A-971432
CAS No. : 1240308-45-5
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|---|---|---|
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| 5mg | $211 | In-stock |
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| Cat. No. : | HY-110291 |
| M.Wt: | 366.24 |
| Formula: | C18H17Cl2NO3 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
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]
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].
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 |
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