DY 268 |
Catalog No.GC46012
One-Click Copy Product Info
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DY 268 is apotent farnesoid X receptor (FXR) antagonist with an IC50 value of 7.5nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1609564-75-1
Sample solution is provided at 25 µL, 10mM.
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DY 268 is a potent farnesoid X receptor (FXR) antagonist with an IC50 value of 7.5nM[1]. DY 268 elevates endogenous bile acid levels by inhibiting the FXR signaling pathway, increasing bile acid synthesis, and reducing bile acid excretion, thereby inducing preterm birth in pregnant mice[2]. DY 268 has been widely used to alleviate the morphological damage and intestinal dysfunction caused by the spike protein of SARS-CoV-2 in preclinical models[3].
In vitro, pretreatment of BV2 cells with DY 268 (10µM) for 0.5h abolished the inhibitory effects of Methyl dichloroacetate (MD) on NLRP3 and COX2, reversed the inhibitory effect of MD on NF-κB transcriptional activity, and exacerbated lipopolysaccharide (LPS)-induced cell damage[4]. Treatment with 1μM DY 268 for 48 hours promoted cell senescence and inhibited the expression of alkaline phosphatase (ALP) in RAW264.7 cells[5]. Incubation with 10μM DY 268 for 48 hours reduced the constitutive expression of bile salt efflux pump (BSEP) mRNA in HepaRG cells[6]. 5μM of DY 268 treatment of HIEC-6 cells for 48 hours blocked the downregulation of pro-inflammatory cytokine mRNA and protein levels induced by Taxifolin (TAX) (60μM), reversed the inhibition of the NLRP3 inflammasome complex induced by TAX, and decreased the expression of barrier and antioxidant-related genes as well as tight junction proteins under γ-ray irradiation condition[7].
In vivo, DY 268 treatment via oral administration at a dose of 10mg/kg, twice a day for three days, reduced the Ubiquitin specific peptidase 2b (USP2b) mRNA and protein expression in the livers of C57BL/6J mice[8]. Intragastric administration of DY 268 at a dose of 20mg/kg every 2 days for 4 weeks inhibited oat β-glucan-induced gallstone formation in mice[9].
References:[1] Donna D Y, Lin W, Forman B M, et al. Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor[J]. Bioorganic & medicinal chemistry, 2014, 22(11): 2919-2938.
[2] You S, Cui A M, Hashmi S F, et al. Dysregulation of bile acids increases the risk for preterm birth in pregnant women[J]. Nature communications, 2020, 11(1): 2111.
[3] Lopes A L F, da Silva Araújo A K, de Sousa Chaves L, et al. Farnesoid X receptor blockade attenuates morphological damage, intestinal secretion, and prevents mucus loss induced by SARS-CoV-2 spike protein in the mouse intestine[J]. Journal of Pharmacy and Pharmacology, 2026, 78(7): rgag074.
[4] Jia Y, Li Q, Xu X, et al. Methyl dichloroasterrate alleviates lipopolysaccharide-induced neuroinflammation and depression-like behaviors in mice by upregulating FXR expression[J]. International Immunopharmacology, 2026, 185: 117009.
[5] Deng X, Lin B, Xiao W, et al. Specnuezhenide alleviates senile osteoporosis by activating TGR5/FXR signaling in bone marrow mesenchymal stem cells and RANKL-induced osteoclasts[J]. Drug design, development and therapy, 2025: 1595-1608.
[6] Tastet V, Le Vée M, Carteret J, et al. Repression of bile salt efflux pump expression by tri-ortho-cresyl phosphate in cultured human hepatic cells[J]. Toxicology in Vitro, 2025, 105: 106021.
[7] Lyu B, Xu F, Wang Z, et al. Taxifolin ameliorates radiation-induced colitis via the gut microbiota–BAs–FXR/NLRP3 axis[J]. Phytomedicine, 2026: 158675.
[8] Ali W, Nadolny C, Zhang X, et al. Transcriptional regulation of ubiquitin specific peptidase 2b by farnesoid X receptor and its implications in the pathogenesis of hepatocellular carcinoma[J]. American Journal of Cancer Research, 2026, 16(8): 3660.
[9] Tian L, Lin Y, Yue P, et al. Oat β‐Glucan and Galactooligosaccharides Influence Gallstone Formation by Modulating the Gut Microbiota, Particularly Desulfovibrionales[J]. iMetaMed, 2026, 2(1): e70029.
| Cell experiment [1]: | |
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Cell lines |
HepG2 cells |
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Preparation Method |
HepG2 cells were cultured in DMEM medium supplemented with 10% inactivated fetal bovine serum and 1% penicillin-streptomycin at 37°C, in a humidified atmosphere containing 5% CO2. Tissue factor activity was assessed via generation of coagulation factor Xa (FXa) after exposure of HepG2 cells to 600µM chenodeoxycholic acid (CDCA) for 24h with and without the addition of the 10µM DY 268. |
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Reaction Conditions |
10µM; 24h |
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Applications |
DY 268 treatment inhibited CDCA-induced the increase of tissue factor in HepG2 cells. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6J mice |
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Preparation Method |
C57BL/6J mice were housed in a free-noise room under well-controlled conditions (Room temperature 25±4°C, humidity 48±5%) and were allowed to be acclimatized for at least 7 days before any experimental manipulation. Mice were fed a regular chow diet and treated with vehicle (1,2-propanediol), or DY 268 (10mg/kg) twice a day for three days via oral gavage. Liver samples were collected for analysis. |
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Dosage form |
10mg/kg; twice a day; 3 days; p.o. |
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Applications |
DY 268 treatment reduced the USP2b mRNA and protein expression in the livers of mice. |
| References: [1] Greimel T, Jahnel J, Pohl S, et al. Bile acid-induced tissue factor activity in hepatocytes correlates with activation of farnesoid X receptor[J]. Laboratory Investigation, 2021, 101(10): 1394-1402. [2] Ali W, Nadolny C, Zhang X, et al. Transcriptional regulation of ubiquitin specific peptidase 2b by farnesoid X receptor and its implications in the pathogenesis of hepatocellular carcinoma[J]. American Journal of Cancer Research, 2026, 16(8): 3660. | |
| Cas No. | 1609564-75-1 | SDF | |
| Chemical Name | 1-[(3-methoxyphenyl)methyl]-N-[4-methyl-3-(4-morpholinylsulfonyl)phenyl]-3-(4-methylphenyl)-1H-pyrazole-4-carboxamide | ||
| Canonical SMILES | CC(C=C1)=CC=C1C2=NN(CC3=CC=CC(OC)=C3)C=C2C(NC4=CC=C(C)C(S(N5CCOCC5)(=O)=O)=C4)=O | ||
| Formula | C30H32N4O5S | M.Wt | 560.7 |
| Solubility | DMSO : 50 mg/mL (89.18 mM; ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7835 mL | 8.9174 mL | 17.8348 mL |
| 5 mM | 356.7 μL | 1.7835 mL | 3.567 mL |
| 10 mM | 178.3 μL | 891.7 μL | 1.7835 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)