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  4. A-971432

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 .

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A-971432 Chemical Structure

A-971432 Chemical Structure

CAS No. : 1240308-45-5

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Based on 1 publication(s) in Google Scholar

A-971432 Related Antibodies

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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]
Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.362 μM
Compound: 29; A-971432
Agonist activity at S1P1 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
Agonist activity at S1P1 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding based MFB method
[PMID: 26509640]
CHO EC50
4.1 nM
Compound: 29; A-971432
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
[PMID: 26509640]
CHO EC50
5.7 nM
Compound: 29; A-971432
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay
[PMID: 26509640]
HEK293 IC50
> 10 μM
Compound: 29; A-971432
Displacement of [33P]S1P from S1P3 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
Displacement of [33P]S1P from S1P3 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
[PMID: 26509640]
HEK293 IC50
0.006 μM
Compound: 29; A-971432
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
Displacement of [33P]S1P from S1P5 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
[PMID: 26509640]
HEK293 IC50
0.362 μM
Compound: 29; A-971432
Displacement of [33P]S1P from S1P1 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
Displacement of [33P]S1P from S1P1 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method
[PMID: 26509640]
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].

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

A-971432 Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 3 mg/mL (8.19 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: ≥99.0%

SDS (251 KB)

COA (245 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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A-971432 Related Classifications

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.

Keywords:

A-9714321240308-45-5A971432A 971432Otherselectiveorally activeblood?brain barriercognitive declinealzheimer’s diseasemultiple sclerosisInhibitorinhibitorinhibit

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