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A-971432 

Cat. No.: HY-110291
Handling Instructions

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 .

For research use only. We do not sell to patients.

A-971432 Chemical Structure

A-971432 Chemical Structure

CAS No. : 1240308-45-5

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Description

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].

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

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.
Molecular Weight

366.24

Formula

C18H17Cl2NO3

CAS No.
SMILES

O=C(C1CN(C1)CC2=CC=C(C=C2)OCC3=CC=C(C(Cl)=C3)Cl)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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A-971432
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HY-110291
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