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  3. A-971432

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。

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A-971432 Chemical Structure

A-971432 Chemical Structure

CAS No. : 1240308-45-5

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A-971432 is a potent, selective and orally active sphingosine-1-phosphate (S1P) receptor 5 agonist with IC50s of .362, >10, 0.006 µM for S1P1, S1P3, S1P5 respectively. A-971432 protects blood–brain barrier (BBB) homeostasis. A-971432 reverses age-related cognitive decline. A-971432 has the potential for the research of alzheimer’s disease or multiple sclerosis [1][2].

IC50 & Target

S1P5[1][2]

体外研究
(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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

A-971432 (1, 2 mg/kg; p.o.) shows excellent PK characteristics and oral bioavailability[1].
A-971432 (0.1 mg/kg; P.o.; daily for 21 days) shows pro-cognitive impact in a dose-dependent manner[1].
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[2].
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[2].
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[2].
Pharmacokinetic Parameters of A-971432 in Balb/C mice, SD rat, beagle dog, cyno monkey[1].

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
Balb/C mice, SD rat, beagle dog, cyno monkey; p.o. or i.v.; 2 mg/kg for Balb/C mice, SD rat; 1mg/kg for SD rat, beagle dog, cyno monkey[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/C mice, SD rat, beagle dog, cyno monkey[1]
Dosage: 1, 2 mg/kg
Administration: P.o. or i.v.
Result: Showed high oral bioavailability, high exposure, low clearance, a long half-life.
Animal Model: Male C57BL6J mice[1]
Dosage: 0.1 mg/kg
Administration: P.o.; daily for 21 days
Result: Showed pro-cognitive impact in a dose-dependent manner.
Animal Model: 7-week R6/2 mice[2]
Dosage: 0.1 mg/kg
Administration: I.p.; daily for 4 weeks
Result: Restored normal motor function within the first week of treatment, and preserved them from the gradual motor deficit, classically occurring during the disease, for the entire period of the treatment.
Animal Model: 4-week R6/2 mice[2]
Dosage: 0.1 mg/kg
Administration: I.p., daily for 2 weeks
Result: Preserved BBB integrity and delayed the onset of motor symptoms in R6/2 mice and suppressed aggregation of mHtt in the CNS blood vessels.
分子量

366.24

Formula

C18H17Cl2NO3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 3 mg/mL (8.19 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7304 mL 13.6523 mL 27.3045 mL
5 mM 0.5461 mL 2.7304 mL 5.4609 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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浓度
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分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

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动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

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动物的平均体重

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每只动物的给药体积

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工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥99.0%

参考文献

A-971432 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7305 mL 13.6523 mL 27.3045 mL 68.2613 mL
5 mM 0.5461 mL 2.7305 mL 5.4609 mL 13.6523 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
A-971432
目录号:
HY-110291
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