| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
EP4 7.6 (pKd)
BGC-20-1531 specifically targets the Prostaglandin E2 (PGE2) receptor subtype EP4, which is a G-protein-coupled receptor (GPCR). The EP4 receptor plays a key role in mediating pain, inflammation, and other physiological processes in response to PGE2. By antagonizing EP4, BGC-20-1531 blocks PGE2-driven signaling. |
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| ln Vitro |
Human middle cerebral (pKb=7.8) and meningeal (pKb=7.6) arteries' PGE2-induced vasodilatation was competitively inhibited by BGC-20-1531 free base, whereas PGE2-induced responses in coronary, pulmonary, or renal arteries were unaffected[1].
BGC-20-1531 demonstrates potent and selective inhibitory activity against the EP4 receptor, with a pKB value of 7.6 (KB ~ 25 nM). This indicates a strong functional antagonism. It exhibits high selectivity for EP4 over other prostanoid receptors (EP1, EP2, EP3, DP, FP, IP, TP), making it a valuable tool for studying specific EP4-mediated pathways. |
| ln Vivo |
The dose-dependent inhibition of PGE2-induced increase in canine carotid blood flow is caused by BGC-20-1531 free base (1-10 mg/kg; iv)[1].
In vivo, BGC-20-1531 free base has shown potential for research into migraine headache. The specific activity includes the ability to attenuate PGE2-induced thermal hyperalgesia and mechanical allodynia in pre-clinical animal models. These effects are consistent with the role of EP4 receptors in sensitizing peripheral nociceptors. |
| Enzyme Assay |
The specific in vitro protocol for assessing EP4 receptor binding would utilize a radioligand binding assay. HEK-293 or CHO cells stably expressing the human EP4 receptor are harvested and homogenized to prepare membrane fractions. The membranes are then incubated with [3H]-PGE2 and increasing concentrations of BGC-20-1531. After incubation, bound and free radioligands are separated by filtration, and the radioactivity is measured to calculate Ki or IC50.
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| Cell Assay |
In a functional cellular assay, HEK-293 cells stably transfected with the human EP4 receptor and a CRE-luciferase reporter gene are used. The cells are seeded in 96-well plates and cultured overnight. After serum starvation, cells are pre-incubated with various concentrations of BGC-20-1531 (0.1-10,000 nM) for 30 minutes, then stimulated with PGE2. After 4-6 hours of incubation, luciferase activity is measured as a proxy for cAMP-mediated signaling, and the pKB is calculated from the rightward shift of the PGE2 concentration-response curve.
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| Animal Protocol |
Animal/Disease Models: Beagle dogs[1]
Doses: 1- 10 mg/kg Route of Administration: Iv Experimental Results: Caused a dose-dependent antagonism of the PGE2-induced increase in canine carotid blood flow. A standard in vivo protocol for migraine research uses a rat or mouse model of PGE2-induced hyperalgesia. Male Sprague-Dawley rats are injected with PGE2 (1 ug) intraplantarly into the hind paw to induce thermal hyperalgesia and mechanical allodynia. BGC-20-1531 is administered orally or intraperitoneally at doses of 3-30 mg/kg, 30 minutes before PGE2 challenge. Paw withdrawal latency (radiant heat) and withdrawal threshold (von Frey filaments) are measured at baseline and multiple times post-injection to evaluate the reversal of PGE2-induced hypersensitivity by the antagonist. |
| ADME/Pharmacokinetics |
Detailed pharmacokinetic parameters for BGC-20-1531 in published literature are limited. As a small molecule EP4 antagonist, it is designed for oral bioavailability. Standard PK parameters for this class include moderate clearance and moderate volume of distribution. The compound is likely metabolized by hepatic CYP enzymes. Exact values for Tmax, half-life, and oral bioavailability for this specific formulation are not present in standard chemical databases.
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| Toxicity/Toxicokinetics |
Specific toxicological data for BGC-20-1531 has not been published in standard reference databases. As a preclinical research compound, standard safety profiling would be expected to assess any cytotoxic effects on primary cell lines (e.g., hepatocytes) and potential off-target receptor interactions. In a research context, the selectivity profile suggests a low risk of broad systemic toxicity, though detailed LD50 or NOAEL values are not provided.
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| References | |
| Additional Infomation |
See also: Bgc-20-1531 (Note has been moved).
BGC-20-1531 is exclusively a research tool and has not been approved by the FDA or other regulatory agencies for clinical use. It is a highly valuable EP4 antagonist tool compound for investigating the role of PGE2 signaling via EP4 in pain, inflammation, and cancer biology. The free base formulation refers to the non-salt active form of the compound. |
| Molecular Formula |
C26H24N2O6S
|
|---|---|
| Molecular Weight |
492.5436
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| Exact Mass |
492.135
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| CAS # |
736183-35-0
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| Related CAS # |
BGC-20-1531 hydrochloride;1962928-26-2
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| PubChem CID |
18444613
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| Appearance |
Light yellow to brown solid powder
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| LogP |
4.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
35
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| Complexity |
794
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1=C([H])C([H])=C([H])C([H])=C1C([H])([H])[H])(N([H])C(C1=C([H])C(C([H])([H])OC2C([H])=C([H])C(C3C([H])=C([H])C(=C([H])N=3)OC([H])([H])[H])=C([H])C=2[H])=C(C([H])([H])[H])O1)=O)(=O)=O
|
| InChi Key |
IXDVRRPNWPOPGV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H24N2O6S/c1-17-6-4-5-7-25(17)35(30,31)28-26(29)24-14-20(18(2)34-24)16-33-21-10-8-19(9-11-21)23-13-12-22(32-3)15-27-23/h4-15H,16H2,1-3H3,(H,28,29)
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| Chemical Name |
4-[[4-(5-methoxypyridin-2-yl)phenoxy]methyl]-5-methyl-N-(2-methylphenyl)sulfonylfuran-2-carboxamide
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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: 250 mg/mL (507.57 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0303 mL | 10.1515 mL | 20.3029 mL | |
| 5 mM | 0.4061 mL | 2.0303 mL | 4.0606 mL | |
| 10 mM | 0.2030 mL | 1.0151 mL | 2.0303 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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