| Size | Price | Stock | Qty |
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| 1mg |
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| Targets |
L-888,291 targets the prostaglandin D2 receptor subtype 1 (DP1) and the thromboxane receptor (TP). DP1 is a G protein-coupled receptor that is activated by prostaglandin D2 (PGD2), a lipid mediator involved in allergic inflammation and vasodilation. L-888,291 acts as a selective antagonist at DP1, with a Ki of 132 nM, and also shows activity at TP, with a Ki of 17 nM. L-888,291 is the racemate of L-888607.
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| ln Vitro |
L 888607 racemate (compound 3) is really eight times more powerful at the TP receptor (Ki = 17 nM) than it is at the DP1 receptor (Ki = 132 nM), while maintaining a low binding affinity for that receptor [1].
In vitro, L-888,291 binds to DP1 and TP receptors with the indicated affinities. The compound inhibits DP1-mediated signaling, as measured by cAMP accumulation or other downstream readouts. L-888,291 is a synthetic ligand that has been studied for its interactions with various receptors. Its activity at DP1 and TP makes it a valuable tool for studying prostaglandin D2 signaling. |
| ln Vivo |
In vivo, L-888,291 has been studied for its potential in inflammatory and allergic conditions. As a DP1 antagonist, it may modulate PGD2-mediated effects on inflammation and vasodilation. However, specific in vivo efficacy data are limited in the available literature. L-888,291 is primarily used as a research tool for studying DP1 receptor pharmacology.
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| Enzyme Assay |
The non-cellular assay for L-888,291 involves measuring its binding affinity for DP1 and TP receptors using radioligand binding assays. Membrane preparations from cells expressing DP1 or TP receptors are incubated with a radiolabeled receptor ligand (such as [³H]-PGD2 for DP1 or [³H]-SQ-29,548 for TP) and varying concentrations of L-888,291. The inhibition of radioligand binding is measured, and the Ki is determined from competition curves.
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| Cell Assay |
The cellular assay for L-888,291 involves treating cells expressing DP1 receptors with the compound and measuring its effects on receptor-mediated signaling. Cells are pre-incubated with L-888,291, and the inhibition of agonist-induced cAMP accumulation is measured using a competitive immunoassay. The IC50 is determined from concentration-response curves.
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| Animal Protocol |
In the in vivo efficacy study, L-888,291 is administered to animal models of allergic inflammation or thrombosis. The compound is typically administered by injection or oral gavage. Inflammatory markers, vascular function, and other relevant endpoints are measured to assess the compound's effects. However, specific published protocols for L-888,291 are limited.
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| ADME/Pharmacokinetics |
L-888,291 has a molecular weight of 375.84 and a molecular formula of C₁₉H₁₅ClFNO₂S. The compound is a synthetic organic compound. It should be stored as a powder at -20°C, protected from light and moisture. L-888,291 should be handled with appropriate laboratory safety precautions. The compound is soluble in DMSO and other organic solvents.
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| Toxicity/Toxicokinetics |
The toxicological profile of L-888,291 has not been extensively characterized in the published literature. As a DP1 and TP receptor ligand, it may affect inflammation, vascular function, and platelet aggregation. Comprehensive toxicology data are limited, and L-888,291 is not approved for clinical use. The compound should be handled with appropriate laboratory safety precautions.
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| References | |
| Additional Infomation |
L-888,291 is a synthetic ligand that has been studied for its interactions with DP1 and TP receptors. It is the racemate of L-888607 and is used as a research tool for studying prostaglandin D2 signaling and thromboxane receptor function. L-888,291 is not approved for clinical use and is strictly a research compound.
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| Molecular Formula |
C19H15CLFNO2S
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|---|---|
| Molecular Weight |
375.84
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| Exact Mass |
375.05
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| CAS # |
1030017-51-6
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| Related CAS # |
L 888607;860033-06-3;(R)-L 888607;2446042-90-4
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| PubChem CID |
44450494
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.547
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
502
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GSBAVONRPNJJOH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H15ClFNO2S/c20-12-1-4-14(5-2-12)25-19-15-6-3-13(21)10-16(15)22-8-7-11(18(19)22)9-17(23)24/h1-6,10-11H,7-9H2,(H,23,24)
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| Chemical Name |
2-[4-(4-chlorophenyl)sulfanyl-7-fluoro-2,3-dihydro-1H-pyrrolo[1,2-a]indol-3-yl]acetic acid
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| Synonyms |
L888,291; L 888,291; L-888,291
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~6 mg/mL (~15.96 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.6 mg/mL (1.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.6 mg/mL (1.60 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.6 mg/mL (1.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6607 mL | 13.3035 mL | 26.6071 mL | |
| 5 mM | 0.5321 mL | 2.6607 mL | 5.3214 mL | |
| 10 mM | 0.2661 mL | 1.3304 mL | 2.6607 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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