CAS No. : 1240308-45-5
MCE 国际站：A-971432
产品活性：A-971432 是一种有效的、选择性的和具有口服活性的 1-磷酸鞘氨醇 (S1P) 受体 5 激动剂，S1P1、S1P3、S1P5 的 IC50s 分别为 0.362， >10， 0.006 µM。A-971432 保护血脑屏障 (BBB) 稳态。A-971432 可逆转与年龄相关的认知衰退。A-971432 具有研究阿尔茨海默病或多发性硬化症的潜力。
研究领域：Others
作用靶点：Others
In Vitro: A-971432 (compound 29) (0-10 µM) shows selectivity with IC50s of 0.362, >10, 0.006 µM for S1P1, S1P3, S1P5 respectively.
A-971432 (0.1-1000 nM) induces full agonism with an EC50s of 5.7 nM and 4.1 nM for HEK cells and CHO cells, respectively.
In Vivo: A-971432 (1, 2 mg/kg; p.o.) shows excellent PK characteristics and oral bioavailability.
A-971432 (0.1 mg/kg; P.o.; daily for 21 days) shows pro-cognitive impact in a dose-dependent manner.
A-971432 (11 weeks R6/2 mice; 0.1 mg/kg; i.p.) increases the phosphorylation of AKT and ERK and significantly incremented the levels of BDNF in the cortex.
A-971432 (0.1 mg/kg; i.p.) attenuates the classic progressive BBB leakage and therefore the FITC-albumin extravasation in striatal parenchyma, and protects blood–brain barrier (BBB) homeostasis and suppresses aggregation of mHtt in the CNS blood vessels.
A-971432 (0.1 mg/kg; i.p.; daily for 4 weeks) prevents the worsening of motor deficit in symptomatic R6/2 mice by chronic infusion.
Pharmacokinetic Parameters of A-971432 in Balb/C mice, SD rat, beagle dog, cyno monkey.
| IV | PO | |||||||||||
| species | dose (mg/kg) | sample analyzed) | protein binding (%) | t1/2 (h) | AUC (ng.h/mL) | VL (L/h/kg) | Vss(L/kg) | t1/2 (h) | tmax (h) | Cmax (ng/mL) | AUC (ng.h/mL) | F(%) |
| BALB/C mouse | 2 | plasma | 93 | 7.6 | 8500 | 0.24 | 1.9 | 7.4 | 2.0 | 300 | 4800 | 57 |
| BALB/C mouse | 2 | brain | nd | 9.8 | 3200 (Cmax=133 ng/nL) | nd | nd | 10 | 2-24 | 43 | 1600 | 56 |
| SD rat | 1 | plasm | 93 | 9.0 | 6400 | 0.16 | 1.3 | 14 | 4.3 | 400 | 8700 | >100 |
| SD rat | 2 | brain | 99.5 | nd | nd | nd | nd | 15 | 8 | 120 | 3100 | nd |
| beagle dog | 1 | plasma | 96 | 9.3 | 12000 | 0.09 | 1.2 | 10 | 1.5 | 690 | 11000 | 92 |
| cyno monkey | 1 | plasma | 97 | 3.5 | 6400 | 0.16 | 0.82 | 6.7 | 1.7 | 650 | 5500 | 86 |
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文献和实验μL 体系 2× MasterMix 25 μL 上游 Primer （ 10 μM 1-5 μL 下游 Primer （ 10 μM ） 1-5 μL 模板 lamid DNA ～ 50 ng genomic DNA ～ 1000 ng cDNA ～ 500 ng 粗提液 ～ 2 μL 灭菌蒸馏水至 50 μL PCR 扩增实例： 一、plasmid DNA 扩增 1．提取的质粒 DNA 扩增 以pUC19 质粒为模板扩增 100，250，500
Lipoprotein Isolation - First week
, refractometry and dialysis. Day 3 Lyophilization. Day 1: Bleeding and centrifugation. Note: You need to wear gloves throughout the procedure. Each groups takes 10-15 locusts. 1. Take 2-5 ml of PBS in a clean
Lipoprotein Isolation - First week
3 Lyophilization. Day 1: Bleeding and centrifugation. Note: You need to wear gloves throughout the procedure. Each groups takes 10-15 locusts. 1. Take 2-5 ml of PBS in a clean 100 ml beaker and add 25 µl of 200 mM PMSF
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