
Setipiprant
An oral/topical CRTH2 (DP2) receptor antagonist that blocks the inhibitory effect of PGD2 on hair follicles. Originally developed by Pfizer/Actelion as an oral AGA drug; safe and effective for topical use in hair growth serums and scalp sprays.
Overview
Setipiprant is a highly selective CRTH2 (DP2) receptor antagonist renowned for precisely blocking the prostaglandin D2 (PGD2) pathway, hailed as “the closest-to-clinically-validated PGD2-targeting hair growth ingredient.” Through multi-targeted inhibition of PGD2 toxicity on follicles, it removes the core suppressive mechanism of androgenetic alopecia and effectively restarts and prolongs the anagen phase. Its core benefits include dramatically reducing scalp PGD2 levels, rapidly awakening dormant follicles, significantly increasing hair density and thickness, and exhibiting virtually no systemic side effects. Widely used in premium hair growth serums, scalp sprays, ampoules, and professional anti-hair loss products.
Synonyms: ACT-129968; KYTH-105; setipiprantum; 2-(2-(1-naphthoyl)-8-fluoro-1,2,3,4-tetrahydropyrido[4,3-b]indol-5-yl)aceticacid; 2-[8-fluoro-2-(naphthalene-1-carbonyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]aceticacid; 8-Fluoro-1,2,3,4-tetrahydro-2-(1-naphthalenylcarbonyl)-5H-pyrido[4,3-b]indole-5-aceticacid;2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)aceticacid
Product Categories: API; CRTH2 (DP2) Receptor Antagonists; Prostaglandin D2 Receptor Antagonists; PGD2 Pathway Inhibitors
Mol File: 866460-33-5.mol
Physicochemical Properties
Boiling point: 690.4±55.0 °C(Predicted)
Density: 1.37±0.1 g/cm3(Predicted)
Storage temp.: Store at -20°C
Solubility: DMSO:48.67(Max Conc. mg/mL);120.94(Max Conc. mM); DMF:50.0(Max Conc. mg/mL);124.25(Max Conc. mM); DMF:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.24(Max Conc. mM); Ethanol:3.0(Max Conc. mg/mL);7.45(Max Conc. mM)
Form: Solid
Color: Light yellow to yellow
MSDS Information
Experimental Data
1.Cell Experiment
Solubility in DMSO: ≥ 36 mg/mL (89.46 mM; Hygroscopic DMSO significantly affects the solubility of the product, please use freshly opened DMSO)
* "≥" means soluble, but saturation unknown.
Preparing Stock Solutions:

Please choose a suitable solvent to prepare the stock solution based on the product's solubility in different solvents. Once the solution is prepared, aliquot and store it to avoid product degradation caused by repeated freeze-thaw cycles.
Storage conditions and shelf life of the stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, use within 2 years; when stored at -20°C, use within 1 year.
2.Animal Experiment
Please choose the appropriate dissolution method based on your experimental animals and administration route.
For the following dissolution solutions, please first prepare a clear stock solution according to the In Vitro method, then add solubilizers in sequence:
—— To ensure the reliability of the experimental results, the clear stock solution can be appropriately stored based on storage conditions; for in vivo experimental working solutions, it is recommended to prepare them fresh and use them on the same day;
The percentages shown before each solvent below refer to the volume proportion of that solvent in the final solution you are preparing; if precipitation or crystallization occurs during preparation, solubilization can be assisted by heating and/or ultrasonic treatment.
Protocol 1
Please add each solvent in order: 10% DMSO, 40% PEG300, 5% Tween-80, 45% Saline
Solubility: ≥ 2.5 mg/mL (6.21 mM); clear solution
This protocol can achieve a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Using 1 mL of working solution as an example, take 100 μL of a 25.0 mg/mL clear DMSO stock solution and add it to 400 μL of PEG300, then mix well; next, add 50 μL of Tween-80 to the above mixture and mix thoroughly; then continue by adding 450 μL of saline and adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in ddH₂O and adjust the volume to 100 mL to obtain a clear, transparent saline solution.
Pharmacodynamics
Mechanism Of Action
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