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300266 DP2 Antagonist II - Calbiochem

300266
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Overview

Replacement Information

Products

Catalogue NumberPackaging Qty/Pack
300266-2MG Glass bottle 2 mg
Description
OverviewThe (R) enantiomer of a cell-permeable alkynylphenoxyacetic acid that acts as a high affinity antagonist against the G protein-coupled PGD2 (Cat. No. 538909) receptor CRTH2/DP2 (Ki = 5.3 and 5.0 nM against human & murine DP2, respectively), exhibiting much reduced potency against a panel of more than 50 other receptors and ion channels. Effectively inhibits DP2-dependent chemotaxis of primary human eosinophils (IC50 = 100 nM). Exhibits higher Caco-2 permeability than DP2 Antagonist I (Cat. No. 300264), but less oral bioavailability in mice.
Catalogue Number300266
Brand Family Calbiochem®
Synonyms(R)-(5-Chloro-1'-(5-chloro-2-fluorobenzyl)-2,2',5'-trioxospiro(indole-3,3→-pyrrolidin)-1(2H)-yl)acetic acid, CRTH2 Antagonist II, GPR44 Antagonist II
References
ReferencesCrosignani, S., et al. 2008. J Med Chem. 51, 2227.
Product Information
FormWhite powder
Hill FormulaC₂₀H₁₃Cl₂FN₂O₅
Chemical formulaC₂₀H₁₃Cl₂FN₂O₅
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetDP2
Primary Target K<sub>i</sub>5.3 nM
Purity≥93% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Yes
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

References

Reference overview
Crosignani, S., et al. 2008. J Med Chem. 51, 2227.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision12-April-2013 JSW
Synonyms(R)-(5-Chloro-1'-(5-chloro-2-fluorobenzyl)-2,2',5'-trioxospiro(indole-3,3→-pyrrolidin)-1(2H)-yl)acetic acid, CRTH2 Antagonist II, GPR44 Antagonist II
DescriptionThe (R) enantiomer of a cell-permeable alkynylphenoxyacetic acid that acts as a high affinity antagonist against the G protein-coupled PGD2 (Cat. No. 538909) receptor CRTH2/DP2 (Ki = 5.3 and 5.0 nM against 1.5 nM PGD2 for human & murine DP2 binding, respectively), exhibiting much reduced or little potency against a panel of more than 50 other receptors and ion channels, including PGD2 receptor DP1, PGE receptors (EP2, EP3, EP4), and PGF receptor FP (IC50 >30 µM). Effectively inhibits DP2-dependent chemotaxis of primary human eosinophils (IC50 = 100 nM; chemotractant = 100 nM DK-PGD2) in vitro. Shown to exhibit higher Caco-2 permeability than DP2 Antagonist I (Cat. No. 300264; Papp in unit of 10-6 cm/s = 26.4 vs. 5.2, respectively), but less oral bioavailability (32% in rat for Inhibitor II vs. 80% in mice for Inhibitor I with same oral dosage of 5 mg/kg).
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₀H₁₃Cl₂FN₂O₅
Structure formulaStructure formula
Purity≥93% by HPLC
SolubilityDMSO (100 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Yes
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesCrosignani, S., et al. 2008. J Med Chem. 51, 2227.