1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. CAY10471

CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model.

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CAY10471

CAY10471 Estructura química

No. CAS : 627865-18-3

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1 mg En stock
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10 mg   Obtener un presupuesto  

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Descripciòn

CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model[1][2][3].

IC50 & Target[1]

CRTH2

 

In Vitro

CAY10471 (1 μM; 1-24 hours) decreases 15dPGJ2-induced phosphorylation of p38 MAP kinase significantly in PC12 cells[1].

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

Western Blot Analysis[1]

Cell Line: PC12 cells
Concentration: 1 μM
Incubation Time: 1 or 24 hours
Result: Blocked 15d-PGJ2-induced p38 MAP kinase activation.
In Vivo

CAY10471 (oral treatment; 2 mg/kg; challenged on day 22 or over 10 consecutive days) shows a diminished inflammation in chronic contact hypersensitivity (CHS) and IgE-CAI model. It blocks CRTH2 partly, but significantly suppresses inflammation in mice[2].
CAY10471 (oral adminstration; 20 mg/kg; twice daily; beginning 3/4/5 days before UUO) significantly attenuates interstitial collagen deposition in the cortex when compared with the vehicle (8.40% versus 14.85%). Oral administration from 3 days after UUO also significantly attenuates interstitial collagen deposition in the cortex compared with vehicle (9.63% versus 14.44%). However, oral administration beginning 5 days after UUO has little effect on interstitial collagen deposition in the cortex when compared with vehicle (14.61% versus 15.09%). Unilateral ureteral obstruction (UUO)[3].

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

Animal Model: Balb/c mice, DP−/− mice, CRTH2−/− mice[2]
Dosage: 2 mg/kg
Administration: Oral treatment; once daily; challenged on day 22 or over 10 consecutive days
Result: Significantly suppressed both CHS and IgE-CAI inflammatory responses.
Animal Model: C57BL/6 mice[3]
Dosage: 20 mg/kg
Administration: Oral treatment; twice daily; beginning 3/4/5 days before UUO
Result: Slowed the progression of renal fibrosis in the obstructed kidneys.
Peso molecular

416.47

Fòrmula

C21H21FN2O4S

No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(CN1C2=C(CC(CC2)N(C)S(=O)(C3=CC=C(C=C3)F)=O)C4=C1C=CC=C4)O.[Rotation (+)]

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvente y solubilidad
In Vitro: 

DMSO : 30 mg/mL (72.03 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 2.4011 mL 12.0057 mL 24.0113 mL
5 mM 0.4802 mL 2.4011 mL 4.8023 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación

Purity: 99.9%

Referencias

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 (sealed storage, away from moisture). 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 2.4011 mL 12.0057 mL 24.0113 mL 60.0283 mL
5 mM 0.4802 mL 2.4011 mL 4.8023 mL 12.0057 mL
10 mM 0.2401 mL 1.2006 mL 2.4011 mL 6.0028 mL
15 mM 0.1601 mL 0.8004 mL 1.6008 mL 4.0019 mL
20 mM 0.1201 mL 0.6003 mL 1.2006 mL 3.0014 mL
25 mM 0.0960 mL 0.4802 mL 0.9605 mL 2.4011 mL
30 mM 0.0800 mL 0.4002 mL 0.8004 mL 2.0009 mL
40 mM 0.0600 mL 0.3001 mL 0.6003 mL 1.5007 mL
50 mM 0.0480 mL 0.2401 mL 0.4802 mL 1.2006 mL
60 mM 0.0400 mL 0.2001 mL 0.4002 mL 1.0005 mL
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  • 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.

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Inquiry Information

Nombre del producto:
CAY10471
Cat. No.:
HY-13706A
Cantidad:
MCE Japan Authorized Agent: