| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg | |||
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| Targets |
EP1 receptor, a Gq-coupled prostanoid receptor activated by PGE2. EP1-antanoist-1 binds competitively to the orthosteric site, preventing PGE2 binding and subsequent Gq/PLC-β activation, IP3 production, and intracellular Ca2+ release. It does not affect other EP subtypes (EP2, EP3, EP4) or TP receptors at concentrations up to 10 µM, demonstrating selectivity. This distinguishes it from non-selective NSAIDs.
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| ln Vitro |
In vitro, EP1-antanoist-1 inhibits PGE2-induced calcium flux in HEK-293 cells expressing human EP1 with an IC50 of approximately 3 nM (pIC50 8.5). In functional assays, it blocks PGE2-induced contraction of guinea pig ileum and human myometrium with pA2 values >8.0. It has no agonist activity at EP1 and does not affect EP2-mediated cAMP production. Its binding affinity (pKi 7.54) is consistent with its functional potency.
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| ln Vivo |
In vivo, EP1-antanoist-1 has been tested in rodent models of inflammatory pain. Oral administration (1–10 mg/kg) reduces carrageenan-induced mechanical hyperalgesia and formalin-induced nociceptive behavior. It also attenuates PGE2-induced fever in rats. In models of colitis, it reduces visceral hypersensitivity and colonic inflammation. These effects are consistent with EP1 blockade, supporting the receptor's role in pain and inflammation.
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| Enzyme Assay |
Cell-free binding assays use membranes from HEK-293 cells expressing human EP1. Incubate with [3H]PGE2 (0.5 nM) and increasing concentrations of EP1-antanoist-1 (0.01–1000 nM) in a buffer containing 50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4. Nonspecific binding defined with 10 µM PGE2. After 2 h at room temperature, filter through GF/B filters and count radioactivity. Ki is calculated from Cheng-Prusoff equation.
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| Cell Assay |
Functional assays use HEK-293 cells stably expressing human EP1 and aequorin or Fluo-4. Cells are loaded with calcium indicator and placed in a plate reader. Increasing concentrations of EP1-antanoist-1 are added, then PGE2 (EC80 concentration) is added to stimulate calcium release. The inhibition of calcium signal is plotted and IC50 determined. Selectivity is confirmed by testing against EP2, EP3, EP4, and TP receptors in similar assays.
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| Animal Protocol |
In vivo, EP1-antanoist-1 is suspended in 0.5% methylcellulose and administered orally (1, 3, 10 mg/kg) to male Sprague-Dawley rats 1 h before intraplantar injection of carrageenan (1% in saline). Paw withdrawal threshold to mechanical stimulation is measured using von Frey filaments at 0, 2, 4, 6 h. In the formalin test, compound is given 30 min before intraplantar formalin injection, and licking/biting time is recorded in the early and late phases. Plasma concentrations can be measured by LC-MS.
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| ADME/Pharmacokinetics |
Molecular formula C19H15BrCl2N2O3, MW 470.14. Appearance: solid. Solubility: DMSO (≥10 mg/mL). Storage: powder at -20°C for 3 years. Purity >98%. For in vivo, suspension in 0.5% methylcellulose + 0.1% Tween-80. LogP ~4.8, high protein binding. Half-life in rats after oral dosing ~3 h.
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| Toxicity/Toxicokinetics |
No published toxicology data. At doses up to 10 mg/kg in rodents, no overt toxicity observed. As an EP1 antagonist, potential side effects include interference with renal function and gastric mucosal protection, though EP1 is less involved than EP3/EP4. Standard safety pharmacology studies are needed.
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| References | |
| Additional Infomation |
Research compound, not approved for clinical use. It is a highly useful tool for studying EP1-mediated processes, particularly in pain, inflammation, and cancer (where EP1 promotes tumor growth). It has been used in combination with COX-2 inhibitors to delineate downstream pathways. No clinical trials have been initiated.
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| Molecular Formula |
C19H15BRCL2N2O3
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|---|---|
| Molecular Weight |
470.144002199173
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| Exact Mass |
467.964
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| CAS # |
851204-35-8
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| PubChem CID |
11340370
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| Appearance |
White to off-white solid powder
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| LogP |
5.5
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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 |
6
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| Heavy Atom Count |
27
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| Complexity |
515
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=C(C)N(CC2C(OCC3C(Cl)=CC(Cl)=CC=3)=CC=C(Br)C=2)N=1)O
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| InChi Key |
XBECMWNKXTURNS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H15BrCl2N2O3/c1-11-6-17(19(25)26)23-24(11)9-13-7-14(20)3-5-18(13)27-10-12-2-4-15(21)8-16(12)22/h2-8H,9-10H2,1H3,(H,25,26)
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| Chemical Name |
1-[[5-bromo-2-[(2,4-dichlorophenyl)methoxy]phenyl]methyl]-5-methylpyrazole-3-carboxylic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1270 mL | 10.6351 mL | 21.2703 mL | |
| 5 mM | 0.4254 mL | 2.1270 mL | 4.2541 mL | |
| 10 mM | 0.2127 mL | 1.0635 mL | 2.1270 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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