2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. BI-671800

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

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Solid + Solvent
10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

BI-671800 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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)

mCRTH2

3.7 μM (IC50)

In Vitro

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

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

BI-671800 Related Antibodies
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].

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

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.
Clinical Trial
Molecular Weight

501.50

Formula

C25H26F3N5O3
CAS No.
Appearance

Solid

Color

White to off-white

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.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 135 mg/mL (269.19 mM; Need ultrasonic; 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 1.9940 mL 9.9701 mL 19.9402 mL
5 mM 0.3988 mL 1.9940 mL 3.9880 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    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

    This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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 (protect from light). 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 1.9940 mL 9.9701 mL 19.9402 mL 49.8504 mL
5 mM 0.3988 mL 1.9940 mL 3.9880 mL 9.9701 mL
10 mM 0.1994 mL 0.9970 mL 1.9940 mL 4.9850 mL
15 mM 0.1329 mL 0.6647 mL 1.3293 mL 3.3234 mL
20 mM 0.0997 mL 0.4985 mL 0.9970 mL 2.4925 mL
25 mM 0.0798 mL 0.3988 mL 0.7976 mL 1.9940 mL
30 mM 0.0665 mL 0.3323 mL 0.6647 mL 1.6617 mL
40 mM 0.0499 mL 0.2493 mL 0.4985 mL 1.2463 mL
50 mM 0.0399 mL 0.1994 mL 0.3988 mL 0.9970 mL
60 mM 0.0332 mL 0.1662 mL 0.3323 mL 0.8308 mL
80 mM 0.0249 mL 0.1246 mL 0.2493 mL 0.6231 mL
100 mM 0.0199 mL 0.0997 mL 0.1994 mL 0.4985 mL
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BI-671800 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:

BI-6718001093108-50-9BI671800BI 671800Prostaglandin ReceptorInhibitorinhibitorinhibit

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