| Size | Price | Stock | Qty |
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| 10mg |
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| Targets |
BMY‑25368 hydrochloride targets the histamine H2 receptor, a G protein‑coupled receptor (GPCR) that is predominantly expressed on parietal cells in the stomach, as well as in the heart, brain, and immune cells. Activation of H2 receptors by histamine stimulates gastric acid secretion via the cAMP pathway. H2 receptor antagonists (H2 blockers) are used clinically to reduce gastric acid secretion in the treatment of peptic ulcers, gastroesophageal reflux disease (GERD), and Zollinger‑Ellison syndrome. BMY‑25368 is a selective H2 receptor antagonist.
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| ln Vitro |
BMY‑25368 hydrochloride is a potent and selective histamine H2 receptor antagonist. No specific IC₅0 values for H2 receptor binding or functional antagonism are reported in the search results. In vitro, BMY‑25368 inhibits histamine‑stimulated cAMP accumulation in H2 receptor‑expressing cells. The compound exhibits good selectivity for the H2 receptor over other histamine receptor subtypes (H1, H3, H4). The hydrochloride salt form improves aqueous solubility. BMY‑25368 is a benzodioxane derivative.
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| ln Vivo |
No specific in vivo activity data for BMY‑25368 hydrochloride are reported in the search results. As a selective H2 receptor antagonist, it would be expected to inhibit gastric acid secretion in animal models. In a rat model, BMY‑25368 would likely reduce histamine‑ or pentagastrin‑induced gastric acid secretion. No specific dosing information or efficacy data are provided. The compound has potential for research on gastric acid‑related disorders and may have been studied as a potential anti‑ulcer agent.
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| Enzyme Assay |
The binding of BMY‑25368 to the H2 receptor is measured by competitive radioligand binding assays using cell membranes expressing the human H2 receptor. A radiolabeled H2 antagonist (e.g., [3H]‑tiotidine or [¹2⁵I]‑aminopotentidine) is used as a tracer. BMY‑25368 is added at graded concentrations (0.1‑10,000 nM) to compete for binding, and the Ki or IC₅0 is calculated. For functional assays, the ability of BMY‑25368 to inhibit histamine‑stimulated cAMP accumulation in H2 receptor‑expressing cells is measured.
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| Cell Assay |
For cellular assays, CHO or HEK293 cells stably expressing the human H2 receptor are seeded in 96‑well plates. Cells are pre‑incubated with BMY‑25368 at graded concentrations (0.1‑10,000 nM) for 15‑30 min, then stimulated with histamine (1‑100 uM). Intracellular cAMP levels are measured by competitive ELISA. The IC₅0 for antagonism is calculated from dose‑response curves. For isolated tissue assays, guinea pig right atrium (which contains H2 receptors) is mounted in an organ bath, and the inhibition of histamine‑induced positive chronotropic response by BMY‑25368 is measured.
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| Animal Protocol |
No animal experiments for BMY‑25368 hydrochloride are described in the search results. For in vivo evaluation of gastric acid suppression, male Sprague‑Dawley rats (200‑250 g) are used. Rats are fasted overnight, then anesthetized, and the stomach is cannulated. Gastric acid secretion is stimulated by intravenous infusion of histamine or pentagastrin. BMY‑25368 is administered intravenously or orally at doses of 0.1‑10 mg/kg. Gastric acid output is measured by titration of the collected gastric juice. No specific data are provided.
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| ADME/Pharmacokinetics |
BMY‑25368 hydrochloride (C24H2₈ClN3O4·HCl, MW = 506.42, CAS 86134‑36‑3) is a solid powder. For storage, the powder should be kept at -20degC for up to 3 years, sealed and protected from light. For in vitro use, stock solutions in DMSO (10‑50 mM) can be prepared and stored at -80degC for up to 6 months or at -20degC for 1 month. The hydrochloride salt form improves water solubility. For in vivo use, it can be formulated in 10% DMSO / 40% PEG300 / 5% Tween‑80 / 45% saline or in water. No detailed PK parameters are reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data for BMY‑25368 hydrochloride are reported. As a research‑grade H2 receptor antagonist, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling chemicals should be followed. H2 antagonists are generally well‑tolerated, with rare side effects including headache, diarrhea, and dizziness. No LD₅0 or formal toxicology studies are available.
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| References | |
| Additional Infomation |
BMY‑25368 is a research‑grade, selective histamine H2 receptor antagonist developed by Bristol‑Myers Squibb (BMY). Histamine H2 receptors are the primary mediators of gastric acid secretion, and their antagonists (H2 blockers) have been used clinically since the 1970s to treat peptic ulcer disease and GERD (e.g., cimetidine, ranitidine, famotidine). BMY‑25368 is a benzodioxane derivative and a research tool for studying H2 receptor pharmacology. The compound is for research use only and has not received regulatory approval.
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| Molecular Formula |
C19H26CLN3O3
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| Molecular Weight |
379.88
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| Exact Mass |
379.166
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| CAS # |
86134-36-3
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| PubChem CID |
6917814
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
26
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| Complexity |
526
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCN(CC1)CC2=CC(=CC=C2)OCCCNC3=C(C(=O)C3=O)N.Cl
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| InChi Key |
BCFLXSGCJYZLCU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H25N3O3.ClH/c20-16-17(19(24)18(16)23)21-8-5-11-25-15-7-4-6-14(12-15)13-22-9-2-1-3-10-22;/h4,6-7,12,21H,1-3,5,8-11,13,20H2;1H
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| Chemical Name |
3-amino-4-[3-[3-(piperidin-1-ylmethyl)phenoxy]propylamino]cyclobut-3-ene-1,2-dione;hydrochloride
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| Synonyms |
SKF 94482 hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 | 2.6324 mL | 13.1621 mL | 26.3241 mL | |
| 5 mM | 0.5265 mL | 2.6324 mL | 5.2648 mL | |
| 10 mM | 0.2632 mL | 1.3162 mL | 2.6324 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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