2. Immunology/Inflammation GPCR/G Protein
  3. Interleukin Related Adenosine Receptor
  4. FK3453

FK3453 is a dual adenosine A1/A2 inhibitor and a TSLP inhibitor. FK3453 is also a substrate of aldehyde oxidase (AO). FK3453 can inhibit the production of TSLP and IL-33. FK3453 is useful for research on Parkinson’s disease and allergic disorders.

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FK3453

FK3453 Chemical Structure

CAS No. : 560111-91-3

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FK3453 Related Antibodies

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Description

FK3453 is a dual adenosine A1/A2 inhibitor and a TSLP inhibitor. FK3453 is also a substrate of aldehyde oxidase (AO). FK3453 can inhibit the production of TSLP and IL-33. FK3453 is useful for research on Parkinson’s disease and allergic disorders[1][2][3].

In Vitro

FK3453 (1-10 µM; 0-24 h) inhibits constitutive TSLP production in KCMH-1 mouse keratinocytes in a concentration-dependent manner without reducing cell viability[2].
FK3453 (1-10 µM; 4.5 h) inhibits TSLP mRNA expression in PAM212 mouse keratinocytes treated with TPA (HY-18739)[2].
FK3453 (1-10 µM; 4.5-24.5 h) inhibits T4FP-induced and TPA-induced TSLP mRNA expression in NHEKs, as well as TPA-induced IL-33 mRNA expression[2].

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

FK3453 Related Antibodies

RT-PCR[2]

Cell Line: PA (HY-18739) treated PAM212 cells
Concentration: 1, 3 and 10 μM
Incubation Time: Pretreated with 30 min, then co-incubation for 4 h
Result: Reduced the levels of TSLP mRNA in a ntration-dependent manner.
Parmacokinetics
Species Dose Route T1/2β Vdss AUCinf CLt Cmax Tmax F AUC0-∞ T1/2 AUC CL
Rat[1] 3.2 mg/kg i.v. / / / 10.8 mL/min/kg / / / / 0.4 h / /
Rat[1] 3.2 mg/kg p.o. / / / / 544 ng/mL / 34.6 % / / 1789.4 ng·h/mL 29.8 mL/min/kg
Rat[3] 0.1 (male) mg/kg i.v. 0.95 h 0.69 L/kg 111.9 ng·h/mL 14.9 mL/min/kg / / / / / / /
Rat[3] 0.32 (male) mg/kg i.v. 0.50 h 0.91 L/kg 304.1 ng·h/mL 17.6 mL/min/kg / / / / / / /
Rat[3] 3.2 (male) mg/kg i.v. 0.37 h 0.48 L/kg 5170.3 ng·h/mL 10.8 mL/min/kg / / / / / / /
Rat[3] 0.1 (male) mg/kg p.o. / / 34.2 ng·h/mL / 41.0 ng/mL 0.5 h 30.5 % / / / /
Rat[3] 0.32 (male) mg/kg p.o. / / 127.4 ng·h/mL / 36.8 ng/mL 1.5 h 41.9 % / / / /
Rat[3] 3.2 (male) mg/kg p.o. / / / / 544.0 ng/mL 1.0 h 34.6 % 1789.4 ng·h/mL / / /
Rat[3] 0.1 (female) mg/kg i.v. 0.73 h 0.96 L/kg 124.2 ng·h/mL 14.1 mL/min/kg / / / / / / /
Rat[3] 1 (female) mg/kg i.v. 2.77 h 0.77 L/kg 4987.2 ng·h/mL 7.8 mL/min/kg / / / / / / /
Rat[3] 1 (female) mg/kg p.o. / / 3372.4 ng·h/mL / 373.3 ng/mL 1.7 h 67.6 % / / / /
In Vivo

FK3453 (0.3 mM; intracavitary injection; single dose) suppresses TSLP production and reduces the weight of exudate fluid in the air pouch model of inflammation induced by LPS (HY-D1056) in ICR mice[2].

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

Animal Model: ICR mice (five-week-old male, lipopolysaccharide-induced air pouch-type inflammation model)[2]
Dosage: 0.3 mM
Administration: local injection into air pouch; single dose
Result: Significantly inhibited LPS-induced increases in TSLP protein levels in pouch fluid and TSLP mRNA levels in pouch wall tissues.
Strongly decreased the weight of pouch fluids.
Molecular Weight

307.35

Formula

C17H17N5O
CAS No.
SMILES

O=C1C=CC(C2=C(C3=CC=CC=C3)N=C(N)N=C2)=NN1C(C)C
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
References
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FK3453 Related Classifications

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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:

FK3453560111-91-3FK 3453FK-3453Interleukin RelatedAdenosine ReceptorILP1 receptorAOICR miceParkinson’s diseaseallergic diseaseslpaair pouch-type inflammationInhibitorinhibitorinhibit

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