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  3. BI-671800

BI-671800 

Cat. No.: HY-114141 Purity: 99.06%
Handling Instructions

BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has potential for the treatment of poorly controlled asthma.

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

BI-671800 Chemical Structure

BI-671800 Chemical Structure

CAS No. : 1093108-50-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 309 In-stock
Estimated Time of Arrival: December 31
5 mg USD 280 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2650 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Technical Information

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  • References

Description

BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively[1]. BI-671800 has potential for the treatment of poorly controlled asthma[2].

IC50 & Target[1]

hCRTH2

4.5 nM (IC50, in CRTH2 transfected cells)

mCRTH2

3.7 nM (IC50, in CRTH2 transfected cells)

In Vitro

BI-671800 (compound A) exhibits low nM potency as an antagonist of human or mouse CRTH2 in transfected cells[1].

In Vivo

BI-671800 (compound A, 0.1-10 mg/kg, i.g.) shows significant inhibition of AHR in mice[1].
BI-671800 (compound A), effectively blocks edema formation and greatly reduces the inflammatory infiltrate and skin pathology observed in drug vehicle-treated animals[3].

Animal Model: 6-8-week-old age- and sex-matched BALB/c mice (mice were sensitized for 14 days, challenged intranasally)[1].
Dosage: 10-0.1 mg/kg
Administration: Oral gavage for 4 weeks
Result: Shows significant inhibition of AHR in mice.
Storage

4°C, protect from light

Solvent & Solubility
In Vitro: 

DMSO : 135 mg/mL (269.19 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9940 mL 9.9701 mL 19.9402 mL
5 mM 0.3988 mL 1.9940 mL 3.9880 mL
10 mM 0.1994 mL 0.9970 mL 1.9940 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.25 mg/mL (4.49 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.25 mg/mL (4.49 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Molecular Weight

501.50

Formula

C₂₅H₂₆F₃N₅O₃

CAS No.

1093108-50-9

SMILES

O=C(O)CC1=C(N(C)C)N=C(CC2=CC=C(NC(C3=CC=C(C(F)(F)F)C=C3)=O)C=C2)N=C1N(C)C

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
BI-671800
Cat. No.:
HY-114141
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BI-671800

Cat. No.: HY-114141