A-971432 |
| رقم الكتالوجGC42664 |
A-971432 هو ناهض لمستقبلات سفينغوزين -1 فوسفات (S1P) فعال وانتقائي ونشط عن طريق الفم مع IC50s من .362 ،> 10 ، 0.006 ميكرومتر لـ S1P1 ، S1P3 ، S1P5 على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1240308-45-5
Sample solution is provided at 25 µL, 10mM.
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A-971432 is a sphingosine-1-phosphate receptor 5 (S1P5) agonist that is selective for S1P5 over S1P1 and S1P3 (IC50s = 0.006, 0.362, and >10 µM, respectively). It inhibits forskolin-induced cAMP production in CHO cells expressing S1P5 (EC50 = 4.1 nM). A-971432 (1 µM) increases electrical resistance of hCMEC/D3 cells in an in vitro blood-brain barrier model, indicating enhanced barrier integrity, and attenuates blood-brain barrier leakage in an R6/2 transgenic mouse model of Huntington’s disease when administered at a dose of 0.1 mg/kg.[1] [2] A-971432 (0.1 mg/kg per day, i.p.) decreases the number of errors made in a horizontal ladder task and increases latency to fall in the rotarod test in R6/2 mice. It also increases spontaneous alternation in the t-maze in aged mice when administered at a dose of 0.1 mg/kg.[1]
References
[1].Hobson, A.D., Harris, C.M., van der Kam, E.L., et al. Discovery of A-971432, an orally bioavailable selective sphingosine-1-phosphate receptor 5 (S1P5) agonist for the potential treatment of neurodegenerative disorders. J. Med. Chem. 58(23), 9154-9170 (2015).
[2]. Di Pardo, A., Castaldo, S., Amico, E., et al. Stimulation of S1PR5 with A-971432, a selective agonist, preserves blood-brain barrier integrity and exerts therapeutic effect in an animal model of Huntington’s disease. Hum. Mol. Genet. 27(14), 2490-2501 (2018).
| Cas No. | 1240308-45-5 | SDF | |
| Chemical Name | 1-[[4-[(3,4-dichlorophenyl)methoxy]phenyl]methyl]-3-azetidinecarboxylic acid | ||
| Canonical SMILES | ClC1=C(Cl)C=C(COC2=CC=C(CN3CC(C(O)=O)C3)C=C2)C=C1 | ||
| Formula | C18H17Cl2NO3 | M.Wt | 366.2 |
| الذوبان | Slightly soluble in chloroform | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7307 mL | 13.6537 mL | 27.3075 mL |
| 5 mM | 0.5461 mL | 2.7307 mL | 5.4615 mL |
| 10 mM | 0.2731 mL | 1.3654 mL | 2.7307 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)
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